The receptor concept: Pharmacology's big idea

British Journal of Pharmacology

Volumn 147, Issue SUPPL. 1, 2006, Pages

  Rang, H P ^a  

^a UNIVERSITY COLLEGE LONDON   (United Kingdom)

Author keywords

Drug receptors

Indexed keywords

4 AMINOBUTYRIC ACID; G PROTEIN COUPLED RECEPTOR; GUANOSINE DIPHOSPHATE; GUANOSINE TRIPHOSPHATE; RECEPTOR ACTIVITY MODIFYING PROTEIN;

CROSS LINKING; DRUG TARGETING; GENOME; HEART FUNCTION; LIGAND BINDING; MEDICAL RESEARCH; MOLECULAR RECOGNITION; PRIORITY JOURNAL; REVIEW; SIGNAL TRANSDUCTION; TREATMENT RESPONSE;

ANIMALS; HISTORY, 20TH CENTURY; HISTORY, 21ST CENTURY; HUMANS; LIGANDS; PHARMACOLOGY; PORTRAITS; RECEPTORS, CELL SURFACE; SIGNAL TRANSDUCTION;

EID: 30444461377     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1038/sj.bjp.0706457     Document Type: Review

References (37)

1. 3H] alprenolol binding. Proc. Natl. Acad. Sci. U.S.A., 72, 1564-1568.
2. ANGERS, S., SALAHPOUR, A. & BOUVIER, M. (2002). Dimerization: an emerging concept for G protein-coupled receptor ontogeny and function. Annu. Rev. Pharmacol. Toxicol., 42, 409-435.
3. BIRDSALL, N.J. & HULME, E.C. (1976). Biochemical studies on muscarinic acetylcholine receptors. J. Neurochem., 27, 7-16.
4. BLACK, J.W. & LEFF, P. (1983). Operational models of pharmacological agonists. Proc. Roy. Soc. B., 220, 141-162.
5. CHANGEUX, J.-P. & PODLESKI, T. (1968). On the excitability and cooperativity of the electroplax membrane. Proc. Natl. Acad. Sci. U.S.A., 59, 944-950.
6. CLARK, A.J. (1926a). The reaction between acetyl choline and muscle cells. J. Physiol., 61, 530-546.
7. CLARK, A.J. (1926b). The antagonism of acetyl choline by atropine. J. Physiol., 61, 547-556.
8. CLARK, A.J. (1933). The mode of action of drugs on cells. London: Edward Arnold.
9. COLQUHOUN, D. (1973). The relation between classical and cooperative models for drug action. In: Drug Receptors, Rang, H.P. ed. London: Macmillan.
10. COLQUHOUN, D. (1998). Binding, gating, affinity and efficacy: the interpretation of structure-activity relationships for agonists and the effects of mutating receptors. Br. J. Pharmacol., 125, 923-947.
11. COSTA, T. & HERZ, A. (1989). Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. Proc. Natl. Acad. Sci. U.S.A., 86, 7321-7325.
12. DE LEAN, A., STADEL, J.M. & LEFKOWITZ, R.J. (1980). A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor. J. Biol. Chem., 255, 7108-7117.
13. DEL CASTILLO, J. & KATZ, B. (1957). Interaction at end-plate receptors between different choline derivatives. Proc. Roy. Soc. B., 146, 369-381.
14. GADDUM, J.H. (1926). The action of adrenaline and ergotamine on the uterus of the rabbit. J. Physiol., 61, 141-150.
15. GADDUM, J.H. (1937). The quantitative effects of antagonistic drugs. J. Physiol., 89, 6-7P.
16. GETHER, U. (2000). Uncovering molecular mechanisms linked to activation of G protein-coupled receptors. Endocr. Rev., 21, 90-113.
17. GETHER, U. & KOBILKA, B.K. (1998). G protein-coupled receptors. II. Mechanism of agonist activation. J. Biol. Chem., 273, 17979-17982.
18. GILL, E.W. & RANG, H.P. (1966). An alkylating derivative of benzilylcholine with specific and long-lasting parasympatholytic activity. Mol. Pharmacol., 2, 284-297.
19. JENKINSON, D.H. (1960). The antagonism between tubocurarine and substances which depolarise the motor end-plate. J. Physiol., 152, 308-324.
20. JENKINSON, D.H. (1996). Classical approaches to the study of drug-receptor interactions. In: Textbook of Receptor Pharmacology, eds. Foreman, J.C. & Johansen, T. pp 4-62. Boca Raton: CRC Press.
21. KATZ, B. & THESLEFF, S. (1957). A study of the 'desensitization' produced by acetylcholine at the motor end-plate. J. Physiol., 138, 63-80.
22. KENAKIN, T. (1997). Pharmacologic Analysis of Drug-Receptor Interactions, 3rd edn. New York: Lipincott-Raven.
23. KENAKIN, T. (2001). Inverse, protean, and ligand-selective agonism: matters of receptor conformation. FASEB J., 15, 598-611.
24. KENAKIN, T. (2002). Drug efficacy at G protein-coupled receptors. Annu. Rev. Pharmacol. Toxicol., 42, 349-379.
25. MCLATCHIE, L.M., FRASER, N.J., MAIN, M.J., WISE, A., BROWN, J., THOMPSON, N., SOLARI, R., LEE, M.G. & FOORD, S.M. (1998). RAMPs regulate the transport and ligand specificity of the calcitonin-recetor-like-receptor. Nature, 393, 333-339.
26. MILEDI, R., MOLINOFF, P. & POTTER, L.T. (1971). Isolation of the cholinergic receptor protein of Torpedo electric tissue. Nature, 229, 554-557.
27. MONOD, J., WYMAN, J. & CHANGEUX, J.-P. (1965). On the nature of allosteric transitions: a plausible model. J. Mol. Biol., 12, 88-118.
28. NETTLES, K.W. & GREENE, G.L. (2005). Ligand control of coregulator recruitment to nuclear receptors. Annu. Rev. Physiol., 67, 309-333.
29. OSTROM, R.S. & INSEL, P.A. (2004). The evolving role of lipid rafts and caveolae in G protein-coupled receptor signaling: implications for molecular pharmacology. Br. J. Pharmacol., 143, 235-245.
30. PATON, W.D.M. & RANG, H.P. (1965). The uptake of atropine and related drugs by intestinal smooth muscle of the guinea-pig in relation to acetylcholine receptors. Proc. Roy. Soc. Lond. B., 163, 1-44.
31. PEREZ, D.M. & KARNIK, S.S. (2005). Multiple Signaling States of G-Protein-Coupled Receptors. Pharmacol. Rev., 57, 147-161.
32. RANG, H.P. & RITTER, J.M. (1970). On the mechanism of desensitisation at cholinergic receptors. Mol. Pharmacol., 6, 357-382.
33. SCHILD, H.O. (1947). pA, a new scale for the measurement of drug antagonism. Br. J. Pharmacol., 2, 189-206.
34. STEPHENSON, R.P. (1956). A modification of receptor theory. Br. J. Pharmacol., 11, 379-393.
35. TAKEUCHI, A. & TAKEUCHI, N. (1969). A study of the action of picrotoxin on the inhibitory neuromuscular junction of the crayfish. J. Physiol., 205, 377-391.
36. WASER, P.G. (1960). The cholinergic receptor. J. Pharm. Pharmacol., 12, 577-594.
37. WEISS, J.M., MORGAN, P.H., LUTZ, M.W. & KENAKIN, T.P. (1996). The cubic ternary complex receptor occupancy model. (Series of 3 papers). J. Theoret. Biol., 178, 151-167, 169-182, 381-397.