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Volumn 181, Issue 3, 1996, Pages 273-291

Rational design of receptor partial agonists and possible mechanisms of receptor partial activation: A theory

Author keywords

[No Author keywords available]

Indexed keywords

MEMBRANE RECEPTOR; PARTIAL AGONIST; RECEPTOR BLOCKING AGENT;

EID: 0030573674     PISSN: 00225193     EISSN: None     Source Type: Journal    
DOI: 10.1006/jtbi.1996.0130     Document Type: Article
Times cited : (24)

References (46)
  • 1
    • 77049220618 scopus 로고
    • Affinity and intrinsic activity in the theory of competitive inhibition
    • ARIËNS, E. J. (1954). Affinity and intrinsic activity in the theory of competitive inhibition. Arch. Int. Pharmacodynamie Therapie 99, 32-49.
    • (1954) Arch. Int. Pharmacodynamie Therapie , vol.99 , pp. 32-49
    • Ariëns, E.J.1
  • 2
    • 0011804582 scopus 로고
    • Affinity and intrinsic-activity in the theory of competitive inhibition. Part III. Homologous decamethonium-derivatives and succinyl-cholineesters
    • ARIËNS, E. J. & DE GROOT, W. M. (1954). Affinity and intrinsic-activity in the theory of competitive inhibition. Part III. Homologous decamethonium-derivatives and succinyl-cholineesters. Arch. Intern. Pharmacodynamie Therapie 99, 193-205.
    • (1954) Arch. Intern. Pharmacodynamie Therapie , vol.99 , pp. 193-205
    • Ariëns, E.J.1    De Groot, W.M.2
  • 3
    • 0011876812 scopus 로고
    • Affinity and intrinsic-activity in the theory of competitive-and noncompetitive inhibition and analysis of some forms of dualism in action
    • ARIËNS, E. J., SIMONIS, A. M. & DE GROOT, W. M. (1955). Affinity and intrinsic-activity in the theory of competitive-and noncompetitive inhibition and analysis of some forms of dualism in action. Arch. Int. Pharmacodynamie Therapie 100, 298-322.
    • (1955) Arch. Int. Pharmacodynamie Therapie , vol.100 , pp. 298-322
    • Ariëns, E.J.1    Simonis, A.M.2    De Groot, W.M.3
  • 5
    • 0001341484 scopus 로고
    • A theoretical basis of molecular pharmacology. Part II: Interactions of one or two compounds with two interdependent receptor systems
    • ARIËNS, E. J., VAN ROSSUM, J. M. & SIMONIS, A. M. (1956a). A theoretical basis of molecular pharmacology. Part II: Interactions of one or two compounds with two interdependent receptor systems. Arzneimittel-Forsch. 6, 611-621.
    • (1956) Arzneimittel-forsch. , vol.6 , pp. 611-621
    • Ariëns, E.J.1    Van Rossum, J.M.2    Simonis, A.M.3
  • 7
    • 0004198357 scopus 로고
    • Drug-receptor interaction: Interaction of one or more drugs with one receptor system
    • Ariëns, E. J., ed. New York: Academic Press
    • ARIËNS, E. J., SIMONIS, A. M. & VAN ROSSUM, J. M. (1964a). Drug-receptor interaction: Interaction of one or more drugs with one receptor system. In: Molecular Pharmacology, Vol. I (Ariëns, E. J., ed), pp. 119-286. New York: Academic Press.
    • (1964) Molecular Pharmacology , vol.1 , pp. 119-286
    • Ariëns, E.J.1    Simonis, A.M.2    Van Rossum, J.M.3
  • 8
    • 0000457493 scopus 로고
    • Drug-receptor interaction: Interaction of one or more drugs with different receptor systems
    • Ariëns, E. J., ed. New York: Academic Press
    • ARIËNS, E. J., SIMONIS, A. M. & VAN ROSSUM, J. M. (1964b). Drug-receptor interaction: Interaction of one or more drugs with different receptor systems, in Molecular Pharmacology, Vol. I (Ariëns, E. J., ed), pp. 287-393. New York: Academic Press.
    • (1964) Molecular Pharmacology , vol.1 , pp. 287-393
    • Ariëns, E.J.1    Simonis, A.M.2    Van Rossum, J.M.3
  • 9
    • 0000161089 scopus 로고
    • Receptor theory and structure activity relationships
    • Harper N. J. & Simmonds, A. B., eds. London: Academic Press
    • ARIËNS, E. J. (1966). Receptor theory and structure activity relationships. In: Advances in Drug Research (Harper N. J. & Simmonds, A. B., eds) pp. 235-285. London: Academic Press.
    • (1966) Advances in Drug Research , pp. 235-285
    • Ariëns, E.J.1
  • 11
    • 0021058380 scopus 로고
    • Operational models of pharmacological agonism
    • BLACK, J. W. & LEFF, P. (1983). Operational models of pharmacological agonism. Proc. R. Soc. Lond. B 220, 141-162.
    • (1983) Proc. R. Soc. Lond. B , vol.220 , pp. 141-162
    • Black, J.W.1    Leff, P.2
  • 12
    • 0002838483 scopus 로고
    • Drug receptors and pharmacodynamics
    • Katzung, B. G., ed. Norwalk, CN: Appleton & Lange
    • BOURNE, H. R. & ROBERTS, J. M. (1995). Drug receptors and pharmacodynamics. In: Basic and Clinical Pharmacology - Sixth edition (Katzung, B. G., ed) pp. 9-32. Norwalk, CN: Appleton & Lange.
    • (1995) Basic and Clinical Pharmacology - Sixth Edition , pp. 9-32
    • Bourne, H.R.1    Roberts, J.M.2
  • 13
    • 0002060353 scopus 로고
    • The relation between classical and cooperative models for drug action
    • Rang H. P., ed. London: Academic Press
    • COLQUHOUN, D. (1972). The relation between classical and cooperative models for drug action, in Drug Receptors (Rang H. P., ed) pp. 149-182. London: Academic Press.
    • (1972) Drug Receptors , pp. 149-182
    • Colquhoun, D.1
  • 15
    • 0026659149 scopus 로고
    • Relationship between benzodiazepine receptor occupancy and functional effects in vivo of four ligands of differing intrinsic efficacies
    • FACKLAM, M., SCHOCH, P., BONETTI, E. P., JENCK, F., MARTIN, J. R., MOREAU, J-L. & HAEFELY, W. E. (1992). Relationship between benzodiazepine receptor occupancy and functional effects in vivo of four ligands of differing intrinsic efficacies. J. Pharmacol. Exp. Ther. 261, 1113-1121.
    • (1992) J. Pharmacol. Exp. Ther. , vol.261 , pp. 1113-1121
    • Facklam, M.1    Schoch, P.2    Bonetti, E.P.3    Jenck, F.4    Martin, J.R.5    Moreau, J.-L.6    Haefely, W.E.7
  • 16
    • 0002355204 scopus 로고
    • The use of α-haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes
    • FURCHGOTT, R. F. (1966). The use of α-haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes. Adv. Drug Res. 3, 21-55.
    • (1966) Adv. Drug Res. , vol.3 , pp. 21-55
    • Furchgott, R.F.1
  • 17
    • 84981848149 scopus 로고
    • Comparison of dissociation constants and relative efficacies of selected agonists acting on parasympathetic receptors
    • FURCHGOTT, R. F. & BURSZTYN, P. (1967). Comparison of dissociation constants and relative efficacies of selected agonists acting on parasympathetic receptors. Ann. N. Y. Acad. Sci. 144, 882-898.
    • (1967) Ann. N. Y. Acad. Sci. , vol.144 , pp. 882-898
    • Furchgott, R.F.1    Bursztyn, P.2
  • 18
    • 0023746646 scopus 로고
    • Xamoterol: A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use
    • FURLONG, R. & BROGDEN, R. N. (1988). Xamoterol: A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use. Drugs 36, 455-474.
    • (1988) Drugs , vol.36 , pp. 455-474
    • Furlong, R.1    Brogden, R.N.2
  • 19
    • 0025043989 scopus 로고
    • Novel anxiolytics that act as partial agonists at benzodiazepine receptors
    • HAEFELY, W., MARTIN, J. R. & SCHOCH, P. (1990). Novel anxiolytics that act as partial agonists at benzodiazepine receptors. TiPS 11, 452-456.
    • (1990) TiPS , vol.11 , pp. 452-456
    • Haefely, W.1    Martin, J.R.2    Schoch, P.3
  • 20
    • 0023276499 scopus 로고
    • Pharmacological analysis of the cardiac actions of Xamoterol, a beta adrenoceptor antagonist with partial agonistic activity, in Guinea pig heart: Evidence for involvement of adenylate cyclase system in its cardiac stimulant actions
    • HOTTORI, Y., SAKUMA, I., NAKAO, Y. & KANNO, M. (1987). Pharmacological analysis of the cardiac actions of Xamoterol, a beta adrenoceptor antagonist with partial agonistic activity, in Guinea pig heart: Evidence for involvement of adenylate cyclase system in its cardiac stimulant actions. J. Pharmacol. Exp. Ther. 242, 1077-1085.
    • (1987) J. Pharmacol. Exp. Ther. , vol.242 , pp. 1077-1085
    • Hottori, Y.1    Sakuma, I.2    Nakao, Y.3    Kanno, M.4
  • 21
    • 0021321714 scopus 로고
    • The effects of beta1-adrenoceptor partial agonist ICI 118,587 on left ventricular function in patients with coronary heart disease
    • IKÄHEIMO, M. J. & TAKKUNEN, J. T. (1984). The effects of beta1-adrenoceptor partial agonist ICI 118,587 on left ventricular function in patients with coronary heart disease. Int. J. Cardiol. 5, 339-351.
    • (1984) Int. J. Cardiol. , vol.5 , pp. 339-351
    • Ikäheimo, M.J.1    Takkunen, J.T.2
  • 22
    • 0021215468 scopus 로고
    • Cardioselective, kinetics, hemodynamics, and metabolic effects of xamoterol
    • JENNINGS, G., BOBIK, A., ODDIE, C. & RESTALL, R. (1984). Cardioselective, kinetics, hemodynamics, and metabolic effects of xamoterol. Clin. Pharmacol. Ther. 35, 594-603.
    • (1984) Clin. Pharmacol. Ther. , vol.35 , pp. 594-603
    • Jennings, G.1    Bobik, A.2    Oddie, C.3    Restall, R.4
  • 23
    • 0021211721 scopus 로고
    • The classification of drugs and drug receptors in isolated tissues
    • KENAKIN T. P. (1984). The classification of drugs and drug receptors in isolated tissues. Pharmacol. Rev. 36, 165-222.
    • (1984) Pharmacol. Rev. , vol.36 , pp. 165-222
    • Kenakin, T.P.1
  • 24
    • 0021808471 scopus 로고
    • The quantification of relative efficacy of agonists
    • KENAKIN T. P. (1985). The quantification of relative efficacy of agonists. J. Pharmacol. Methods 13, 281-308.
    • (1985) J. Pharmacol. Methods , vol.13 , pp. 281-308
    • Kenakin, T.P.1
  • 26
    • 0011883711 scopus 로고
    • Pharmakologische eigenschaften einiger langwirksamer cholinesterase-hemmkörper aus der reihe der polymethylen-bis-carbaminoyl-m-trimethylammoniumphenole
    • KRAUPP, O., STUMPF, C., HERZFELD, E. & PILLAT, U. B. (1955). Pharmakologische eigenschaften einiger langwirksamer cholinesterase-hemmkörper aus der reihe der polymethylen-bis-carbaminoyl-m-trimethylammoniumphenole. Arch. Int. Pharmacodynamie Therapie 102, 281-303.
    • (1955) Arch. Int. Pharmacodynamie Therapie , vol.102 , pp. 281-303
    • Kraupp, O.1    Stumpf, C.2    Herzfeld, E.3    Pillat, U.B.4
  • 27
    • 0021831787 scopus 로고
    • 1-adrenoceptor partial agonist, on resting haemodynamic variables and exercise tolerance in patients with left ventricular dysfunction
    • 1-adrenoceptor partial agonist, on resting haemodynamic variables and exercise tolerance in patients with left ventricular dysfunction. Br. Heart J. 54, 17-21.
    • (1985) Br. Heart J. , vol.54 , pp. 17-21
    • Molajo, A.O.1    Bennett, D.H.2
  • 29
    • 0011883902 scopus 로고
    • Steric aspects of adrenergic drugs. II. Effects of dl-isomers and desoxy derivatives on the reserpine-pretreated vas deferens
    • PATIL, P. N., LAPIDUS, J. B. & TYE, A. (1967). Steric aspects of adrenergic drugs. II. Effects of dl-isomers and desoxy derivatives on the reserpine-pretreated vas deferens. J. Pharmacol. Exp. Ther. 115, 1-12.
    • (1967) J. Pharmacol. Exp. Ther. , vol.115 , pp. 1-12
    • Patil, P.N.1    Lapidus, J.B.2    Tye, A.3
  • 31
    • 0022251438 scopus 로고
    • Stereostructure-activity relationship of opioid agonist and antagonist bivalent ligands. Evidence for bridging between vicinal opioid receptors
    • PORTUGESE, P. S., LARSON, D. L., YIM, C. B., SAYRE, L. M., RONSISVALLE, G., LIPKOWSKI, A. W., ET AL. (1985). Stereostructure-activity relationship of opioid agonist and antagonist bivalent ligands. Evidence for bridging between vicinal opioid receptors. J. Med. Chem. 28, 1140-1141.
    • (1985) J. Med. Chem. , vol.28 , pp. 1140-1141
    • Portugese, P.S.1    Larson, D.L.2    Yim, C.B.3    Sayre, L.M.4    Ronsisvalle, G.5    Lipkowski, A.W.6
  • 33
    • 0020583609 scopus 로고
    • 1 partial agonist (Corwin) on left ventricular function and myocardial infarction
    • 1 partial agonist (Corwin) on left ventricular function and myocardial infarction. Am. J. Cardiol. 51, 1267-1274.
    • (1983) Am. J. Cardiol. , vol.51 , pp. 1267-1274
    • Rousseau, M.F.1    Pouleur, H.2    Vincent, M.-F.3
  • 34
    • 0003218218 scopus 로고
    • Endocrine systems: Mechanisms of disease, target cells, and receptors
    • Williams R. H., ed, Philadelphia: W. B. Saunders Co
    • ROTH, J. & GRUNFELD, C. (1981). Endocrine systems: mechanisms of disease, target cells, and receptors. In: Textbook of Endocrinology, sixth edition (Williams R. H., ed), Philadelphia: W. B. Saunders Co.
    • (1981) Textbook of Endocrinology, Sixth Edition
    • Roth, J.1    Grunfeld, C.2
  • 35
    • 0018360305 scopus 로고
    • Receptor interactions of imidazolines. I. Affinity and efficacy for α-adrenergic receptors in rat aorta
    • RUFFOLO, R. R., ROSING, E. L. & WADDEL, J. E. (1979). Receptor interactions of imidazolines. I. Affinity and efficacy for α-adrenergic receptors in rat aorta. J. Pharmacol. Exp. Ther. 209, 429-436.
    • (1979) J. Pharmacol. Exp. Ther. , vol.209 , pp. 429-436
    • Ruffolo, R.R.1    Rosing, E.L.2    Waddel, J.E.3
  • 36
    • 0018903858 scopus 로고
    • Receptor interactions of imidazolines. IV. Structural requirements for alpha adrenergic receptor occupation and receptor activation by clonidine and a series of structural analogs in rat aorta
    • RUFFOLO, R. R., WADDELL, J. E. & YADEN, E. L. (1980). Receptor interactions of imidazolines. IV. Structural requirements for alpha adrenergic receptor occupation and receptor activation by clonidine and a series of structural analogs in rat aorta. J. Pharmacol. Exp. Ther. 213, 267-272.
    • (1980) J. Pharmacol. Exp. Ther. , vol.213 , pp. 267-272
    • Ruffolo, R.R.1    Waddell, J.E.2    Yaden, E.L.3
  • 37
    • 0019984467 scopus 로고
    • Receptor interactions of imidazolines: α-adrenoceptors of rat and rabbit aortae differentiated by relative potencies, affinities and efficacies of imidazoline agonists
    • RUFFOLO, R. R. & WADDELL, J. E. (1982). Receptor interactions of imidazolines: α-adrenoceptors of rat and rabbit aortae differentiated by relative potencies, affinities and efficacies of imidazoline agonists. Br. J. Pharmacol. 77, 169-176.
    • (1982) Br. J. Pharmacol. , vol.77 , pp. 169-176
    • Ruffolo, R.R.1    Waddell, J.E.2
  • 38
    • 0025572437 scopus 로고
    • 1-adrenoceptor partial agonist treatment for congestive heart failure
    • 1-adrenoceptor partial agonist treatment for congestive heart failure. Cardiology 77, 357-366.
    • (1990) Cardiology , vol.77 , pp. 357-366
    • Shabetai, R.1
  • 39
    • 0020078940 scopus 로고
    • Dimeric enkephalins display enhanced affinity and selectivity for the delta opiate receptor
    • SHIMOHIGASHI, Y., COSTA, T., MATSUURA, S., CHEN, H.-C. & RODBARD, D. (1982). Dimeric enkephalins display enhanced affinity and selectivity for the delta opiate receptor. Mol. Pharmacol. 21, 558-563.
    • (1982) Mol. Pharmacol. , vol.21 , pp. 558-563
    • Shimohigashi, Y.1    Costa, T.2    Matsuura, S.3    Chen, H.-C.4    Rodbard, D.5
  • 40
    • 0010673662 scopus 로고
    • A modification of receptor theory
    • STEPHENSON, R. P. (1956). A modification of receptor theory. Br. J. Pharmacol. 11, 379-393.
    • (1956) Br. J. Pharmacol. , vol.11 , pp. 379-393
    • Stephenson, R.P.1
  • 41
    • 0017652208 scopus 로고
    • A model of two functionally antagonistic receptor populations achieved by the same agonist
    • SZABADI, E. (1977). A model of two functionally antagonistic receptor populations achieved by the same agonist. J. theor. Biol. 69, 101-112.
    • (1977) J. Theor. Biol. , vol.69 , pp. 101-112
    • Szabadi, E.1
  • 42
    • 0002163185 scopus 로고
    • Molecular basis of pharmacologic selectivity
    • Pratt W. B. & Taylor P., eds. New York: Churchill Livingstone
    • TAYLOR, P. & INSEL, P. A. (1990). Molecular basis of pharmacologic selectivity. In: Principles of Drug Actions - The Basis of Pharmacology, Third edition (Pratt W. B. & Taylor P., eds) pp. 1-102. New York: Churchill Livingstone.
    • (1990) Principles of Drug Actions - The Basis of Pharmacology, Third Edition , pp. 1-102
    • Taylor, P.1    Insel, P.A.2
  • 43
    • 0015535998 scopus 로고
    • On the analysis of pharmacological experiments in term of an allosteric receptor model
    • THRON, C. D. (1973). On the analysis of pharmacological experiments in term of an allosteric receptor model. Mol. Pharmacol. 9, 1-9.
    • (1973) Mol. Pharmacol. , vol.9 , pp. 1-9
    • Thron, C.D.1
  • 44
    • 84965047860 scopus 로고
    • Pharmacodynamics of drugs affecting skeletal muscle. Structure-action relationships in homologous series of quaternary ammonium salts
    • VAN ROSSUM, J. M. & ARIËNS, E. J. (1959a). Pharmacodynamics of drugs affecting skeletal muscle. Structure-action relationships in homologous series of quaternary ammonium salts. Arch. Int. Pharmacodynamie Therapie 118, 393-417.
    • (1959) Arch. Int. Pharmacodynamie Therapie , vol.118 , pp. 393-417
    • Van Rossum, J.M.1    Ariëns, E.J.2
  • 45
    • 84965076157 scopus 로고
    • Pharmacodynamics of parasympathetic drugs. Structure-action relationships in homologous series of quaternary ammonium salts
    • VAN ROSSUM, J. M. & ARIËNS, E. J. (1959b). Pharmacodynamics of parasympathetic drugs. Structure-action relationships in homologous series of quaternary ammonium salts. Arch. Int. Pharmacodynamie Therapie 118, 418-446.
    • (1959) Arch. Int. Pharmacodynamie Therapie , vol.118 , pp. 418-446
    • Van Rossum, J.M.1    Ariëns, E.J.2
  • 46
    • 0027300816 scopus 로고
    • The competitive and noncompetitive antagonism of receptor-mediated drug actions in the presence of spare receptors
    • ZHU, B. T. (1993). The competitive and noncompetitive antagonism of receptor-mediated drug actions in the presence of spare receptors. J. Pharmacol. Toxicol. Methods 29, 85-91.
    • (1993) J. Pharmacol. Toxicol. Methods , vol.29 , pp. 85-91
    • Zhu, B.T.1


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