Partial agonism: Mechanisms based on ligand-receptor interactions and on stimulus-response coupling

Journal of Receptor and Signal Transduction Research

Volumn 19, Issue 1-4, 1999, Pages 597-629

  Pliška, Vladimir ^a  

^a ETH ZURICH   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

ARGIPRESSIN; ARGIPRESTOCIN; DIBENAMINE; HISTAMINE; OXYTOCIN; PARTIAL AGONIST;

BINDING KINETICS; CONCENTRATION RESPONSE; CONFERENCE PAPER; CONFORMATIONAL TRANSITION; DRUG RECEPTOR BINDING; EXPERIMENTAL MODEL; LIGAND BINDING; MOLECULAR DYNAMICS; NONHUMAN; PROTEIN QUATERNARY STRUCTURE; REACTION ANALYSIS; RECEPTOR DOWN REGULATION; SIGNAL TRANSDUCTION; STIMULUS RESPONSE; STRUCTURE ACTIVITY RELATION;

EID: 0033065904     PISSN: 10799893     EISSN: None     Source Type: Journal    
DOI: 10.3109/10799899909036675     Document Type: Conference Paper

References (33)

1. Parker, R.B.; and Waud, D.R. Pharmacological estimation of drug-receptor dissociation constants. Statistical evaluation. I. Agonists. J. Pharmacol. exp. Therap. 177, 1-12, 1971.
2. Pliška, V. Dose-response models: similarity with population growth dynamics. Trends Pharmacol. Sci. 8, 50-52, 1987.
3. Clark, A. J. Handbuch der experimentellen Pharmakologie, Ergänzungswerk IV: General Pharmacology, Verlag von Julius Springer, Berlin 1937.
4. Ariëns, E. J.; van Rossum, J. M.; and Simonis, A. M. A theoretical basis of molecular pharmacology. Part I: Interactions of one or two compounds with one receptor system Azneim.-Forsch. 6, 282-293, 1956.
5. Paton, W. D. M. A theory of drug action based on the rate of drug-receptor combination. Proc. Roy. Soc. B 154, 21-69, 1961.
6. Stephenson, R. P. A modification of receptor theory. Brit. J. Pharmacol. 11, 379-393, 1956.
7. 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, 21-55, 1966.
8. Pliška, V. Pharmacological approaches to the identification and classification of myometrial oxytocin receptors. J. Receptor Res. 8, 245-259, 1988.
9. De Lean, A.; Munson, P.J.; and Rodbard, D. Multi-subsite receptors for multivalent ligands. Application to drugs, hormones, and neurotransmitters. Mol. Pharmacol. 15, 60-70, 1979.
10. Black, J.W.; and Leff, P. Operational models of pharmacological agonism. Proc. Roy. Soc. Lond. B 220, 141-162, 1983.
11. Leff, P.; and Harper, D. Do pharmacological methods for quantification of agonists work when the ternary complex mechanism operates? J. theor. Biol. 140, 381-397, 1989.
12. Ariens, E.J.; Simonis, A.M.; and van Rossum, J.M. Drug-receptor interaction: Interaction of one or more drugs with one receptor system. In Molecular Pharmacology. The Mode of Action of Biologically Active Compounds, Vol. I, p. 119-286, edited by E.J. Ariëns, Academic Press, Inc., New York, 1964.
13. Pliška, V. Pharmacological versus binding analysis of receptor systems: How do they interplay? Myometrial cell receptors for oxytocin as a paradigm. Experientia 47, 216-221, 1991.
14. Höltje, H.-D.; and Folkers, G. Molecular Modeling: Basic Principles and Applications, VCH, Weinheim, 1997.
15. Kenakin, T. Agonist-specific receptor conformation. Trends Pharmacol. Sci. 18, 416-417, 1997.
16. Birnbaumer, M. Mutations and diseases of G protein coupled receptors. J. Receptor & Signal Transduction Res. 15, 131-160, 1995.
17. Pliška, V. The role of lipophilicity in biological response to drugs and endogenous ligands. In Methods and Principles in Medicinal Chemistry, Vol. 4: Lipophilicity in Drug Action and Toxicology, edited by V. Pliška, B. Testa, and H. van de Waterbeemd, p. 263-293, VCH, Weinheim, 1996.
18. Pfeiffer, C.C. Optical isomerism and pharmacological action, a generalization. Science 124, 29-31, 1956.
19. Nickerson, M. Receptor occupancy and tissue response. Nature 178, 697-698, 1956.
20. Gosselin, R.E. Drug receptor inactivation: A new kinetic model. Brit. J. Pharmacol. 39, 214P, 1970.
21. Lefkowitz, R.J.; Cotecchia, S.; Samama, P.; and Costa, T. Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins. Trends Pharmacol. Sci. 14, 303-307, 1993.
22. Koshland, D.E. Jr. Regulatory control through conformation changes in proteins. In Advances in Enzyme Regulations, Vol. 6, edited by G. Weber, p. 291-301, Pergamon Press, Oxford, 1968.
23. Lutz, R.A.; Kopp, M.; and Pliška, V. Kinetic analysis of ligand-receptor association data that display an overshoot phenomenon. J. Receptor & Signal Transduction Res. 15, 691-702, 1995.
24. Birnbaumer, L.; and Birnbaumer, M. Signal transduction by G proteins: 1994 edition. J. Receptor & Signal Transduction Res. 15, 213-252, 1995.
25. Ariëns, E.J.; and van Rossum, J.M. Affinity, intrinsic activity and the all-or-none response. Arch. int. pharmacodyn. 113, 89-100, 1957.
26. Grunwald, E.; and Steel, C. Solvent reorganization and thermodynamic enthalpy-entropy compensation. J. Am. Chem. Soc. 117, 5687-5692, 1995.
27. Klebe, G.; and Böhm, H.-J. Energetic and entropie factors determining binding affinity in protein-ligand complexes. J. Receptor & Signal Transduction Res. 17, 459-473, 1997.
28. Ariëns, E.J.; Simonis, A.M.; and van Rossum, J.M. The relation between stimulus and effect. In Molecular Pharmacology. The Mode of Action of Biologically Active Compounds, Vol. I, edited by E.J. Ariëns, p. 394-466, Academic Press, Inc. New York, 1964.
29. 2]-oxytocin Eur. J. Pharmacol. 49, 213-222, 1978.
30. Lindeberg, G.; Vilhardt, H.; Larsson, L.E.; Melin, P.; and Pliška, V. Effect of O-alkylated analogues of lysine vasopressin on adenylate cyclase in pig kidney membranes J. Receptor Res. 1, 389-402, 1980.
31. Ariëns, E.J.; and Simonis, A.M. Autonomic drugs and their receptors. Arch. int. pharmacodyn. 127, 479-496, 1960.
32. Eggena, P.; Schwartz, I.L.; and Walter, R. A sensitive hydroosmotic toad bladder assay. Affinity and intrinsic activity of neurohypophyseal peptides. J. Gen. Physiol. 52, 465-481, 1968.
33. IUPAC-IUB Joint Commission on Biochemical Nomenclature (JCBN). Nomenclature and symbolism for amino acids and peptides. Recommendations 1983. Eur. J. Biochem. 138, 9-37, 1984. Corrections to recommendations 1983: Eur. J. Biochem. 213, 2, 1993.