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Volumn , Issue , 2009, Pages 1-389

A pharmacology primer: Theory, application and methods

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EID: 85133558537     PISSN: None     EISSN: None     Source Type: Book    
DOI: 10.1016/B978-0-12-374585-9.X0001-1     Document Type: Book
Times cited : (77)

References (282)
  • 2
    • 0017065767 scopus 로고
    • Blockade of histamine-induced contractions of intestinal smooth muscle by irreversibly acting agents
    • Kenakin T.P., Cook D.A. Blockade of histamine-induced contractions of intestinal smooth muscle by irreversibly acting agents. Can. J. Physiol. Pharmacol. 1976, 54:386-392.
    • (1976) Can. J. Physiol. Pharmacol. , vol.54 , pp. 386-392
    • Kenakin, T.P.1    Cook, D.A.2
  • 4
    • 71749103928 scopus 로고
    • Cyclic nucleotides and cell function
    • H. P. Publishing, New York, G. Weissman, R. Claiborne (Eds.)
    • Goldberg N.D. Cyclic nucleotides and cell function. Cell membranes, biochemistry, cell biology, and pathology 1975, 185-202. H. P. Publishing, New York. G. Weissman, R. Claiborne (Eds.).
    • (1975) Cell membranes, biochemistry, cell biology, and pathology , pp. 185-202
    • Goldberg, N.D.1
  • 5
    • 0018909079 scopus 로고
    • Is prenalterol (H 133/80) really a selective beta-1 adrenoceptor agonist? Tissue selectivity resulting from differences in stimulus-response relationships
    • Kenakin T.P., Beek D. Is prenalterol (H 133/80) really a selective beta-1 adrenoceptor agonist? Tissue selectivity resulting from differences in stimulus-response relationships. J. Pharmacol. Exp. Ther. 1980, 213:406-413.
    • (1980) J. Pharmacol. Exp. Ther. , vol.213 , pp. 406-413
    • Kenakin, T.P.1    Beek, D.2
  • 6
    • 0025783597 scopus 로고
    • The relative efficiency of beta-adrenoceptor coupling to myocardial inotropy and diastolic relaxation: Organ-selective treatment of diastolic dysfunction
    • Kenakin T.P., Ambrose J.R., Irving P.E. The relative efficiency of beta-adrenoceptor coupling to myocardial inotropy and diastolic relaxation: Organ-selective treatment of diastolic dysfunction. J. Pharmacol. Exp. Ther. 1991, 257:1189-1197.
    • (1991) J. Pharmacol. Exp. Ther. , vol.257 , pp. 1189-1197
    • Kenakin, T.P.1    Ambrose, J.R.2    Irving, P.E.3
  • 7
    • 0021172243 scopus 로고
    • The measurement of the relative efficacy of agonists by selective potentiation of tissue responses: Studies with isoprenaline and prenalterol in cardiac tissue
    • Kenakin T.P., Beek D. The measurement of the relative efficacy of agonists by selective potentiation of tissue responses: Studies with isoprenaline and prenalterol in cardiac tissue. J. Auton. Pharmacol. 1984, 4:153-159.
    • (1984) J. Auton. Pharmacol. , vol.4 , pp. 153-159
    • Kenakin, T.P.1    Beek, D.2
  • 8
    • 4444285556 scopus 로고
    • The action of acetylcholine and other drugs on the efflux of potassium and rubidium from smooth muscle of the guinea-pig intestine
    • Burgen A.S.V., Spero L. The action of acetylcholine and other drugs on the efflux of potassium and rubidium from smooth muscle of the guinea-pig intestine. Br. J. Pharmacol. 1968, 34:99-115.
    • (1968) Br. J. Pharmacol. , vol.34 , pp. 99-115
    • Burgen, A.S.V.1    Spero, L.2
  • 9
    • 0031434924 scopus 로고    scopus 로고
    • Differences between natural and recombinant G-protein coupled receptor systems with varying receptor G-protein stoichiometry
    • Kenakin T.P. Differences between natural and recombinant G-protein coupled receptor systems with varying receptor G-protein stoichiometry. Trends Pharmacol. Sci. 1997, 18:456-464.
    • (1997) Trends Pharmacol. Sci. , vol.18 , pp. 456-464
    • Kenakin, T.P.1
  • 10
    • 34447636845 scopus 로고    scopus 로고
    • Collateral efficacy as pharmacological problem applied to new drug discovery
    • Kenakin T.P. Collateral efficacy as pharmacological problem applied to new drug discovery. Expert Opin. Drug Disc. 2006, 1:635-652.
    • (2006) Expert Opin. Drug Disc. , vol.1 , pp. 635-652
    • Kenakin, T.P.1
  • 11
    • 17644402459 scopus 로고    scopus 로고
    • Transduction of receptor signals by arrestins
    • Lefkowitz R.J., Shenoy S.K. Transduction of receptor signals by arrestins. Science 2005, 308:512-517.
    • (2005) Science , vol.308 , pp. 512-517
    • Lefkowitz, R.J.1    Shenoy, S.K.2
  • 12
    • 25844477611 scopus 로고    scopus 로고
    • Composition and function of G protein-coupled receptor signalsomes controlling mitogen-activated protein kinase activity
    • Luttrell L.M. Composition and function of G protein-coupled receptor signalsomes controlling mitogen-activated protein kinase activity. J. Mol. Neurosci. 2005, 26:253-263.
    • (2005) J. Mol. Neurosci. , vol.26 , pp. 253-263
    • Luttrell, L.M.1
  • 13
    • 0141593597 scopus 로고    scopus 로고
    • Arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G-protein-coupled receptors
    • Azzi M., Charest P.G., Angers S., Rousseau G., Kohout T. arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G-protein-coupled receptors. Proc. Natl. Acad. Sci. USA 2003, 100:11406-11411.
    • (2003) Proc. Natl. Acad. Sci. USA , vol.100 , pp. 11406-11411
    • Azzi, M.1    Charest, P.G.2    Angers, S.3    Rousseau, G.4    Kohout, T.5
  • 14
    • 33751162165 scopus 로고    scopus 로고
    • 2 adrenergic receptor ligands toward adenylyl cyclase and mitogen-activated protein kinase reveals the pluridimensionality of efficacy
    • 2 adrenergic receptor ligands toward adenylyl cyclase and mitogen-activated protein kinase reveals the pluridimensionality of efficacy. Mol. Pharmacol. 2006, 70:1575-1584.
    • (2006) Mol. Pharmacol. , vol.70 , pp. 1575-1584
    • Galandrin, S.1    Bouvier, M.2
  • 15
    • 38849136696 scopus 로고    scopus 로고
    • Pharmacological onomastics: What's in a name?
    • Kenakin T.P. Pharmacological onomastics: What's in a name?. Br. J. Pharmacol. 2008, 153:432-438.
    • (2008) Br. J. Pharmacol. , vol.153 , pp. 432-438
    • Kenakin, T.P.1
  • 16
    • 0035891883 scopus 로고    scopus 로고
    • 2A receptors by agonists and antagonists
    • 2A receptors by agonists and antagonists. Brain Res. Bulletin 2001, 56:441-451.
    • (2001) Brain Res. Bulletin , vol.56 , pp. 441-451
    • Gray, J.A.1    Roth, B.L.2
  • 19
    • 0019130426 scopus 로고
    • Endorphin: Radioreceptor binding assay
    • Ferrar P., Li C.H. endorphin: Radioreceptor binding assay. Int. J. Pept. Protein Res. 1980, 16:66-69.
    • (1980) Int. J. Pept. Protein Res. , vol.16 , pp. 66-69
    • Ferrar, P.1    Li, C.H.2
  • 22
    • 0034677966 scopus 로고    scopus 로고
    • Drug discovery: A historical perspective
    • Drews J. Drug discovery: A historical perspective. Science 2000, 287:1960-1964.
    • (2000) Science , vol.287 , pp. 1960-1964
    • Drews, J.1
  • 24
    • 0002112970 scopus 로고
    • General pharmacology
    • Springer, Berlin, Ergansungsweerk band, A. Heffter (Ed.)
    • Clark A.J. General pharmacology. Handbuch der Experimentellen Pharmakologie 1937, 4:165-176. Springer, Berlin, Ergansungsweerk band. A. Heffter (Ed.).
    • (1937) Handbuch der Experimentellen Pharmakologie , vol.4 , pp. 165-176
    • Clark, A.J.1
  • 26
    • 0000140263 scopus 로고    scopus 로고
    • Novel GPCR's and their endogenous ligands: Expanding the boundaries of physiology and pharmacology
    • Marchese A., George S.R., Kolakowski L.F., Lynch K.R., O'Dowd B.F. Novel GPCR's and their endogenous ligands: Expanding the boundaries of physiology and pharmacology. Trends Pharmacol. Sci. 1999, 20:370-375.
    • (1999) Trends Pharmacol. Sci. , vol.20 , pp. 370-375
    • Marchese, A.1    George, S.R.2    Kolakowski, L.F.3    Lynch, K.R.4    O'Dowd, B.F.5
  • 27
    • 0035895505 scopus 로고    scopus 로고
    • The sequence of the human genome
    • Venter J.C., et al. The sequence of the human genome. Science 2001, 291:1304-1351.
    • (2001) Science , vol.291 , pp. 1304-1351
    • Venter, J.C.1
  • 30
    • 0033019171 scopus 로고    scopus 로고
    • Human adrenoceptor polymorphisms: Evolving recognition of clinical importance
    • Buscher R., Hermann V., Insel P.A. Human adrenoceptor polymorphisms: Evolving recognition of clinical importance. Trends Pharmacol. Sci. 1999, 20:94-99.
    • (1999) Trends Pharmacol. Sci. , vol.20 , pp. 94-99
    • Buscher, R.1    Hermann, V.2    Insel, P.A.3
  • 31
    • 0010673662 scopus 로고
    • A modification of receptor theory
    • Stephenson R.P. A modification of receptor theory. Br. J. Pharmacol. 1956, 11:379-393.
    • (1956) Br. J. Pharmacol. , vol.11 , pp. 379-393
    • Stephenson, R.P.1
  • 32
    • 32844471146 scopus 로고    scopus 로고
    • Origins of pharmacology
    • Norton S. Origins of pharmacology. Mol. Interventions 2005, 5:144-149.
    • (2005) Mol. Interventions , vol.5 , pp. 144-149
    • Norton, S.1
  • 33
    • 0022475505 scopus 로고
    • Differences in agonist dissociation constant estimates for 5-HT at 5-HT2-receptors: a problem of acute desensitization?
    • Leff P., Martin G.R., Morse J.M. Differences in agonist dissociation constant estimates for 5-HT at 5-HT2-receptors: a problem of acute desensitization?. Br. J. Pharmacol. 1986, 89:493-499.
    • (1986) Br. J. Pharmacol. , vol.89 , pp. 493-499
    • Leff, P.1    Martin, G.R.2    Morse, J.M.3
  • 35
    • 0019790028 scopus 로고
    • Conformational changes and drug action
    • Burgen A.S.V. Conformational changes and drug action. Fed. Proc. 1966, 40:2723-2728.
    • (1966) Fed. Proc. , vol.40 , pp. 2723-2728
    • Burgen, A.S.V.1
  • 36
    • 0000095559 scopus 로고
    • The problem of the haem interaction in haemoglobin and the basis for the Bohr effect
    • Wyman J.J., Allen D.W. The problem of the haem interaction in haemoglobin and the basis for the Bohr effect. J. Polymer Sci. 1951, 7:499-518.
    • (1951) J. Polymer Sci. , vol.7 , pp. 499-518
    • Wyman, J.J.1    Allen, D.W.2
  • 37
    • 70449143838 scopus 로고
    • Interaction at end-plate receptors between different choline derivatives
    • Del Castillo J., Katz B. Interaction at end-plate receptors between different choline derivatives. Proc. Roy. Soc. Lond. B. 1957, 146:369-381.
    • (1957) Proc. Roy. Soc. Lond. B. , vol.146 , pp. 369-381
    • Del Castillo, J.1    Katz, B.2
  • 38
    • 0034710976 scopus 로고    scopus 로고
    • Can allosteric regulation be predicted from structure?
    • Freire E. Can allosteric regulation be predicted from structure?. Proc. Natl. Acad. Sci. U.S.A. 2000, 97:11680-11682.
    • (2000) Proc. Natl. Acad. Sci. U.S.A. , vol.97 , pp. 11680-11682
    • Freire, E.1
  • 40
    • 0001169515 scopus 로고
    • Antagonists with negative intrinsic activity at opioid receptors coupled to GTP-binding proteins
    • Costa T., Herz A. Antagonists with negative intrinsic activity at opioid receptors coupled to GTP-binding proteins. Proc. Natl. Acad. Sci. U.S.A. 1989, 86:7321-7325.
    • (1989) Proc. Natl. Acad. Sci. U.S.A. , vol.86 , pp. 7321-7325
    • Costa, T.1    Herz, A.2
  • 41
    • 0027513982 scopus 로고
    • A mutation-induced activated state of the 2-adrenergic receptor: Extending the ternary complex model
    • Samama P., Cotecchia S., Costa T., Lefkowitz R.J. A mutation-induced activated state of the 2-adrenergic receptor: Extending the ternary complex model. J. Biol. Chem. 1993, 268:4625-4636.
    • (1993) J. Biol. Chem. , vol.268 , pp. 4625-4636
    • Samama, P.1    Cotecchia, S.2    Costa, T.3    Lefkowitz, R.J.4
  • 42
    • 0002112970 scopus 로고
    • General pharmacology
    • Springer, Berlin, Ergansungsweerk band, A. Heffter (Ed.)
    • Clark A.J. General pharmacology. Handbuch der Experimentellen Pharmakologie 1937, 4:165-176. Springer, Berlin, Ergansungsweerk band. A. Heffter (Ed.).
    • (1937) Handbuch der Experimentellen Pharmakologie , vol.4 , pp. 165-176
    • Clark, A.J.1
  • 43
    • 0010673662 scopus 로고
    • A modification of receptor theory
    • Stephenson R.P. A modification of receptor theory. Br. J. Pharmacol. 1956, 11:379-393.
    • (1956) Br. J. Pharmacol. , vol.11 , pp. 379-393
    • Stephenson, R.P.1
  • 44
    • 77049220618 scopus 로고
    • Affinity and intrinsic activity in the theory of competitive inhibition
    • Ariens E.J. Affinity and intrinsic activity in the theory of competitive inhibition. Arch. Int. Pharmacodyn. Ther. 1954, 99:32-49.
    • (1954) Arch. Int. Pharmacodyn. Ther. , vol.99 , pp. 32-49
    • Ariens, E.J.1
  • 46
    • 0001806350 scopus 로고
    • A critical survey of receptor theories of drug action
    • Springer-Verlag, Berlin, J.M. Van Rossum (Ed.)
    • MacKay D. A critical survey of receptor theories of drug action. Kinetics of drug action 1977, 255-322. Springer-Verlag, Berlin. J.M. Van Rossum (Ed.).
    • (1977) Kinetics of drug action , pp. 255-322
    • MacKay, D.1
  • 47
    • 0002355204 scopus 로고
    • The use of haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes
    • Academic Press, New York, N.J. Harper, A.B. Simmonds (Eds.)
    • Furchgott R.F. The use of haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes. Advances in drug research 1966, 21-55. Academic Press, New York. N.J. Harper, A.B. Simmonds (Eds.).
    • (1966) Advances in drug research , pp. 21-55
    • Furchgott, R.F.1
  • 48
    • 0000328674 scopus 로고
    • The classification of adrenoreceptors (adrenergic receptors): An evaluation from the standpoint of receptor theory
    • Springer-Verlag, Berlin, H. Blaschko, E. Muscholl (Eds.)
    • Furchgott R.F. The classification of adrenoreceptors (adrenergic receptors): An evaluation from the standpoint of receptor theory. Handbook of experimental pharmacology, catecholamines 1972, Vol. 33:283-335. Springer-Verlag, Berlin. H. Blaschko, E. Muscholl (Eds.).
    • (1972) Handbook of experimental pharmacology, catecholamines , vol.33 , pp. 283-335
    • Furchgott, R.F.1
  • 49
    • 0021058380 scopus 로고
    • Operational models of pharmacological agonist
    • Black J.W., Leff P. Operational models of pharmacological agonist. Proc. R. Soc. Lond. [Biol.] 1983, 220:141.
    • (1983) Proc. R. Soc. Lond. [Biol.] , vol.220 , pp. 141
    • Black, J.W.1    Leff, P.2
  • 51
    • 0019137579 scopus 로고
    • A ternary complex model explains the agonist-specific binding properties of adenylate cyclase coupled adrenergic receptor
    • DeLean A., Stadel J.M., Lefkowitz R.J. A ternary complex model explains the agonist-specific binding properties of adenylate cyclase coupled adrenergic receptor. J. Biol. Chem. 1980, 255:7108-7117.
    • (1980) J. Biol. Chem. , vol.255 , pp. 7108-7117
    • DeLean, A.1    Stadel, J.M.2    Lefkowitz, R.J.3
  • 52
    • 0006063198 scopus 로고    scopus 로고
    • The pharmacologic consequences of modeling synoptic receptor systems
    • CRC Press, Boca Raton, A. Christopoulos (Ed.)
    • Kenakin T.P. The pharmacologic consequences of modeling synoptic receptor systems. Biomedical applications of computer modeling 2000, 1-20. CRC Press, Boca Raton. A. Christopoulos (Ed.).
    • (2000) Biomedical applications of computer modeling , pp. 1-20
    • Kenakin, T.P.1
  • 53
    • 70449143838 scopus 로고
    • Interaction at end-plate receptors between different choline derivatives
    • Del Castillo J., Katz B. Interaction at end-plate receptors between different choline derivatives. Proc. R. Soc. London, B. 1957, 146:369-381.
    • (1957) Proc. R. Soc. London, B. , vol.146 , pp. 369-381
    • Del Castillo, J.1    Katz, B.2
  • 54
    • 0001613910 scopus 로고
    • On the nature of allosteric transition
    • Monod J., Wyman J., Changeux J.P. On the nature of allosteric transition. J. Mol. Biol. 1965, 12:306-329.
    • (1965) J. Mol. Biol. , vol.12 , pp. 306-329
    • Monod, J.1    Wyman, J.2    Changeux, J.P.3
  • 55
    • 0002060353 scopus 로고
    • The relationship between classical and cooperative models for drug action
    • University Park Press, Baltimore, H.P. Rang (Ed.)
    • Colquhoun D. The relationship between classical and cooperative models for drug action. A symposium on drug receptors 1973, 149-182. University Park Press, Baltimore. H.P. Rang (Ed.).
    • (1973) A symposium on drug receptors , pp. 149-182
    • Colquhoun, D.1
  • 56
    • 0014115893 scopus 로고
    • On the application of "a plausible model" of allosteric proteins to the receptor for acetylcholine
    • Karlin A. On the application of "a plausible model" of allosteric proteins to the receptor for acetylcholine. J. Theoret. Biol. 1967, 16:306-320.
    • (1967) J. Theoret. Biol. , vol.16 , pp. 306-320
    • Karlin, A.1
  • 57
    • 0015535998 scopus 로고
    • On the analysis of pharmacological experiments in terms of an allosteric receptor model
    • Thron C.D. On the analysis of pharmacological experiments in terms of an allosteric receptor model. Mol. Pharmacol. 1973, 9:1-9.
    • (1973) Mol. Pharmacol. , vol.9 , pp. 1-9
    • Thron, C.D.1
  • 59
    • 0017303494 scopus 로고
    • Regulation of adrenergic receptors by guanyl-5-yl imidodiphosphate and other purine nucleotides
    • Lefkowitz R.J., Mullikin D., Caron M.G. Regulation of adrenergic receptors by guanyl-5-yl imidodiphosphate and other purine nucleotides. J. Biol. Chem. 1976, 251:4686-4692.
    • (1976) J. Biol. Chem. , vol.251 , pp. 4686-4692
    • Lefkowitz, R.J.1    Mullikin, D.2    Caron, M.G.3
  • 60
    • 0017280145 scopus 로고
    • An agonist-specific effect of guanine nucleotides on the binding of the beta adrenergic receptor
    • MaGuire M.E., Van Arsdale P.M., Gilman A.G. An agonist-specific effect of guanine nucleotides on the binding of the beta adrenergic receptor. Mol. Pharmacol. 1976, 12:335-339.
    • (1976) Mol. Pharmacol. , vol.12 , pp. 335-339
    • MaGuire, M.E.1    Van Arsdale, P.M.2    Gilman, A.G.3
  • 61
    • 0029935383 scopus 로고    scopus 로고
    • The cubic ternary complex receptor-occupancy model
    • I. Model description
    • Weiss J.M., Morgan P.H., Lutz M.W., Kenakin T.P. The cubic ternary complex receptor-occupancy model. J. Theroet. Biol. 1996, 178:151-167.
    • (1996) J. Theroet. Biol. , vol.178 , pp. 151-167
    • Weiss, J.M.1    Morgan, P.H.2    Lutz, M.W.3    Kenakin, T.P.4
  • 62
    • 0029983553 scopus 로고    scopus 로고
    • The cubic ternary complex receptor-occupancy model
    • II. Understanding apparent affinity
    • Weiss J.M., Morgan P.H., Lutz M.W., Kenakin T.P. The cubic ternary complex receptor-occupancy model. J. Theroet. Biol. 1996, 178:169-182.
    • (1996) J. Theroet. Biol. , vol.178 , pp. 169-182
    • Weiss, J.M.1    Morgan, P.H.2    Lutz, M.W.3    Kenakin, T.P.4
  • 63
    • 0030596736 scopus 로고    scopus 로고
    • The cubic ternary complex receptor-occupancy model
    • III. Resurrecting efficacy
    • Weiss J.M., Morgan P.H., Lutz M.W., Kenakin T.P. The cubic ternary complex receptor-occupancy model. J. Theoret. Biol. 1996, 181:381-397.
    • (1996) J. Theoret. Biol. , vol.181 , pp. 381-397
    • Weiss, J.M.1    Morgan, P.H.2    Lutz, M.W.3    Kenakin, T.P.4
  • 66
    • 0001870572 scopus 로고    scopus 로고
    • Agonist efficacy and allosteric models of receptor action
    • Onaran H.O., Costa T. Agonist efficacy and allosteric models of receptor action. Ann. N. Y. Acad. Sci. 1997, 812:98-115.
    • (1997) Ann. N. Y. Acad. Sci. , vol.812 , pp. 98-115
    • Onaran, H.O.1    Costa, T.2
  • 68
    • 34447636845 scopus 로고    scopus 로고
    • Collateral efficacy as pharmacological problem applied to new drug discovery
    • Kenakin T.P. Collateral efficacy as pharmacological problem applied to new drug discovery. Expert Opin. Drug Disc. 2006, 1:635-652.
    • (2006) Expert Opin. Drug Disc. , vol.1 , pp. 635-652
    • Kenakin, T.P.1
  • 73
    • 0015861774 scopus 로고
    • Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (I50) of an enzymatic reaction
    • Cheng Y.C., Prusoff W.H. Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (I50) of an enzymatic reaction. Biochem. Pharmacol. 1973, 22:3099-3108.
    • (1973) Biochem. Pharmacol. , vol.22 , pp. 3099-3108
    • Cheng, Y.C.1    Prusoff, W.H.2
  • 75
    • 0028972931 scopus 로고
    • Positive and negative allosteric interactions on muscarinic receptors
    • Hejnova L., Tucek S., El-Fakahany E.E. Positive and negative allosteric interactions on muscarinic receptors. Eur. J. Pharmacol. 1995, 291:427-430.
    • (1995) Eur. J. Pharmacol. , vol.291 , pp. 427-430
    • Hejnova, L.1    Tucek, S.2    El-Fakahany, E.E.3
  • 76
    • 1842333847 scopus 로고    scopus 로고
    • Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors
    • Jakubic J., El-Fakahany E.E. Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol. Pharmacol. 1997, 52:172-177.
    • (1997) Mol. Pharmacol. , vol.52 , pp. 172-177
    • Jakubic, J.1    El-Fakahany, E.E.2
  • 77
    • 1842333847 scopus 로고    scopus 로고
    • Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors
    • Jakubic J., Bacakova L., El-Fakahany E.E., Tucek S. Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol. Pharmacol. 1997, 52:172-179.
    • (1997) Mol. Pharmacol. , vol.52 , pp. 172-179
    • Jakubic, J.1    Bacakova, L.2    El-Fakahany, E.E.3    Tucek, S.4
  • 78
    • 0028231689 scopus 로고
    • Mechanisms of steric and cooperative interactions of alcuronium on cardiac muscarinic acetylcholine receptors
    • Proska J., Tucek S. Mechanisms of steric and cooperative interactions of alcuronium on cardiac muscarinic acetylcholine receptors. Mol. Pharmacol. 1994, 45:709-717.
    • (1994) Mol. Pharmacol. , vol.45 , pp. 709-717
    • Proska, J.1    Tucek, S.2
  • 79
    • 0009196548 scopus 로고    scopus 로고
    • Quantification of allosteric interactions at G-protein coupled receptors using radioligand assays
    • Wiley and Sons, New York, S.J. Enna (Ed.)
    • Christopoulos A. Quantification of allosteric interactions at G-protein coupled receptors using radioligand assays. Current protocol in pharmacology 2000, 1.22.21-1.22.40. Wiley and Sons, New York. S.J. Enna (Ed.).
    • (2000) Current protocol in pharmacology , pp. 1.22.21-1.22.40
    • Christopoulos, A.1
  • 80
    • 0029126526 scopus 로고
    • Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: Interactions of strychnine and acetylcholine at muscarinic receptors
    • Lazareno S., Birdsall N.J.M. Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: Interactions of strychnine and acetylcholine at muscarinic receptors. Mol. Pharmacol. 1995, 48:362-378.
    • (1995) Mol. Pharmacol. , vol.48 , pp. 362-378
    • Lazareno, S.1    Birdsall, N.J.M.2
  • 84
    • 0020324707 scopus 로고
    • Mechanisms of hormone-effector coupling: The adrenergic receptor and adenylate cyclase
    • Lefkowitz R.J., Caron M.G., Michel T., Stadel J.M. Mechanisms of hormone-effector coupling: The adrenergic receptor and adenylate cyclase. Fed. Proc. 1982, 41:2664-2670.
    • (1982) Fed. Proc. , vol.41 , pp. 2664-2670
    • Lefkowitz, R.J.1    Caron, M.G.2    Michel, T.3    Stadel, J.M.4
  • 85
    • 0021336303 scopus 로고
    • The kinetics of competitive radioligand binding predicted by the law of mass action
    • Motulsky H.J., Mahan L.C. The kinetics of competitive radioligand binding predicted by the law of mass action. Mol. Pharmacol. 1984, 25:1-9.
    • (1984) Mol. Pharmacol. , vol.25 , pp. 1-9
    • Motulsky, H.J.1    Mahan, L.C.2
  • 86
    • 0022408262 scopus 로고
    • The relationship between muscarinic receptor occupancy and adenylate cyclase inhibition in the rabbit myocardium
    • Ehlert F.J. The relationship between muscarinic receptor occupancy and adenylate cyclase inhibition in the rabbit myocardium. Mol. Pharmacol. 1985, 28:410-421.
    • (1985) Mol. Pharmacol. , vol.28 , pp. 410-421
    • Ehlert, F.J.1
  • 87
    • 0028012102 scopus 로고
    • Activation of heterologously expressed D3 dopamine receptors: Comparison with D2 dopamine receptors
    • Chio C.L., Lajiness M.E., Huff R.M. Activation of heterologously expressed D3 dopamine receptors: Comparison with D2 dopamine receptors. Mol. Pharmacol 1994, 45:51-60.
    • (1994) Mol. Pharmacol , vol.45 , pp. 51-60
    • Chio, C.L.1    Lajiness, M.E.2    Huff, R.M.3
  • 91
    • 0030006847 scopus 로고    scopus 로고
    • 2-adrenergic receptors in rat C6 glioma cells: Functional interactions between closely related subtypes
    • 2-adrenergic receptors in rat C6 glioma cells: Functional interactions between closely related subtypes. Mol. Pharmacol 1996, 50:175-184.
    • (1996) Mol. Pharmacol , vol.50 , pp. 175-184
    • Zhong, H.1    Guerrero, S.W.2    Esbenshade, T.A.3    Minneman, K.P.4
  • 92
    • 0028981057 scopus 로고
    • 16 couple a wide variety of receptors to phospholipase C
    • 16 couple a wide variety of receptors to phospholipase C. J. Biol. Chem 1995, 270:15175-15180.
    • (1995) J. Biol. Chem , vol.270 , pp. 15175-15180
    • Offermanns, S.1    Simon, M.I.2
  • 94
    • 0031434924 scopus 로고    scopus 로고
    • Differences between natural and recombinant G-protein coupled receptor systems with varying receptor/G-protein stoichiometry
    • Kenakin T.P. Differences between natural and recombinant G-protein coupled receptor systems with varying receptor/G-protein stoichiometry. Trends Pharmacol. Sci 1997, 18:456-464.
    • (1997) Trends Pharmacol. Sci , vol.18 , pp. 456-464
    • Kenakin, T.P.1
  • 95
    • 8044237686 scopus 로고
    • An attempt to study the effects of chemical structure on the affinity and efficacy of compounds related to acetylcholine
    • Barlow R.B., Scott K.A., Stephenson R.P. An attempt to study the effects of chemical structure on the affinity and efficacy of compounds related to acetylcholine. Br. J. Pharmacol 1967, 21:509-522.
    • (1967) Br. J. Pharmacol , vol.21 , pp. 509-522
    • Barlow, R.B.1    Scott, K.A.2    Stephenson, R.P.3
  • 96
    • 0019182114 scopus 로고
    • N,N-Diethyl-2-(1-pyridyl)ethylamine, a partial agonist for the histamine receptor in guinea pig ileum
    • Kenakin T.P., Cook D.A. N,N-Diethyl-2-(1-pyridyl)ethylamine, a partial agonist for the histamine receptor in guinea pig ileum. Can. J. Physiol. Pharmacol 1980, 58:1307-1310.
    • (1980) Can. J. Physiol. Pharmacol , vol.58 , pp. 1307-1310
    • Kenakin, T.P.1    Cook, D.A.2
  • 97
    • 0002355204 scopus 로고
    • The use of haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes
    • Academic Press, London, New York, N.J. Harper, A.B. Simmonds (Eds.)
    • Furchgott R.F. The use of haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes. Advances in drug research 1966, Vol. 3:21-55. Academic Press, London, New York. N.J. Harper, A.B. Simmonds (Eds.).
    • (1966) Advances in drug research , vol.3 , pp. 21-55
    • Furchgott, R.F.1
  • 99
    • 0021355975 scopus 로고
    • The relative contribution of affinity and efficacy to agonist activity: Organ selectivity of noradrenaline and oxymetazoline
    • Kenakin T.P. The relative contribution of affinity and efficacy to agonist activity: Organ selectivity of noradrenaline and oxymetazoline. Br. J. Pharmacol 1984, 81:131-141.
    • (1984) Br. J. Pharmacol , vol.81 , pp. 131-141
    • Kenakin, T.P.1
  • 100
    • 78651175536 scopus 로고
    • The uptake of atropine and related drugs by intestinal smooth muscle of the guinea pig in relation to acetylcholine receptors
    • Paton W.D.M., Rang H.P. The uptake of atropine and related drugs by intestinal smooth muscle of the guinea pig in relation to acetylcholine receptors. Proc. R. Soc. Lond. [Biol.] 1965, 163:1-44.
    • (1965) Proc. R. Soc. Lond. [Biol.] , vol.163 , pp. 1-44
    • Paton, W.D.M.1    Rang, H.P.2
  • 101
    • 0002177268 scopus 로고
    • The quantitative effects of antagonistic drugs
    • Gaddum J.H. The quantitative effects of antagonistic drugs. J. Physiol. Lond. 1937, 89:7P-9P.
    • (1937) J. Physiol. Lond. , vol.89 , pp. 7P-9P
    • Gaddum, J.H.1
  • 103
    • 0009644628 scopus 로고
    • Some quantitative uses of drug antagonists
    • Arunlakshana O., Schild H.O. Some quantitative uses of drug antagonists. Br. J. Pharmacol. 1959, 14:48-58.
    • (1959) Br. J. Pharmacol. , vol.14 , pp. 48-58
    • Arunlakshana, O.1    Schild, H.O.2
  • 104
    • 0024446412 scopus 로고
    • Pharmacologic discrimination between receptor heterogeneity and allosteric interaction: Resultant analysis of gallamine and pirenzeipine antagonism of muscarinic responses in rat trachea
    • Kenakin T.P., Boselli C. Pharmacologic discrimination between receptor heterogeneity and allosteric interaction: Resultant analysis of gallamine and pirenzeipine antagonism of muscarinic responses in rat trachea. J. Pharmacol. Exp. Ther. 1989, 250:944-952.
    • (1989) J. Pharmacol. Exp. Ther. , vol.250 , pp. 944-952
    • Kenakin, T.P.1    Boselli, C.2
  • 105
    • 0020053249 scopus 로고
    • The Schild regression in the process of receptor classification
    • Kenakin T.P. The Schild regression in the process of receptor classification. Can. J. Physiol. Pharmacol. 1982, 60:249-265.
    • (1982) Can. J. Physiol. Pharmacol. , vol.60 , pp. 249-265
    • Kenakin, T.P.1
  • 106
    • 0010673662 scopus 로고
    • A modification of receptor theory
    • Stephenson R.P. A modification of receptor theory. Br. J. Pharmacol. 1956, 11:379-393.
    • (1956) Br. J. Pharmacol. , vol.11 , pp. 379-393
    • Stephenson, R.P.1
  • 107
    • 33745833578 scopus 로고
    • On equilibrium dissociation constants for complexes of drug receptor subtypes: Selective and nonselective interactions of partial agonists with two adrenoceptor subtypes mediating positive chronotropic effects of isoprenaline in kitten atria
    • Kaumann A.J., Marano M. On equilibrium dissociation constants for complexes of drug receptor subtypes: Selective and nonselective interactions of partial agonists with two adrenoceptor subtypes mediating positive chronotropic effects of isoprenaline in kitten atria. Naunyn Schmiedebeberg's Arch. Pharmacol. 1982, 219:216-221.
    • (1982) Naunyn Schmiedebeberg's Arch. Pharmacol. , vol.219 , pp. 216-221
    • Kaumann, A.J.1    Marano, M.2
  • 108
    • 0018095505 scopus 로고
    • The pharmacological classification of practolol and choropractolol
    • Kenakin T.P., Black J.W. The pharmacological classification of practolol and choropractolol. Mol. Pharmacol. 1978, 14:607-623.
    • (1978) Mol. Pharmacol. , vol.14 , pp. 607-623
    • Kenakin, T.P.1    Black, J.W.2
  • 110
    • 0029094516 scopus 로고    scopus 로고
    • Analysis of competitive agonist-antagonist interactions by nonlinear regression
    • Lew M.J., Angus J.A. Analysis of competitive agonist-antagonist interactions by nonlinear regression. Trends Pharmacol. Sci. 1996, 16:328-337.
    • (1996) Trends Pharmacol. Sci. , vol.16 , pp. 328-337
    • Lew, M.J.1    Angus, J.A.2
  • 111
    • 0021990306 scopus 로고
    • An operational model of pharmacological agonism: The effect of E/[A] curve shape on agonist dissociation constant estimation
    • Black J.W., Leff P., Shankley N.P., Wood J. An operational model of pharmacological agonism: The effect of E/[A] curve shape on agonist dissociation constant estimation. Br. J. Pharmacol. 1985, 84:561-571.
    • (1985) Br. J. Pharmacol. , vol.84 , pp. 561-571
    • Black, J.W.1    Leff, P.2    Shankley, N.P.3    Wood, J.4
  • 112
    • 0027260718 scopus 로고
    • Estimation of partial agonist affinity by interaction with a full agonist: A direct operational model-fit approach
    • Leff P., Dougall I.G., Harper D. Estimation of partial agonist affinity by interaction with a full agonist: A direct operational model-fit approach. Br. J. Pharmacol. 1993, 110:239-244.
    • (1993) Br. J. Pharmacol. , vol.110 , pp. 239-244
    • Leff, P.1    Dougall, I.G.2    Harper, D.3
  • 113
    • 1842333847 scopus 로고    scopus 로고
    • Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors
    • Jakubic J, Bacakova I, El-Fakahany E.E, Tucek S Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol. Pharmacol 1997, 52:172-179.
    • (1997) Mol. Pharmacol , vol.52 , pp. 172-179
    • Jakubic, J.1    Bacakova, I.2    El-Fakahany, E.E.3    Tucek, S.4
  • 114
    • 0002449434 scopus 로고
    • The active site of enzyme action
    • Koshland D.E. The active site of enzyme action. Adv. Enzymol 1960, 22:45-97.
    • (1960) Adv. Enzymol , vol.22 , pp. 45-97
    • Koshland, D.E.1
  • 115
    • 0026689405 scopus 로고
    • Modulation by certain conserved aspartate residues of the allosteric interaction of gallamine and the ml muscarinic receptor
    • Lee N.H., Hu J., El-Fakahany E.E. Modulation by certain conserved aspartate residues of the allosteric interaction of gallamine and the ml muscarinic receptor. J. Pharmacol. Exp. Ther 1992, 262:312-316.
    • (1992) J. Pharmacol. Exp. Ther , vol.262 , pp. 312-316
    • Lee, N.H.1    Hu, J.2    El-Fakahany, E.E.3
  • 117
    • 1242294467 scopus 로고    scopus 로고
    • Allosteric inhibition through core disruption
    • Horn J.R, Shoichet B.K. Allosteric inhibition through core disruption. J. Mol. Biol 2004, 336:1283-1291.
    • (2004) J. Mol. Biol , vol.336 , pp. 1283-1291
    • Horn, J.R.1    Shoichet, B.K.2
  • 118
  • 119
    • 3142781225 scopus 로고    scopus 로고
    • Small-molecule inhibitors of protein-protein interactions: progressing towards the dream
    • Arkin M.R., Wells J.A. Small-molecule inhibitors of protein-protein interactions: progressing towards the dream. Nature Rev. Drug Disc 2004, 3:301-317.
    • (2004) Nature Rev. Drug Disc , vol.3 , pp. 301-317
    • Arkin, M.R.1    Wells, J.A.2
  • 120
    • 0037666888 scopus 로고    scopus 로고
    • Implications of protein flexibility for drug discovery
    • Teague S.J. Implications of protein flexibility for drug discovery. Nature Reviews Drug Discovery 2003, 2:527-541.
    • (2003) Nature Reviews Drug Discovery , vol.2 , pp. 527-541
    • Teague, S.J.1
  • 121
    • 15744391870 scopus 로고    scopus 로고
    • The CCR5 receptor-based mechanism of action of 873140, a potent allosteric non-competitive HIV entry-inhibitor
    • Watson C., Jenkinson S., Kazmierski W., Kenakin T.P. The CCR5 receptor-based mechanism of action of 873140, a potent allosteric non-competitive HIV entry-inhibitor. Mol. Pharmacol 2005, 67:1268-1282.
    • (2005) Mol. Pharmacol , vol.67 , pp. 1268-1282
    • Watson, C.1    Jenkinson, S.2    Kazmierski, W.3    Kenakin, T.P.4
  • 123
    • 0030986787 scopus 로고    scopus 로고
    • HIV-1 induced cell fusion is mediated by multiple regions within both the viral envelope and the CCR-5 co-receptor
    • Bieniassz P.D., Fridell R.A., Aramori I., Ferguson S.S., Caron M.G., Cullen B.R. HIV-1 induced cell fusion is mediated by multiple regions within both the viral envelope and the CCR-5 co-receptor. EMBO J 1997, 16:2599-2609.
    • (1997) EMBO J , vol.16 , pp. 2599-2609
    • Bieniassz, P.D.1    Fridell, R.A.2    Aramori, I.3    Ferguson, S.S.4    Caron, M.G.5    Cullen, B.R.6
  • 124
    • 0032543307 scopus 로고    scopus 로고
    • Structure of an HIV gp120 envelope glycoprotein in complex with the CD4 receptor and a neutralizing human antibody
    • Kwong P.D., Wyatt R., Robinson J., Sweet R.W., Sodroski J., Hendricks W.A. Structure of an HIV gp120 envelope glycoprotein in complex with the CD4 receptor and a neutralizing human antibody. Nature 1998, 393:648-659.
    • (1998) Nature , vol.393 , pp. 648-659
    • Kwong, P.D.1    Wyatt, R.2    Robinson, J.3    Sweet, R.W.4    Sodroski, J.5    Hendricks, W.A.6
  • 127
    • 0032546844 scopus 로고    scopus 로고
    • The HIV-1 envelope glycoproteins: Fusogens, antigens, and immunogens
    • Wyatt R., Sodroski J. The HIV-1 envelope glycoproteins: Fusogens, antigens, and immunogens. Science 1998, 280:1884-1888.
    • (1998) Science , vol.280 , pp. 1884-1888
    • Wyatt, R.1    Sodroski, J.2
  • 132
    • 0032507962 scopus 로고    scopus 로고
    • Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development
    • Zou Y.R., Kottmann A.H., Kuroda M., Taniuchi I., Littman D.R. Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development. Nature 1998, 393:595-599.
    • (1998) Nature , vol.393 , pp. 595-599
    • Zou, Y.R.1    Kottmann, A.H.2    Kuroda, M.3    Taniuchi, I.4    Littman, D.R.5
  • 135
    • 0019972810 scopus 로고
    • The cholinergic hypothesis of geriatric memory dysfunction
    • Bartus R.T., Dean R.L., Beer B., Lippa A.S. The cholinergic hypothesis of geriatric memory dysfunction. Science 1982, 217:408-417.
    • (1982) Science , vol.217 , pp. 408-417
    • Bartus, R.T.1    Dean, R.L.2    Beer, B.3    Lippa, A.S.4
  • 136
    • 0029055030 scopus 로고
    • Allosteric modulation of muscarinic acetylcholine receptors
    • Tucek S., Proska J. Allosteric modulation of muscarinic acetylcholine receptors. Trends Pharmacol. Sci 1995, 16:205-212.
    • (1995) Trends Pharmacol. Sci , vol.16 , pp. 205-212
    • Tucek, S.1    Proska, J.2
  • 137
    • 0033528461 scopus 로고    scopus 로고
    • Acetylcholinesterase inhibitors for Alzheimer's disease
    • Flicker L. Acetylcholinesterase inhibitors for Alzheimer's disease. Br. Med. J 1999, 318:615-616.
    • (1999) Br. Med. J , vol.318 , pp. 615-616
    • Flicker, L.1
  • 138
    • 0002567031 scopus 로고    scopus 로고
    • New approach to drug therapy of Alzheimer's dementia
    • Maelicke A, Albuquerque E.X New approach to drug therapy of Alzheimer's dementia. Drug Discovery Today 1996, 1:53-59.
    • (1996) Drug Discovery Today , vol.1 , pp. 53-59
    • Maelicke, A.1    Albuquerque, E.X.2
  • 140
    • 0023958554 scopus 로고
    • Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods
    • Ehlert F.J. Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods. Mol. Pharmacol 1988, 33:187-194.
    • (1988) Mol. Pharmacol , vol.33 , pp. 187-194
    • Ehlert, F.J.1
  • 141
    • 0021990306 scopus 로고
    • An operational model of pharmacological agonism: The effect of E/[A] curve shape on agonist dissociation constant estimation
    • Black J.W., Leff P., Shankley N.P., Wood J. An operational model of pharmacological agonism: The effect of E/[A] curve shape on agonist dissociation constant estimation. Br. J. Pharmacol 1985, 84:561-571.
    • (1985) Br. J. Pharmacol , vol.84 , pp. 561-571
    • Black, J.W.1    Leff, P.2    Shankley, N.P.3    Wood, J.4
  • 142
    • 27844519281 scopus 로고    scopus 로고
    • New concepts in durg discovery: Collateral efficacy and permissive antagonism
    • Kenakin T.P. New concepts in durg discovery: Collateral efficacy and permissive antagonism. Nature Rev. Durg Disc 2005, 4:919-927.
    • (2005) Nature Rev. Durg Disc , vol.4 , pp. 919-927
    • Kenakin, T.P.1
  • 143
    • 33751183557 scopus 로고    scopus 로고
    • Determining the potency and molecular mechanism of action of insurmountable antagonists
    • Kenakin T.P., Jenkinson S., Watson C. Determining the potency and molecular mechanism of action of insurmountable antagonists. J. Pharmacol. Exp. Ther 2006, 319:710-723.
    • (2006) J. Pharmacol. Exp. Ther , vol.319 , pp. 710-723
    • Kenakin, T.P.1    Jenkinson, S.2    Watson, C.3
  • 145
    • 0009196548 scopus 로고    scopus 로고
    • Overview of receptor allosterism
    • John Wiley and Sons, New York
    • Christopoulos A. Overview of receptor allosterism. Current protocols in pharmacology 2000, Vol 1:1.21.21-1.21.45. John Wiley and Sons, New York.
    • (2000) Current protocols in pharmacology , vol.1 , pp. 1.21.21-1.21.45
    • Christopoulos, A.1
  • 148
    • 0031024171 scopus 로고    scopus 로고
    • Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
    • Lipinski C., Lombardo F., Dominy B., Feeney P. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug. Deliv. Rev. 2001, 23:3-25.
    • (2001) Adv. Drug. Deliv. Rev. , vol.23 , pp. 3-25
    • Lipinski, C.1    Lombardo, F.2    Dominy, B.3    Feeney, P.4
  • 149
    • 0021812342 scopus 로고
    • Identification of serotonin M-receptor subtypes and their specific blockade by a new class of drugs
    • Richardson B.P., Engel G., Donatsch P., Stadler P.A. Identification of serotonin M-receptor subtypes and their specific blockade by a new class of drugs. Nature 1985, 316:126-131.
    • (1985) Nature , vol.316 , pp. 126-131
    • Richardson, B.P.1    Engel, G.2    Donatsch, P.3    Stadler, P.A.4
  • 151
    • 0034461768 scopus 로고    scopus 로고
    • Drug-like properties and the causes of poor solubility and poor permeability
    • Lipinski C.A. Drug-like properties and the causes of poor solubility and poor permeability. J. Pharmacol. Tox. Meth. 2000, 44:235-249.
    • (2000) J. Pharmacol. Tox. Meth. , vol.44 , pp. 235-249
    • Lipinski, C.A.1
  • 152
    • 1842333847 scopus 로고    scopus 로고
    • Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors
    • Jakubic J., Bacakova I., El-Fakahany E.E., Tucek S. Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol. Pharmacol. 1997, 52:172-179.
    • (1997) Mol. Pharmacol. , vol.52 , pp. 172-179
    • Jakubic, J.1    Bacakova, I.2    El-Fakahany, E.E.3    Tucek, S.4
  • 153
    • 17944365465 scopus 로고    scopus 로고
    • Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: Synthesis and structure-Activity relationships for 1-[N-(Methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes
    • Finke P.E., Oates B., Mills S.G., MacCoss M., Malkowitz L., Springer M.S., Gould S.L., DeMartino J.A., Carella A., Carver G., et al. Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: Synthesis and structure-Activity relationships for 1-[N-(Methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes. Bioorg. Med. Chem. Lett. 2001, 11:2475-2479.
    • (2001) Bioorg. Med. Chem. Lett. , vol.11 , pp. 2475-2479
    • Finke, P.E.1    Oates, B.2    Mills, S.G.3    MacCoss, M.4    Malkowitz, L.5    Springer, M.S.6    Gould, S.L.7    DeMartino, J.A.8    Carella, A.9    Carver, G.10
  • 154
    • 0033003760 scopus 로고    scopus 로고
    • A simple statistical parameter for use in evaluation and validation of high throughput screening assays
    • Zhang J.-H., Chung T.D.Y., Oldenburg K.R. A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J. Biomeolecular Screening 1999, 4:67-72.
    • (1999) J. Biomeolecular Screening , vol.4 , pp. 67-72
    • Zhang, J.-H.1    Chung, T.D.Y.2    Oldenburg, K.R.3
  • 155
    • 0021745755 scopus 로고
    • Functional group contributions to drug-receptor interactions
    • Andrews P.R., Craik D.J., Martin J.L. Functional group contributions to drug-receptor interactions. J. Med. Chem. 1984, 27:1648-1657.
    • (1984) J. Med. Chem. , vol.27 , pp. 1648-1657
    • Andrews, P.R.1    Craik, D.J.2    Martin, J.L.3
  • 156
    • 1942453243 scopus 로고    scopus 로고
    • Ligand efficiency: A useful metric for lead selection
    • Hopkins A.L., Groom C.R., Alex A. Ligand efficiency: A useful metric for lead selection. Drug Disc. Today 2004, 9:430-431.
    • (2004) Drug Disc. Today , vol.9 , pp. 430-431
    • Hopkins, A.L.1    Groom, C.R.2    Alex, A.3
  • 159
    • 14644420930 scopus 로고    scopus 로고
    • Interfacial inhibition of macromolecular interactions: Nature's paradigm for drug discovery
    • Pommier Y., Cherfils J. Interfacial inhibition of macromolecular interactions: Nature's paradigm for drug discovery. Trend. Pharmacol. Sci. 2005, 26:138-145.
    • (2005) Trend. Pharmacol. Sci. , vol.26 , pp. 138-145
    • Pommier, Y.1    Cherfils, J.2
  • 160
    • 0001870572 scopus 로고    scopus 로고
    • Agonist efficacy and allosteric models of receptor action
    • Onaran H.O., Costa T. Agonist efficacy and allosteric models of receptor action. Ann. N. Y. Acad. Sci. 1997, 812:98-115.
    • (1997) Ann. N. Y. Acad. Sci. , vol.812 , pp. 98-115
    • Onaran, H.O.1    Costa, T.2
  • 162
    • 0036591660 scopus 로고    scopus 로고
    • The ligand paradox between affinity and efficacy: Can you be there and not make a difference?
    • Kenakin T.P., Onaran O. The ligand paradox between affinity and efficacy: Can you be there and not make a difference?. Trends Pharmacol. Sci. 2002, 23:275-280.
    • (2002) Trends Pharmacol. Sci. , vol.23 , pp. 275-280
    • Kenakin, T.P.1    Onaran, O.2
  • 163
    • 34447645129 scopus 로고    scopus 로고
    • Resonance energy transfer approaches in molecular pharmacology and beyond
    • Marullo S., Bouvier M. Resonance energy transfer approaches in molecular pharmacology and beyond. Trends Pharmacol. Sci. 2007, 28:362-365.
    • (2007) Trends Pharmacol. Sci. , vol.28 , pp. 362-365
    • Marullo, S.1    Bouvier, M.2
  • 164
    • 20844434337 scopus 로고    scopus 로고
    • A FLASH-based approach to determine G protein-coupled receptor activation in living cells
    • Hoffmann C., Gaietta G., Bünemann M., Adams S., Oberdorff-Maass S., Behr B., et al. A FLASH-based approach to determine G protein-coupled receptor activation in living cells. Nat. Methods 2005, 2:171-176.
    • (2005) Nat. Methods , vol.2 , pp. 171-176
    • Hoffmann, C.1    Gaietta, G.2    Bünemann, M.3    Adams, S.4    Oberdorff-Maass, S.5    Behr, B.6
  • 165
    • 0141593597 scopus 로고    scopus 로고
    • Arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G-protein-coupled receptors
    • Azzi M., Charest P.G., Angers S., Rousseau G., Kohout T. arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G-protein-coupled receptors. Proc. Natl. Acad. Sci. USA 2003, 100:11406-11411.
    • (2003) Proc. Natl. Acad. Sci. USA , vol.100 , pp. 11406-11411
    • Azzi, M.1    Charest, P.G.2    Angers, S.3    Rousseau, G.4    Kohout, T.5
  • 166
    • 10644230013 scopus 로고    scopus 로고
    • Using confidence intervals around individual means to assess statistical significance between two means
    • Julious S.A. Using confidence intervals around individual means to assess statistical significance between two means. Pharmaceut. Stat. 2004, 3:217-222.
    • (2004) Pharmaceut. Stat. , vol.3 , pp. 217-222
    • Julious, S.A.1
  • 168
    • 27344435806 scopus 로고    scopus 로고
    • Quantitative risk modeling for new pharmaceutical compounds
    • Tang Z., Taylor M.J., Lisboa P., Dyas M. Quantitative risk modeling for new pharmaceutical compounds. Drug Disc. Today 2005, 22:1520-1526.
    • (2005) Drug Disc. Today , vol.22 , pp. 1520-1526
    • Tang, Z.1    Taylor, M.J.2    Lisboa, P.3    Dyas, M.4
  • 170
    • 0027336957 scopus 로고
    • (.+-.)-3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: A conformationally restricted analog of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor
    • King F.D., Brown A.M., Gaster L.M., Kaumann A.J., Medhurst A.D., Parker S.G., Parsons A.A., Patch T.L., Raval P. (.+-.)-3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: A conformationally restricted analog of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor. J. Med. Chem. 1993, 36:1918.
    • (1993) J. Med. Chem. , vol.36 , pp. 1918
    • King, F.D.1    Brown, A.M.2    Gaster, L.M.3    Kaumann, A.J.4    Medhurst, A.D.5    Parker, S.G.6    Parsons, A.A.7    Patch, T.L.8    Raval, P.9
  • 176
    • 0037124196 scopus 로고    scopus 로고
    • Drugs, leads, and drug-likeness: An analysis of some recently launched drugs
    • Proudfoot J.R. Drugs, leads, and drug-likeness: An analysis of some recently launched drugs. Bioogan. Med. Chem. Lett. 2002, 12:1647-1650.
    • (2002) Bioogan. Med. Chem. Lett. , vol.12 , pp. 1647-1650
    • Proudfoot, J.R.1
  • 178
    • 26944446576 scopus 로고    scopus 로고
    • In vitro safety pharmacology profiling: An essential tool for successful drug development
    • Whitebread S., Hamon J., Bojanic D., Urban L. In vitro safety pharmacology profiling: An essential tool for successful drug development. Drug Disc. Today 2005, 10:1421-1433.
    • (2005) Drug Disc. Today , vol.10 , pp. 1421-1433
    • Whitebread, S.1    Hamon, J.2    Bojanic, D.3    Urban, L.4
  • 179
    • 22944438384 scopus 로고    scopus 로고
    • Research on adverse drug events: Muscarinic m3 receptor binding affinity could predict the risk of antipsychotics to induce type 2 diabetes
    • Silvetre J.S., Prous J. Research on adverse drug events: Muscarinic m3 receptor binding affinity could predict the risk of antipsychotics to induce type 2 diabetes. Meth. Find. Exp. Clin. Pharmacol. 2005, 27:289-304.
    • (2005) Meth. Find. Exp. Clin. Pharmacol. , vol.27 , pp. 289-304
    • Silvetre, J.S.1    Prous, J.2
  • 180
    • 27644596457 scopus 로고    scopus 로고
    • Predicting in vivo drug interactions from in vitro drug discovery data
    • Wienkers L.C., Heath T.G. Predicting in vivo drug interactions from in vitro drug discovery data. Nature Rev. Drug Discovery 2005, 4:825-833.
    • (2005) Nature Rev. Drug Discovery , vol.4 , pp. 825-833
    • Wienkers, L.C.1    Heath, T.G.2
  • 181
    • 21044451732 scopus 로고    scopus 로고
    • GPCR antitarget modeling: Pharmacophore models for biogenic amine binding GPCRs to avoid GPCR-mediated side effect
    • Klabunde T., Evers A. GPCR antitarget modeling: Pharmacophore models for biogenic amine binding GPCRs to avoid GPCR-mediated side effect. Chem. Bio. Chem. 2005, 6:876-889.
    • (2005) Chem. Bio. Chem. , vol.6 , pp. 876-889
    • Klabunde, T.1    Evers, A.2
  • 182
    • 12144257810 scopus 로고    scopus 로고
    • Derivation and validation of toxicophores for mutagenicity prediction
    • Kazius J., Bursi R. Derivation and validation of toxicophores for mutagenicity prediction. J. Med. Chem. 2005, 48:312-320.
    • (2005) J. Med. Chem. , vol.48 , pp. 312-320
    • Kazius, J.1    Bursi, R.2
  • 183
    • 0014104395 scopus 로고
    • Effect of polymorphism on the absorption of chloramphenicol from chloramphenicol palmitate
    • Aguiar A.J., Krc J., Kinkel A.W., Samyn A.C. Effect of polymorphism on the absorption of chloramphenicol from chloramphenicol palmitate. J. Pharm. Sci. 1967, 56(7):847-853.
    • (1967) J. Pharm. Sci. , vol.56 , Issue.7 , pp. 847-853
    • Aguiar, A.J.1    Krc, J.2    Kinkel, A.W.3    Samyn, A.C.4
  • 186
    • 84971199691 scopus 로고
    • Calculation of drug solubilities by pharmacy students
    • Cates I.A. Calculation of drug solubilities by pharmacy students. Amer. J. Pharm. Ed. 1981, 45:11-13.
    • (1981) Amer. J. Pharm. Ed. , vol.45 , pp. 11-13
    • Cates, I.A.1
  • 188
    • 0001334658 scopus 로고    scopus 로고
    • Design principles for orally bioavailable drugs
    • Navia M.A., Chaturvedi P.R. Design principles for orally bioavailable drugs. Drug Disc. Today 1996, 1:179-199.
    • (1996) Drug Disc. Today , vol.1 , pp. 179-199
    • Navia, M.A.1    Chaturvedi, P.R.2
  • 189
    • 2642527944 scopus 로고    scopus 로고
    • Combined application of parallel artificial membrane permeability assay and Caco-2 permeability assays in drug discovery
    • Kerns E.H., Di L., Petusky S., Farris M., Ley R., Jupp P. Combined application of parallel artificial membrane permeability assay and Caco-2 permeability assays in drug discovery. J. Pharm. Sci. 2004, 93:1440-1453.
    • (2004) J. Pharm. Sci. , vol.93 , pp. 1440-1453
    • Kerns, E.H.1    Di, L.2    Petusky, S.3    Farris, M.4    Ley, R.5    Jupp, P.6
  • 190
    • 14644398632 scopus 로고    scopus 로고
    • Cell culture-based models of intestinal permeability: A critique
    • Balimane P.V., Chong S. Cell culture-based models of intestinal permeability: A critique. Drug. Disc. Today 2005, 10:335-343.
    • (2005) Drug. Disc. Today , vol.10 , pp. 335-343
    • Balimane, P.V.1    Chong, S.2
  • 192
    • 34247510665 scopus 로고    scopus 로고
    • Hepatocytes-the choice to investigate drug metabolism and toxicity in man: In vitro variability as a reflection of in vivo
    • Gomez-Lechon M., Castell J.V., Donato M.T. Hepatocytes-the choice to investigate drug metabolism and toxicity in man: In vitro variability as a reflection of in vivo. Chemico-Biol. Interactions 2007, 168:30-50.
    • (2007) Chemico-Biol. Interactions , vol.168 , pp. 30-50
    • Gomez-Lechon, M.1    Castell, J.V.2    Donato, M.T.3
  • 193
    • 0014056670 scopus 로고
    • Metabolism, blood levels and rate of excretion of acetohexamide in human subjects
    • Galloway J.A., McMahon R.E., Culp H.W., Marshall F., Young E.C. Metabolism, blood levels and rate of excretion of acetohexamide in human subjects. Diabetes 1965, 16:118-127.
    • (1965) Diabetes , vol.16 , pp. 118-127
    • Galloway, J.A.1    McMahon, R.E.2    Culp, H.W.3    Marshall, F.4    Young, E.C.5
  • 194
    • 0030438721 scopus 로고    scopus 로고
    • Prediction of the human pharmacokinetics of troglitazone, a new and extensively metabolized antidiabetic agent, after oral administration, with an animal scale-up approach
    • Izumi T., Enomoto S., Hosiyama K., Sasahara K., Shibukawa A., Nakagawa T., Suguyama Y. Prediction of the human pharmacokinetics of troglitazone, a new and extensively metabolized antidiabetic agent, after oral administration, with an animal scale-up approach. J. Pharmacol. Exp. Ther. 1996, 277:1630-1641.
    • (1996) J. Pharmacol. Exp. Ther. , vol.277 , pp. 1630-1641
    • Izumi, T.1    Enomoto, S.2    Hosiyama, K.3    Sasahara, K.4    Shibukawa, A.5    Nakagawa, T.6    Suguyama, Y.7
  • 196
    • 0037364162 scopus 로고    scopus 로고
    • ADMET in silico modeling: Towards prediction paradise?
    • van de Waterbeemd H., Gifford E. ADMET in silico modeling: Towards prediction paradise?. Nature Rev. Drug Disc. 2003, 2:192-204.
    • (2003) Nature Rev. Drug Disc. , vol.2 , pp. 192-204
    • van de Waterbeemd, H.1    Gifford, E.2
  • 198
    • 2342444862 scopus 로고    scopus 로고
    • A return to the fundamentals of drug discovery
    • Williams M. A return to the fundamentals of drug discovery. Curr. Opin. Investigational Drugs 2004, 5:29-33.
    • (2004) Curr. Opin. Investigational Drugs , vol.5 , pp. 29-33
    • Williams, M.1
  • 199
    • 4644339418 scopus 로고    scopus 로고
    • Functional pharmacology: The drug discovery bottleneck?
    • Walker M.J.A., Barrett T., Guppy L.J. Functional pharmacology: The drug discovery bottleneck?. Drug Disc. Today 2004, 3:208-215.
    • (2004) Drug Disc. Today , vol.3 , pp. 208-215
    • Walker, M.J.A.1    Barrett, T.2    Guppy, L.J.3
  • 202
    • 0035895513 scopus 로고    scopus 로고
    • What if there were only 30,000 human genes?
    • Claverie J.-M. What if there were only 30,000 human genes?. Science 2001, 291:1255-1257.
    • (2001) Science , vol.291 , pp. 1255-1257
    • Claverie, J.-M.1
  • 203
    • 0034677966 scopus 로고    scopus 로고
    • Drug discovery: A historical perspective
    • Drews J. Drug discovery: A historical perspective. Science 2000, 287:1960-1964.
    • (2000) Science , vol.287 , pp. 1960-1964
    • Drews, J.1
  • 204
    • 0032509889 scopus 로고    scopus 로고
    • Mechanisms of disease: Chemokines-Chemotactic cytokines that mediate inflammation
    • Luster A.D. Mechanisms of disease: Chemokines-Chemotactic cytokines that mediate inflammation. N. Eng. J. Med. 1998, 338:436-445.
    • (1998) N. Eng. J. Med. , vol.338 , pp. 436-445
    • Luster, A.D.1
  • 206
    • 0033811703 scopus 로고    scopus 로고
    • Downregulation of the CCRS beta-chemokine receptor and inhibition of HIV-1 infection by stable VA1-ribozyme chimeric transcripts
    • Cagnon L., Rossi J.J. Downregulation of the CCRS beta-chemokine receptor and inhibition of HIV-1 infection by stable VA1-ribozyme chimeric transcripts. Antisense & Nucleic Acid Drug Development 2000, 10:251-261.
    • (2000) Antisense & Nucleic Acid Drug Development , vol.10 , pp. 251-261
    • Cagnon, L.1    Rossi, J.J.2
  • 209
    • 17944365465 scopus 로고    scopus 로고
    • Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: Synthesis and structure: Activity relationships for 1-[N-(Methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes
    • Finke P.E., Oates B., Mills S.G., MacCoss M., Malkowitz L., Springer M.S., Gould S.L., DeMartino J.A., Carella A., Carver G., et al. Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: Synthesis and structure: Activity relationships for 1-[N-(Methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes. Bioorg. Med. Chem. Lett. 2001, 11:2475-2479.
    • (2001) Bioorg. Med. Chem. Lett. , vol.11 , pp. 2475-2479
    • Finke, P.E.1    Oates, B.2    Mills, S.G.3    MacCoss, M.4    Malkowitz, L.5    Springer, M.S.6    Gould, S.L.7    DeMartino, J.A.8    Carella, A.9    Carver, G.10
  • 213
    • 0031908542 scopus 로고    scopus 로고
    • Production of beta-chemokines in human immunodeficiency virus (HIV) infection: Evidence that high levels of macrophage in inflammatory protein-1-beta are associated with a decreased risk of HIV progression
    • Ullum H., Lepri A.C., Victor J., Aladdin H., Phillips A.N., Gerstoft J., Skinhoj P., Klarlund Pedersen B.K. Production of beta-chemokines in human immunodeficiency virus (HIV) infection: Evidence that high levels of macrophage in inflammatory protein-1-beta are associated with a decreased risk of HIV progression. J. Infect. Dis. 1998, 177:331-336.
    • (1998) J. Infect. Dis. , vol.177 , pp. 331-336
    • Ullum, H.1    Lepri, A.C.2    Victor, J.3    Aladdin, H.4    Phillips, A.N.5    Gerstoft, J.6    Skinhoj, P.7    Klarlund Pedersen, B.K.8
  • 222
    • 0036490096 scopus 로고    scopus 로고
    • Regulators of G-protein signaling as new central nervous system drug targets
    • Neubig R.R., Siderovski D.P. Regulators of G-protein signaling as new central nervous system drug targets. Nature Rev. Drug Disc. 2002, 1:187-196.
    • (2002) Nature Rev. Drug Disc. , vol.1 , pp. 187-196
    • Neubig, R.R.1    Siderovski, D.P.2
  • 223
    • 1342303482 scopus 로고    scopus 로고
    • Of mice and not men: Differences between mouse and human immunology
    • Mestas J., Hughes C.C. Of mice and not men: Differences between mouse and human immunology. J. Immunol. 2004, 172:2731-2738.
    • (2004) J. Immunol. , vol.172 , pp. 2731-2738
    • Mestas, J.1    Hughes, C.C.2
  • 224
    • 0034214841 scopus 로고    scopus 로고
    • NK1 (Substance P) receptor antagonists: Why are they not analgesic in humans?
    • Hill R. NK1 (Substance P) receptor antagonists: Why are they not analgesic in humans?. Trends Pharmacol. Sci. 2000, 21:244-246.
    • (2000) Trends Pharmacol. Sci. , vol.21 , pp. 244-246
    • Hill, R.1
  • 225
    • 0035940445 scopus 로고    scopus 로고
    • SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo
    • Strizki J.M., Xu S., Wagner N.E., Wojcik L., Liu J., Hou Y., Endres M., Palani A., Shapiro S., Clader J.W., et al. SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo. Proc. Natl. Acad. Sci. USA 2001, 98:12718-12723.
    • (2001) Proc. Natl. Acad. Sci. USA , vol.98 , pp. 12718-12723
    • Strizki, J.M.1    Xu, S.2    Wagner, N.E.3    Wojcik, L.4    Liu, J.5    Hou, Y.6    Endres, M.7    Palani, A.8    Shapiro, S.9    Clader, J.W.10
  • 227
    • 0036532579 scopus 로고    scopus 로고
    • Recombinant baculoviruses as mammalian cell gene-delivery vectors
    • Kost T.A., Condreay J.P. Recombinant baculoviruses as mammalian cell gene-delivery vectors. Trends Biotechnol. 2002, 20:173-180.
    • (2002) Trends Biotechnol. , vol.20 , pp. 173-180
    • Kost, T.A.1    Condreay, J.P.2
  • 228
    • 1942517818 scopus 로고    scopus 로고
    • Techniques: Cardiovascular pharmacology and drug discovery in the 21st century
    • Douglas S.A., Ohlstein E.H., Johns D.G. Techniques: Cardiovascular pharmacology and drug discovery in the 21st century. Trends Pharmacol. Sci. 2004, 25:225-233.
    • (2004) Trends Pharmacol. Sci. , vol.25 , pp. 225-233
    • Douglas, S.A.1    Ohlstein, E.H.2    Johns, D.G.3
  • 229
    • 0028838012 scopus 로고
    • Dimerization of cell surface receptors in signal transduction
    • Heldin C.H. Dimerization of cell surface receptors in signal transduction. Cell 1995, 80:213-223.
    • (1995) Cell , vol.80 , pp. 213-223
    • Heldin, C.H.1
  • 230
    • 0036780743 scopus 로고    scopus 로고
    • G-protein-coupled receptor oligomerization and its potential for drug discovery
    • George S.R., O'Dowd B.F., Lee S.P. G-protein-coupled receptor oligomerization and its potential for drug discovery. Nature Rev. Drug Disc. 2002, 1:808-820.
    • (2002) Nature Rev. Drug Disc. , vol.1 , pp. 808-820
    • George, S.R.1    O'Dowd, B.F.2    Lee, S.P.3
  • 231
    • 0034618268 scopus 로고    scopus 로고
    • At1-receptor heterodimers show enhanced G-protein activation and altered receptor sequestration
    • AbdAlla S., Lother H., Quitterer U. At1-receptor heterodimers show enhanced G-protein activation and altered receptor sequestration. Nature 2000, 407:94-98.
    • (2000) Nature , vol.407 , pp. 94-98
    • AbdAlla, S.1    Lother, H.2    Quitterer, U.3
  • 232
    • 0034785580 scopus 로고    scopus 로고
    • Increased AT(1) receptor dimers in preeclampsia mediate enhanced angiotensin II responsiveness
    • AbdAla S., Lother H., el Massiery A., Quitterer U. Increased AT(1) receptor dimers in preeclampsia mediate enhanced angiotensin II responsiveness. Nature Med. 2001, 7:1003-1009.
    • (2001) Nature Med. , vol.7 , pp. 1003-1009
    • AbdAla, S.1    Lother, H.2    el Massiery, A.3    Quitterer, U.4
  • 236
    • 0043069489 scopus 로고    scopus 로고
    • Drug research: Myths, hype, and reality
    • Kubinyi H. Drug research: Myths, hype, and reality. Nature Rev. Drug Disc. 2003, 2:665-668.
    • (2003) Nature Rev. Drug Disc. , vol.2 , pp. 665-668
    • Kubinyi, H.1
  • 237
    • 0033303252 scopus 로고    scopus 로고
    • Pharmacological characterization of receptor-activity-modifying proteins (RAMPs) and the human calcitonin receptor
    • Armour S.L., Foord S., Kenakin T., Chen W.-J. Pharmacological characterization of receptor-activity-modifying proteins (RAMPs) and the human calcitonin receptor. J. Pharmacol. Toxicol. Meth. 1999, 42:217-224.
    • (1999) J. Pharmacol. Toxicol. Meth. , vol.42 , pp. 217-224
    • Armour, S.L.1    Foord, S.2    Kenakin, T.3    Chen, W.-J.4
  • 238
    • 0033054409 scopus 로고    scopus 로고
    • RAMPS: Accessory proteins for seven transmembrane domain receptors
    • Foord S.M., Marshall F.H. RAMPS: Accessory proteins for seven transmembrane domain receptors. Trends Pharmacol. Sci. 1999, 20:184-187.
    • (1999) Trends Pharmacol. Sci. , vol.20 , pp. 184-187
    • Foord, S.M.1    Marshall, F.H.2
  • 239
    • 0033013790 scopus 로고    scopus 로고
    • The amino terminus of receptor activity modifying proteins is a critical determinant of glycosylation state and ligand binding of calcitonin-like receptor
    • Fraser N.J., Wise A., Brown J., McLatchie L.M., Main M.J., Foord S.M. The amino terminus of receptor activity modifying proteins is a critical determinant of glycosylation state and ligand binding of calcitonin-like receptor. Mol. Pharmacol. 1999, 55:1054-1059.
    • (1999) Mol. Pharmacol. , vol.55 , pp. 1054-1059
    • Fraser, N.J.1    Wise, A.2    Brown, J.3    McLatchie, L.M.4    Main, M.J.5    Foord, S.M.6
  • 242
    • 0242499448 scopus 로고    scopus 로고
    • Cytostatic and apoptotic actions of TGF in homeostasis and cancer
    • Siegel P.M., Massague J. Cytostatic and apoptotic actions of TGF in homeostasis and cancer. Nature Rev. Cancer 2003, 3:807-821.
    • (2003) Nature Rev. Cancer , vol.3 , pp. 807-821
    • Siegel, P.M.1    Massague, J.2
  • 244
    • 0023612341 scopus 로고
    • A method to assess concomitant cardiac phosphodiesterase inhibition and positive inotropy
    • Kenakin T.P., Scott D.L. A method to assess concomitant cardiac phosphodiesterase inhibition and positive inotropy. J. Cardiovasc. Pharmacol. 1987, 10:658-666.
    • (1987) J. Cardiovasc. Pharmacol. , vol.10 , pp. 658-666
    • Kenakin, T.P.1    Scott, D.L.2
  • 245
    • 0023108279 scopus 로고
    • An in vivo analysis of purine-mediated renal vasoconstriction in rat isolated kidney
    • Kenakin T.P., Pike N.B. An in vivo analysis of purine-mediated renal vasoconstriction in rat isolated kidney. Br. J. Pharmacol. 1987, 90:373-381.
    • (1987) Br. J. Pharmacol. , vol.90 , pp. 373-381
    • Kenakin, T.P.1    Pike, N.B.2
  • 246
    • 0002370296 scopus 로고
    • Drug and organ selectivity: Similarities and differences
    • Academic Press, New York
    • Kenakin T.P. Drug and organ selectivity: Similarities and differences. Advances in drug research 1985, Vol. 15:71-109. Academic Press, New York.
    • (1985) Advances in drug research , vol.15 , pp. 71-109
    • Kenakin, T.P.1
  • 247
    • 23844474716 scopus 로고    scopus 로고
    • The ultimate model organism: Progress in experimental medicine
    • Littman B.H., Williams S.A. The ultimate model organism: Progress in experimental medicine. Nature Rev. Drug Disc. 2005, 4:631-638.
    • (2005) Nature Rev. Drug Disc. , vol.4 , pp. 631-638
    • Littman, B.H.1    Williams, S.A.2
  • 250
    • 1642401467 scopus 로고    scopus 로고
    • Pharmaceutical productivity: The imperative for new paradigms
    • Milne G.M. Pharmaceutical productivity: The imperative for new paradigms. Annu. Rep. Med. Chem. 2003, 38:383-396.
    • (2003) Annu. Rep. Med. Chem. , vol.38 , pp. 383-396
    • Milne, G.M.1
  • 251
    • 0037107019 scopus 로고    scopus 로고
    • Surrogate endpoints in cancer drug development
    • Sikora K. Surrogate endpoints in cancer drug development. Drug Disc. Today 2002, 7:951-956.
    • (2002) Drug Disc. Today , vol.7 , pp. 951-956
    • Sikora, K.1
  • 253
    • 27144449695 scopus 로고    scopus 로고
    • Designed multiple ligands: An emerging drug discovery paradigm
    • Morphy R., Rankovic Z. Designed multiple ligands: An emerging drug discovery paradigm. J. Med. Chem. 2005, 48:6523-6543.
    • (2005) J. Med. Chem. , vol.48 , pp. 6523-6543
    • Morphy, R.1    Rankovic, Z.2
  • 256
    • 0031051342 scopus 로고    scopus 로고
    • Combined antagonism of leukotrienes and histamine produces predominant inhibition of allergen-induced early and late phase airway obstruction in asthmatics
    • Zhang M., van de Stolpe A., Zuiderveld O., Timmermans H. Combined antagonism of leukotrienes and histamine produces predominant inhibition of allergen-induced early and late phase airway obstruction in asthmatics. Eur. J. Med. Chem. 1997, 32:95-102.
    • (1997) Eur. J. Med. Chem. , vol.32 , pp. 95-102
    • Zhang, M.1    van de Stolpe, A.2    Zuiderveld, O.3    Timmermans, H.4
  • 257
    • 0021857696 scopus 로고
    • The importance of adrenoceptor agonist activity of dobutamine to inotropic selectivity in the anaesthetized cat
    • Kenakin T.P., Johnson S.F. The importance of adrenoceptor agonist activity of dobutamine to inotropic selectivity in the anaesthetized cat. Eur. J. Pharmacol. 1985, 111:347-354.
    • (1985) Eur. J. Pharmacol. , vol.111 , pp. 347-354
    • Kenakin, T.P.1    Johnson, S.F.2
  • 258
    • 8444238556 scopus 로고    scopus 로고
    • Beta-blockers in heart failure: Are pharmacological differences clinically important?
    • Metra M., Dei Cas L., di Lenarda A., Poole-Wilson P. Beta-blockers in heart failure: Are pharmacological differences clinically important?. Heart Fail. Rev. 2004, 9:123-130.
    • (2004) Heart Fail. Rev. , vol.9 , pp. 123-130
    • Metra, M.1    Dei Cas, L.2    di Lenarda, A.3    Poole-Wilson, P.4
  • 259
    • 0021058380 scopus 로고
    • Operational models of pharmacological agonist
    • Black J.W., Leff P. Operational models of pharmacological agonist. Proc. R. Soc. Lond. [Biol.] 1983, 220:141.
    • (1983) Proc. R. Soc. Lond. [Biol.] , vol.220 , pp. 141
    • Black, J.W.1    Leff, P.2
  • 260
    • 0010673662 scopus 로고
    • A modification of receptor theory
    • Stephenson R.P. A modification of receptor theory. Br. J. Pharmacol. 1956, 11:379-393.
    • (1956) Br. J. Pharmacol. , vol.11 , pp. 379-393
    • Stephenson, R.P.1
  • 262
    • 0018909079 scopus 로고
    • Is prenalterol (H 133/80) really a selective beta-1 adrenoceptor agonist? Tissue selectivity resulting from difference in stimulus-response relationships
    • Kenakin T.P., Beek D. Is prenalterol (H 133/80) really a selective beta-1 adrenoceptor agonist? Tissue selectivity resulting from difference in stimulus-response relationships. J. Pharmacol. Exp. Ther.. 1980, 213:406-413.
    • (1980) J. Pharmacol. Exp. Ther.. , vol.213 , pp. 406-413
    • Kenakin, T.P.1    Beek, D.2
  • 263
    • 34548853458 scopus 로고    scopus 로고
    • Allosteric agonist modulators
    • Kenakin T.P. Allosteric agonist modulators. J. Recept. Signal. Transd. 2007, 27:247-259.
    • (2007) J. Recept. Signal. Transd. , vol.27 , pp. 247-259
    • Kenakin, T.P.1
  • 264
    • 0015861774 scopus 로고
    • Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (I50) of an enzymatic reaction
    • Cheng Y.C., Prusoff W.H. Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (I50) of an enzymatic reaction. Biochem. Pharmacol. 1973, 22:3099-3108.
    • (1973) Biochem. Pharmacol. , vol.22 , pp. 3099-3108
    • Cheng, Y.C.1    Prusoff, W.H.2
  • 265
    • 0027522536 scopus 로고
    • Further concerns over Cheng-Prusoff analysis
    • Leff P., Dougall I.G. Further concerns over Cheng-Prusoff analysis. Trends Pharmacol. Sci. 1993, 14:110-112.
    • (1993) Trends Pharmacol. Sci. , vol.14 , pp. 110-112
    • Leff, P.1    Dougall, I.G.2
  • 266
    • 34447624153 scopus 로고    scopus 로고
    • Collateral efficacy in drug discovery: Taking advantage of the good (allosteric) nature of 7TM receptors
    • Kenakin T.P. Collateral efficacy in drug discovery: Taking advantage of the good (allosteric) nature of 7TM receptors. Trends Pharmacol. Sci.. 2007, 28:407-415.
    • (2007) Trends Pharmacol. Sci.. , vol.28 , pp. 407-415
    • Kenakin, T.P.1
  • 267
    • 0030450983 scopus 로고    scopus 로고
    • A novel mechanism of activity-dependent NMDA receptor antagonism describes the effect of ifenprodil in rat cultured cortical neurons
    • Kew J.N.C., Trube G., Kemp J.A. A novel mechanism of activity-dependent NMDA receptor antagonism describes the effect of ifenprodil in rat cultured cortical neurons. J. Physiol. 1996, 497:761-772.
    • (1996) J. Physiol. , vol.497 , pp. 761-772
    • Kew, J.N.C.1    Trube, G.2    Kemp, J.A.3
  • 268
    • 33748325882 scopus 로고    scopus 로고
    • Drug target residence time and its implications for lead optimization
    • Copeland R.A., Pompliano D.L., Meek T.D. Drug target residence time and its implications for lead optimization. Nat. Rev. Drug Disc. 2006, 5::730-739.
    • (2006) Nat. Rev. Drug Disc. , pp. 730-739
    • Copeland, R.A.1    Pompliano, D.L.2    Meek, T.D.3
  • 269
    • 33751183557 scopus 로고    scopus 로고
    • Determining the potency and molecular mechanism of action of insurmountable antagonists
    • Kenakin T.P., Jenkinson S., Watson C. Determining the potency and molecular mechanism of action of insurmountable antagonists. J. Pharmacol. Exp. Ther. 2006, 319:710-723.
    • (2006) J. Pharmacol. Exp. Ther. , vol.319 , pp. 710-723
    • Kenakin, T.P.1    Jenkinson, S.2    Watson, C.3
  • 270
    • 0002177268 scopus 로고
    • The quantitative effects of antagonistic drugs
    • Gaddum J.H. The quantitative effects of antagonistic drugs. J. Physiol. Lond. 1937, 89:7P-9P.
    • (1937) J. Physiol. Lond. , vol.89 , pp. 7P-9P
    • Gaddum, J.H.1
  • 272
    • 84882062420 scopus 로고
    • SAS Institute, Cary, North Carolina, R.J. Freund, C.R. Litell (Eds.)
    • Non-linear models: SAS system recognition 1991, SAS Institute, Cary, North Carolina. R.J. Freund, C.R. Litell (Eds.).
    • (1991) Non-linear models: SAS system recognition
  • 273
    • 0035993439 scopus 로고    scopus 로고
    • Assessing the (a)symmetry of concentration-effect curves: Empirical versus mechanistic models
    • Giraldo J., Vivas N.M., Vila E., Badia A. Assessing the (a)symmetry of concentration-effect curves: Empirical versus mechanistic models. Pharmacol. Therap 2002, 95:21-45.
    • (2002) Pharmacol. Therap , vol.95 , pp. 21-45
    • Giraldo, J.1    Vivas, N.M.2    Vila, E.3    Badia, A.4
  • 274
    • 0033303265 scopus 로고    scopus 로고
    • Development of scintillation-proximity assays for alpha adrenoceptors
    • Gobel J., Saussy D.L., Goetiz A.S. Development of scintillation-proximity assays for alpha adrenoceptors. J. Pharmacol. Toxicol. Meth 1999, 42:2-7.
    • (1999) J. Pharmacol. Toxicol. Meth , vol.42 , pp. 2-7
    • Gobel, J.1    Saussy, D.L.2    Goetiz, A.S.3
  • 275
    • 0003293418 scopus 로고
    • On the nature of the function expressive of the law of human mortality
    • Gompertz B. On the nature of the function expressive of the law of human mortality. Philo. Trans. R. Soc. Lond 1825, 36:513-585.
    • (1825) Philo. Trans. R. Soc. Lond , vol.36 , pp. 513-585
    • Gompertz, B.1
  • 276
    • 0019402921 scopus 로고
    • The measurement of antagonist potency and the importance of selective inhibition of agonist uptake processes
    • Kenakin T.P., Beek D. The measurement of antagonist potency and the importance of selective inhibition of agonist uptake processes. J. Pharmacol. Exp. Ther 1981, 219:112-120.
    • (1981) J. Pharmacol. Exp. Ther , vol.219 , pp. 112-120
    • Kenakin, T.P.1    Beek, D.2
  • 277
    • 4043147979 scopus 로고
    • A flexible growth function for empirical use
    • Richards F.J. A flexible growth function for empirical use. J. Exp. Bot 1959, 10:290-300.
    • (1959) J. Exp. Bot , vol.10 , pp. 290-300
    • Richards, F.J.1
  • 278
  • 279
    • 0033663775 scopus 로고    scopus 로고
    • The use of stimulus-biased assay systems to detect agonist-specific receptor active states: Implications for the trafficking of receptor stimulus by agonists
    • Watson C., Chen G., Irving P.E., Way J., Chen W.-J., Kenakin T.P. The use of stimulus-biased assay systems to detect agonist-specific receptor active states: Implications for the trafficking of receptor stimulus by agonists. Mol. Pharmacol 2000, 58:1230-1238.
    • (2000) Mol. Pharmacol , vol.58 , pp. 1230-1238
    • Watson, C.1    Chen, G.2    Irving, P.E.3    Way, J.4    Chen, W.-J.5    Kenakin, T.P.6
  • 280
    • 0015861774 scopus 로고
    • Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (I50) of an enzymatic reaction
    • Cheng Y.C., Prusoff W.H. Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (I50) of an enzymatic reaction. Biochem. Pharmacol. 1973, 22:3099-3108.
    • (1973) Biochem. Pharmacol. , vol.22 , pp. 3099-3108
    • Cheng, Y.C.1    Prusoff, W.H.2
  • 281
    • 0021947834 scopus 로고
    • Self-cancellation of drug properties as a mode of organ selectivity: The antimuscarinic effects of ambenonium
    • Kenakin T.P., Beek D. Self-cancellation of drug properties as a mode of organ selectivity: The antimuscarinic effects of ambenonium. J. Pharmacol. Exp. Ther. 1985, 232:732-740.
    • (1985) J. Pharmacol. Exp. Ther. , vol.232 , pp. 732-740
    • Kenakin, T.P.1    Beek, D.2
  • 282
    • 1842333847 scopus 로고    scopus 로고
    • Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors
    • Jakubic J., Bacakova L., Lisa V., El-Fakahany E.E., Tucek S. Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol. Pharmacol. 1997, 52:172-179.
    • (1997) Mol. Pharmacol. , vol.52 , pp. 172-179
    • Jakubic, J.1    Bacakova, L.2    Lisa, V.3    El-Fakahany, E.E.4    Tucek, S.5


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