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Download PDF by H. P. Rang: Drug Receptors: A Symposium

By H. P. Rang

ISBN-10: 1349009105

ISBN-13: 9781349009107

ISBN-10: 1349009121

ISBN-13: 9781349009121

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Classification by antagonists Probably the most widely accepted basis of receptor classification is by way of the affinity constants of competitive antagonists, which are readily measurable. Affinity constants of competitive antagonists, can help in the classification of both drugs and receptors. Two simple principles are involved which are a consequence of receptor theory: (I) when different agonists acting on the same receptor are tested with the same competitive antagonist the affinity constants of the latter should be the same, (2) identical receptors in different preparations should produce the same affinity constants with the same competitive antagonists.

1965). Br. J. Pharmac. , 24, 194. Receptor classification and {3-adrenergic receptors 36 PARRAIT, J. R. & WADSWORTH, R. M. (1970). Br. J. , 39,296. SCHILD, H. 0. (1969). Pharmac. Res. , 1, 1. STEPHENSON, R. P. (1956). Br. J. , 11, 379. VANRossuM, J. M. & ARIENS, E. J. (1962). Arch. int. , 136, 385. WAUD, D. R. (1969). J. Pharmac. exp. , 167, 140. , CERNOHORSKY, M. & HYNIE, S. (1967). Acad. , 139, 860. Ann. Y. DISCUSSION Brittain (Ware) The ratio of activities of optical isomers of catecholamines has been used to classify {3-receptors.

H. 0. Schild Summary Three methods of receptor classification are described based on desensitization, activity ratios of agonists and affinity constants of antagonists. The two latter methods have been used to classify ,8-adrenergic receptors and they agree in showing that these receptors form a heterogeneous group. REFERENCES AHLQUIST, R. P. (1948). Am. J. , 153, 586. ARIENS, E. J. (1964). Mol. Pharmac. New York: Academic Press. ARUNLAKSHANA, 0. & ScmLD, H. 0. (1959). Br. J. Pharmac. , 14, 48.

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