메뉴 건너뛰기




Volumn 58, Issue 5, 1999, Pages 735-748

Qualitative and quantitative assessment of relative agonist efficacy

Author keywords

Affinity; Agonism; Concentration response analysis; Intrinsic efficacy; Radioligand binding; Receptor theory

Indexed keywords

ACETYLCHOLINE; METHYLSCOPOLAMINE; MUSCARINIC M1 RECEPTOR; PARTIAL AGONIST; PILOCARPINE; RADIOLIGAND;

EID: 0032777107     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-2952(99)00087-8     Document Type: Review
Times cited : (48)

References (77)
  • 2
    • 0032127619 scopus 로고    scopus 로고
    • The elusive nature of intrinsic efficacy
    • Clarke W.P., Bond R.A. The elusive nature of intrinsic efficacy. Trends Pharmacol Sci. 19:1998;270-276.
    • (1998) Trends Pharmacol Sci , vol.19 , pp. 270-276
    • Clarke, W.P.1    Bond, R.A.2
  • 4
    • 77049220618 scopus 로고
    • Affinity and intrinsic activity in the theory of competitive inhibition
    • Ariëns E.J. Affinity and intrinsic activity in the theory of competitive inhibition. Arch Int Pharmacodyn Ther. 99:1954;32-49.
    • (1954) Arch Int Pharmacodyn Ther , vol.99 , pp. 32-49
    • Ariëns, E.J.1
  • 5
    • 0010673662 scopus 로고
    • A modification of receptor theory
    • Stephenson R.P. A modification of receptor theory. Br J Pharmacol. 11:1956;379-393.
    • (1956) Br J Pharmacol , vol.11 , pp. 379-393
    • Stephenson, R.P.1
  • 6
    • 0002355204 scopus 로고
    • The use of β-haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes
    • Furchgott R.F. The use of β-haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes. Adv Drug Res. 3:1966;21-55.
    • (1966) Adv Drug Res , vol.3 , pp. 21-55
    • Furchgott, R.F.1
  • 7
    • 84965075853 scopus 로고
    • A study of the 'desensitization' produced by acetylcholine at the motor end-plate
    • Katz B., Thesleff S. A study of the 'desensitization' produced by acetylcholine at the motor end-plate. J Physiol (Lond). 138:1957;63-80.
    • (1957) J Physiol (Lond) , vol.138 , pp. 63-80
    • Katz, B.1    Thesleff, S.2
  • 8
    • 0026320866 scopus 로고
    • The energy landscapes and motions of proteins
    • Frauenfelder H., Sligar S.G., Wolynes P.G. The energy landscapes and motions of proteins. Science. 254:1991;1598-1603.
    • (1991) Science , vol.254 , pp. 1598-1603
    • Frauenfelder, H.1    Sligar, S.G.2    Wolynes, P.G.3
  • 9
    • 0016139387 scopus 로고
    • Membrane receptors
    • Cuatrecasas P. Membrane receptors. Annu Rev Biochem. 43:1974;169-214.
    • (1974) Annu Rev Biochem , vol.43 , pp. 169-214
    • Cuatrecasas, P.1
  • 10
    • 0019137579 scopus 로고
    • A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled β-adrenergic receptor
    • De Lean A., Stadel J.M., Lefkowitz R.J. A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled β-adrenergic receptor. J Biol Chem. 255:1980;7108-7117.
    • (1980) J Biol Chem , vol.255 , pp. 7108-7117
    • De Lean, A.1    Stadel, J.M.2    Lefkowitz, R.J.3
  • 13
    • 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 I. Model description. J Theor Biol. 178:1996;151-167.
    • (1996) J Theor Biol , vol.178 , pp. 151-167
    • Weiss, J.M.1    Morgan, P.H.2    Lutz, M.W.3    Kenakin, T.P.4
  • 14
    • 0030797086 scopus 로고    scopus 로고
    • Transduction is a major factor influencing receptor characterization
    • Spedding M., Dacquet C. Transduction is a major factor influencing receptor characterization. Ann NY Acad Sci. 812:1997;29-40.
    • (1997) Ann NY Acad Sci , vol.812 , pp. 29-40
    • Spedding, M.1    Dacquet, C.2
  • 15
    • 0029048987 scopus 로고
    • On the importance of the "antagonist assumption" to how receptors express themselves
    • Kenakin T., Morgan P., Lutz M. On the importance of the "antagonist assumption" to how receptors express themselves. Biochem Pharmacol. 50:1995;17-26.
    • (1995) Biochem Pharmacol , vol.50 , pp. 17-26
    • Kenakin, T.1    Morgan, P.2    Lutz, M.3
  • 17
    • 0027297275 scopus 로고
    • Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins
    • Lefkowitz R.J., Cotecchia S., Samama P., Costa T. Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins. Trends Pharmacol Sci. 14:1993;303-307.
    • (1993) Trends Pharmacol Sci , vol.14 , pp. 303-307
    • Lefkowitz, R.J.1    Cotecchia, S.2    Samama, P.3    Costa, T.4
  • 18
    • 0024578265 scopus 로고
    • Challenges for receptor theory as a tool for drug and drug receptor classification
    • Kenakin T.P. Challenges for receptor theory as a tool for drug and drug receptor classification. Trends Pharmacol Sci. 10:1989;18-22.
    • (1989) Trends Pharmacol Sci , vol.10 , pp. 18-22
    • Kenakin, T.P.1
  • 19
    • 0001708862 scopus 로고
    • Receptor occupancy and tissue response
    • Nickerson M. Receptor occupancy and tissue response. Nature. 178:1956;697-698.
    • (1956) Nature , vol.178 , pp. 697-698
    • Nickerson, M.1
  • 20
    • 85178112770 scopus 로고    scopus 로고
    • Classic approaches to the study of drug-receptor interactions
    • J.C. Foreman, & T. Johansen. Boca Raton: CRC Press
    • Jenkinson D.H. Classic approaches to the study of drug-receptor interactions. Foreman J.C., Johansen T. Textbook of Receptor Pharmacology. 1996;3-62 CRC Press, Boca Raton.
    • (1996) Textbook of Receptor Pharmacology , pp. 3-62
    • Jenkinson, D.H.1
  • 21
    • 0029025454 scopus 로고
    • Extended concentration-response curves used to reflect full agonist efficacies and receptor occupancy-response coupling ranges
    • Lew M.J. Extended concentration-response curves used to reflect full agonist efficacies and receptor occupancy-response coupling ranges. Br J Pharmacol. 115:1995;745-752.
    • (1995) Br J Pharmacol , vol.115 , pp. 745-752
    • Lew, M.J.1
  • 22
    • 0017652208 scopus 로고
    • A model of two functionally antagonistic receptor populations activated by the same agonist
    • Szabadi E. A model of two functionally antagonistic receptor populations activated by the same agonist. J Theor Biol. 69:1977;101-112.
    • (1977) J Theor Biol , vol.69 , pp. 101-112
    • Szabadi, E.1
  • 23
    • 0028239058 scopus 로고
    • Lower efficacy: Interaction with an inhibitory receptor or partial agonism?
    • Rovati G.E., Nicosia S. Lower efficacy Interaction with an inhibitory receptor or partial agonism? Trends Pharmacol Sci. 15:1994;140-144.
    • (1994) Trends Pharmacol Sci , vol.15 , pp. 140-144
    • Rovati, G.E.1    Nicosia, S.2
  • 24
    • 0028360632 scopus 로고
    • Models to explain dose-response relationships that exhibit a downturn phase
    • Pliska V. Models to explain dose-response relationships that exhibit a downturn phase. Trends Pharmacol Sci. 15:1994;178-181.
    • (1994) Trends Pharmacol Sci , vol.15 , pp. 178-181
    • Pliska, V.1
  • 25
    • 0021808471 scopus 로고
    • The quantification of relative efficacy of agonists
    • Kenakin T.P. The quantification of relative efficacy of agonists. J Pharmacol Methods. 13:1985;281-308.
    • (1985) J Pharmacol Methods , vol.13 , pp. 281-308
    • Kenakin, T.P.1
  • 26
    • 0013866946 scopus 로고
    • A general analysis of the receptor-drug interaction
    • Mackay D. A general analysis of the receptor-drug interaction. Br J Pharmacol. 26:1966;9-16.
    • (1966) Br J Pharmacol , vol.26 , pp. 9-16
    • MacKay, D.1
  • 27
    • 84981848149 scopus 로고
    • Comparison of dissociation constants and of relative efficacies of selected agonists acting on parasympathetic receptors
    • Furchgott R., Bursztyn P. Comparison of dissociation constants and of relative efficacies of selected agonists acting on parasympathetic receptors. Ann NY Acad Sci. 144:1967;882-899.
    • (1967) Ann NY Acad Sci , vol.144 , pp. 882-899
    • Furchgott, R.1    Bursztyn, P.2
  • 28
    • 0021058380 scopus 로고
    • Operational models of pharmacological agonism
    • Black J.W., Leff P. Operational models of pharmacological agonism. Proc R Soc Lond B. 220:1983;141-162.
    • (1983) Proc R Soc Lond B , vol.220 , pp. 141-162
    • Black, J.W.1    Leff, P.2
  • 29
    • 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. 84:1985;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
  • 30
    • 0014123460 scopus 로고
    • The affinity and efficacy of onium salts on the frog rectus abdominis
    • Barlow R.B., Scott N.C., Stephenson R.P. The affinity and efficacy of onium salts on the frog rectus abdominis. Br J Pharmacol. 31:1967;188-196.
    • (1967) Br J Pharmacol , vol.31 , pp. 188-196
    • Barlow, R.B.1    Scott, N.C.2    Stephenson, R.P.3
  • 31
    • 0025212261 scopus 로고
    • Estimation of agonist affinity and efficacy by direct, operational model-fitting
    • Leff P., Prentice D.J., Giles H., Martin G.R., Wood J. Estimation of agonist affinity and efficacy by direct, operational model-fitting. J Pharmacol Methods. 23:1990;225-237.
    • (1990) J Pharmacol Methods , vol.23 , pp. 225-237
    • Leff, P.1    Prentice, D.J.2    Giles, H.3    Martin, G.R.4    Wood, J.5
  • 32
    • 0014599320 scopus 로고
    • On the measurement of the affinity of partial agonists for receptors
    • Waud D.R. On the measurement of the affinity of partial agonists for receptors. J Pharmacol Exp Ther. 170:1969;117-122.
    • (1969) J Pharmacol Exp Ther , vol.170 , pp. 117-122
    • Waud, D.R.1
  • 33
    • 0025800971 scopus 로고
    • Determination of the functional dissociation constant of a partial agonist by comparison with a higher efficacy agonist
    • Freeman K.A., Tallarida R.J. Determination of the functional dissociation constant of a partial agonist by comparison with a higher efficacy agonist. J Pharmacol Methods. 25:1991;11-18.
    • (1991) J Pharmacol Methods , vol.25 , pp. 11-18
    • Freeman, K.A.1    Tallarida, R.J.2
  • 35
    • 0002134457 scopus 로고
    • Affinity, efficacy, and receptor classification: Is the classic theory still useful?
    • J.W. Black, D.H. Jenkinson, & V.P. Gerskowitch. New York: Alan R. Liss
    • Colquhoun D. Affinity, efficacy, and receptor classification Is the classic theory still useful? Black J.W., Jenkinson D.H., Gerskowitch V.P. Perspectives on Receptor Classification. 1987;103-114 Alan R. Liss, New York.
    • (1987) Perspectives on Receptor Classification , pp. 103-114
    • Colquhoun, D.1
  • 36
    • 0025141367 scopus 로고
    • Errors in agonist affinity estimation: Do they and should they occur in isolated tissue experiments?
    • Leff P., Dougall I.G., Harper D.H., Dainty I.A. Errors in agonist affinity estimation Do they and should they occur in isolated tissue experiments? Trends Pharmacol Sci. 11:1990;64-67.
    • (1990) Trends Pharmacol Sci , vol.11 , pp. 64-67
    • Leff, P.1    Dougall, I.G.2    Harper, D.H.3    Dainty, I.A.4
  • 37
    • 0002867860 scopus 로고
    • Strategy and tactics in receptor-binding studies
    • E.C. Hulme. New York: Oxford University Press
    • Hulme E.C., Birdsall N.J.M. Strategy and tactics in receptor-binding studies. Hulme E.C. Receptor-Ligand Interactions. A Practical Approach. 1992;63-176 Oxford University Press, New York.
    • (1992) Receptor-Ligand Interactions. a Practical Approach , pp. 63-176
    • Hulme, E.C.1    Birdsall, N.J.M.2
  • 38
    • 0030797087 scopus 로고    scopus 로고
    • To what extent can binding studies allow the quantification of affinity and efficacy?
    • Birdsall N.J.M., Lazareno S. To what extent can binding studies allow the quantification of affinity and efficacy? Ann NY Acad Sci. 812:1997;41-47.
    • (1997) Ann NY Acad Sci , vol.812 , pp. 41-47
    • Birdsall, N.J.M.1    Lazareno, S.2
  • 39
    • 0032030621 scopus 로고    scopus 로고
    • Rethinking receptor-G protein-effector interactions
    • Chidiac P. Rethinking receptor-G protein-effector interactions. Biochem Pharmacol. 55:1998;549-556.
    • (1998) Biochem Pharmacol , vol.55 , pp. 549-556
    • Chidiac, P.1
  • 41
    • 0029150088 scopus 로고
    • Modulation of agonist binding by guanine nucleotides in CHO cells expressing muscarinic m1-m5 receptors
    • Van Giersbergen P.L.M., Leppik R. Modulation of agonist binding by guanine nucleotides in CHO cells expressing muscarinic m1-m5 receptors. Naunyn Schmiedebergs Arch Pharmacol. 352:1995;166-172.
    • (1995) Naunyn Schmiedebergs Arch Pharmacol , vol.352 , pp. 166-172
    • Van Giersbergen, P.L.M.1    Leppik, R.2
  • 42
    • 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. 28:1985;410-421.
    • (1985) Mol Pharmacol , vol.28 , pp. 410-421
    • Ehlert, F.J.1
  • 43
    • 0029812311 scopus 로고    scopus 로고
    • The classification of seven transmembrane receptors in recombinant expression systems
    • Kenakin T. The classification of seven transmembrane receptors in recombinant expression systems. Pharmacol Rev. 48:1996;413-463.
    • (1996) Pharmacol Rev , vol.48 , pp. 413-463
    • Kenakin, T.1
  • 44
    • 0031434924 scopus 로고    scopus 로고
    • Differences between natural and recombinant G protein-coupled receptor systems with varying receptor/G protein stoichiometry
    • Kenakin T. Differences between natural and recombinant G protein-coupled receptor systems with varying receptor/G protein stoichiometry. Trends Pharmacol Sci. 18:1997;456-464.
    • (1997) Trends Pharmacol Sci , vol.18 , pp. 456-464
    • Kenakin, T.1
  • 45
    • 0019790028 scopus 로고
    • Conformational changes and drug action
    • Burgen A.S.V. Conformational changes and drug action. Fedn Proc. 40:1981;2723-2728.
    • (1981) Fedn Proc , vol.40 , pp. 2723-2728
    • Burgen, A.S.V.1
  • 47
    • 0026548156 scopus 로고
    • In vitro mutagenesis and the search for structure-function relationships among G protein-coupled receptors
    • Savarese T.M., Fraser C.M. In vitro mutagenesis and the search for structure-function relationships among G protein-coupled receptors. Biochem J. 283:1992;1-19.
    • (1992) Biochem J , vol.283 , pp. 1-19
    • Savarese, T.M.1    Fraser, C.M.2
  • 49
    • 0031029841 scopus 로고    scopus 로고
    • Constitutively active G protein-coupled receptors: Potential mechanisms of receptor activation
    • Scheer A., Cotecchia S. Constitutively active G protein-coupled receptors Potential mechanisms of receptor activation . J Recept Signal Transduct Res. 17:1997;57-73.
    • (1997) J Recept Signal Transduct Res , vol.17 , pp. 57-73
    • Scheer, A.1    Cotecchia, S.2
  • 51
    • 0025212680 scopus 로고
    • 1-adrenergic receptor involved in coupling to phosphatidylinositol hydrolysis and enhanced sensitivity of biological function
    • 1-adrenergic receptor involved in coupling to phosphatidylinositol hydrolysis and enhanced sensitivity of biological function. Proc Natl Acad Sci USA. 87:1990;2896-2900.
    • (1990) Proc Natl Acad Sci USA , vol.87 , pp. 2896-2900
    • Cotecchia, S.1    Exum, S.2    Caron, M.G.3    Lefkowitz, R.J.4
  • 53
    • 0029054965 scopus 로고
    • Agonist-receptor efficacy. II: Agonist trafficking of receptor signals
    • Kenakin T. Agonist-receptor efficacy. II Agonist trafficking of receptor signals . Trends Pharmacol Sci. 16:1995;232-238.
    • (1995) Trends Pharmacol Sci , vol.16 , pp. 232-238
    • Kenakin, T.1
  • 54
    • 0029061611 scopus 로고
    • Agonist-receptor efficacy. I: Mechanisms of efficacy and receptor promiscuity
    • Kenakin T. Agonist-receptor efficacy. I Mechanisms of efficacy and receptor promiscuity . Trends Pharmacol Sci. 16:1995;188-192.
    • (1995) Trends Pharmacol Sci , vol.16 , pp. 188-192
    • Kenakin, T.1
  • 55
    • 0030049488 scopus 로고    scopus 로고
    • Constitutive activation of a single effector pathway: Evidence for multiple activation states of a G protein-coupled receptor
    • Perez D.M., Hwa J., Gaivin R., Mathur M., Brown F., Graham R.M. Constitutive activation of a single effector pathway Evidence for multiple activation states of a G protein-coupled receptor . Mol Pharmacol. 49:1996;112-122.
    • (1996) Mol Pharmacol , vol.49 , pp. 112-122
    • Perez, D.M.1    Hwa, J.2    Gaivin, R.3    Mathur, M.4    Brown, F.5    Graham, R.M.6
  • 56
    • 0031815337 scopus 로고    scopus 로고
    • Effector pathway-dependent relative efficacy at serotonin type 2A and 2C receptors: Evidence for agonist-directed trafficking of receptor stimulus
    • Berg K.A., Maayani S., Goldfarb J., Scaramellini C., Leff P., Clarke W.P. Effector pathway-dependent relative efficacy at serotonin type 2A and 2C receptors Evidence for agonist-directed trafficking of receptor stimulus . Mol Pharmacol. 54:1998;94-104.
    • (1998) Mol Pharmacol , vol.54 , pp. 94-104
    • Berg, K.A.1    Maayani, S.2    Goldfarb, J.3    Scaramellini, C.4    Leff, P.5    Clarke, W.P.6
  • 57
    • 0030671469 scopus 로고    scopus 로고
    • Agonist-specific receptor conformations
    • Kenakin T. Agonist-specific receptor conformations. Trends Pharmacol Sci. 18:1997;416-417.
    • (1997) Trends Pharmacol Sci , vol.18 , pp. 416-417
    • Kenakin, T.1
  • 58
    • 0001169515 scopus 로고
    • Antagonists with negative intrinsic activity at δ opioid receptors coupled to GTP-binding proteins
    • Costa T., Herz A. Antagonists with negative intrinsic activity at δ opioid receptors coupled to GTP-binding proteins. Proc Natl Acad Sci USA. 86:1989;7321-7325.
    • (1989) Proc Natl Acad Sci USA , vol.86 , pp. 7321-7325
    • Costa, T.1    Herz, A.2
  • 59
    • 0026608113 scopus 로고
    • Drug efficacy at guanine nucleotide-binding regulatory protein-linked receptors: Thermodynamic interpretation of negative antagonism and of receptor activity in the absence of ligand
    • Costa T., Ogino Y., Munson P.J., Onaran H.O., Rodbard D. Drug efficacy at guanine nucleotide-binding regulatory protein-linked receptors Thermodynamic interpretation of negative antagonism and of receptor activity in the absence of ligand . Mol Pharmacol. 41:1992;549-560.
    • (1992) Mol Pharmacol , vol.41 , pp. 549-560
    • Costa, T.1    Ogino, Y.2    Munson, P.J.3    Onaran, H.O.4    Rodbard, D.5
  • 61
    • 0344584211 scopus 로고
    • Reciprocal modulation of agonist and antagonist binding to muscarinic cholinergic receptor by guanine nucleotide
    • Bürgisser E., De Lean A., Lefkowitz R.J. Reciprocal modulation of agonist and antagonist binding to muscarinic cholinergic receptor by guanine nucleotide. Proc Natl Acad Sci USA. 79:1982;1732-1736.
    • (1982) Proc Natl Acad Sci USA , vol.79 , pp. 1732-1736
    • Bürgisser, E.1    De Lean, A.2    Lefkowitz, R.J.3
  • 62
    • 0028856707 scopus 로고
    • 2 adrenergic receptor. Evidence for ligand-specific conformational changes
    • 2 adrenergic receptor. Evidence for ligand-specific conformational changes. J Biol Chem. 270:1995;28268-28275.
    • (1995) J Biol Chem , vol.270 , pp. 28268-28275
    • Gether, U.1    Lin, S.2    Kobilka, B.K.3
  • 63
    • 0031018485 scopus 로고    scopus 로고
    • Structural instability of a constitutively active G protein-coupled receptor. Agonist-independent activation due to conformational flexibility
    • Gether U., Ballesteros J.A., Seifer R., Sanders-Bush E., Weinstein H., Kobilka B.K. Structural instability of a constitutively active G protein-coupled receptor. Agonist-independent activation due to conformational flexibility. J Biol Chem. 272:1997;2587-2590.
    • (1997) J Biol Chem , vol.272 , pp. 2587-2590
    • Gether, U.1    Ballesteros, J.A.2    Seifer, R.3    Sanders-Bush, E.4    Weinstein, H.5    Kobilka, B.K.6
  • 64
    • 0027375964 scopus 로고
    • Molecular mechanisms of membrane receptor desensitization
    • Lohse M.J. Molecular mechanisms of membrane receptor desensitization. Biochim Biophys Acta. 1179:1993;171-188.
    • (1993) Biochim Biophys Acta , vol.1179 , pp. 171-188
    • Lohse, M.J.1
  • 65
    • 0019158736 scopus 로고
    • Catecholamine-specific desensitization of adenylate cyclase. Evidence for a multistep process
    • Su Y.-F., Harden T.K., Perkins J.P. Catecholamine-specific desensitization of adenylate cyclase. Evidence for a multistep process. J Biol Chem. 255:1980;7410-7419.
    • (1980) J Biol Chem , vol.255 , pp. 7410-7419
    • Su, Y.-F.1    Harden, T.K.2    Perkins, J.P.3
  • 66
    • 0025856977 scopus 로고
    • Effects of agonist efficacy on desensitization of phosphoinositide hydrolysis mediated by m1 and m3 muscarinic receptors expressed in Chinese hamster ovary cells
    • Hu J., Wang S.-Z., El-Fakahany E.E. Effects of agonist efficacy on desensitization of phosphoinositide hydrolysis mediated by m1 and m3 muscarinic receptors expressed in Chinese hamster ovary cells. J Pharmacol Exp Ther. 257:1991;938-945.
    • (1991) J Pharmacol Exp Ther , vol.257 , pp. 938-945
    • Hu, J.1    Wang, S.-Z.2    El-Fakahany, E.E.3
  • 67
    • 0028330786 scopus 로고
    • Differential expression of the β-adrenergic receptor modifies agonist stimulation of adenylyl cyclase: A quantitative evaluation
    • Whaley B., Yuan N., Birnbaumer L., Clark R.B., Barber R. Differential expression of the β-adrenergic receptor modifies agonist stimulation of adenylyl cyclase A quantitative evaluation . Mol Pharmacol. 45:1994;481-489.
    • (1994) Mol Pharmacol , vol.45 , pp. 481-489
    • Whaley, B.1    Yuan, N.2    Birnbaumer, L.3    Clark, R.B.4    Barber, R.5
  • 69
    • 0023858575 scopus 로고
    • β-Adrenergic receptor kinase. Activity of partial agonists for stimulation of adenylate cyclase correlates with ability to promote receptor phosphorylation
    • Benovic J.L., Staniszewski C., Mayor F. Jr, Caron M.G., Lefkowitz R.J. β-Adrenergic receptor kinase. Activity of partial agonists for stimulation of adenylate cyclase correlates with ability to promote receptor phosphorylation. J Biol Chem. 263:1988;3893-3897.
    • (1988) J Biol Chem , vol.263 , pp. 3893-3897
    • Benovic, J.L.1    Staniszewski, C.2    Mayor F., Jr.3    Caron, M.G.4    Lefkowitz, R.J.5
  • 71
    • 0031969377 scopus 로고    scopus 로고
    • The relationship between agonist intrinsic activity and the rate of endocytosis of muscarinic receptors in a human neuroblastoma cell line
    • Szekeres P.G., Koenig J.A., Edwardson J.M. The relationship between agonist intrinsic activity and the rate of endocytosis of muscarinic receptors in a human neuroblastoma cell line. Mol Pharmacol. 53:1998;759-765.
    • (1998) Mol Pharmacol , vol.53 , pp. 759-765
    • Szekeres, P.G.1    Koenig, J.A.2    Edwardson, J.M.3
  • 72
    • 0025726761 scopus 로고
    • In vitro down-regulation predicts agonist efficacy at central muscarinic cholinergic receptors
    • Stoll L., Muller W.E. In vitro down-regulation predicts agonist efficacy at central muscarinic cholinergic receptors. Biochem Pharmacol. 41:1991;1963-1966.
    • (1991) Biochem Pharmacol , vol.41 , pp. 1963-1966
    • Stoll, L.1    Muller, W.E.2
  • 75
    • 0029117884 scopus 로고
    • Increased basal phosphorylation of the constitutively active serotonin 2C receptor accompanies agonist-mediated desensitization
    • Westphal R.S., Backstrom J.R., Sanders-Bush E. Increased basal phosphorylation of the constitutively active serotonin 2C receptor accompanies agonist-mediated desensitization. Mol Pharmacol. 48:1995;200-205.
    • (1995) Mol Pharmacol , vol.48 , pp. 200-205
    • Westphal, R.S.1    Backstrom, J.R.2    Sanders-Bush, E.3
  • 77
    • 0001870572 scopus 로고    scopus 로고
    • Agonist efficacy and allosteric models of receptor activation
    • Onaran H.O., Costa T. Agonist efficacy and allosteric models of receptor activation. Ann NY Acad Sci. 812:1997;98-115.
    • (1997) Ann NY Acad Sci , vol.812 , pp. 98-115
    • Onaran, H.O.1    Costa, T.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.