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Science 27 December 1974:
Vol. 186. no. 4170, pp. 1223 - 1224
DOI: 10.1126/science.186.4170.1223
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Articles

beta-Adrenergic Receptor: Stereospecific Interaction of lodinated beta-Blocking Agent with High Affinity Site

G. D. Aurbach 1, S. A. Fedak 1, C. J. Woodard 1, J. S. Palmer 1, D. Hauser 1, and F. Troxler 2

1 Metabolic Diseases Branch, National Institute of Arthritis, Metabolism, and Digestive Diseases, Bethesda, Maryland 20014
2 Sandoz Limited, Basel, Switzerland

An iodine-labeled beta-adrenergic inhibitor (125l-hydroxybenzylpindolol) binds specifically to a site on turkey erythrocyte membranes. A series of beta-adrenergic agonists and inhibitors compete for this binding site, with apparent affinities paralleling biological effectiveness as activators or inhibitors of catecholaminestimulated adenylate cyclase. The activity of d-(+) agonists or inhibitors was 1 percent (or less) than that of the corresponding l-(-) isomers in competing for binding of the iodinated blocker as well as in affecting catecholamine-stimulated adenylate cyclase. 1-(-)-Norepinephrine was about one-tenth as active as l-(-)-isoproterenol in competing for the beta-blocking agent site. The stereospecificity of the interaction with the iodinated beta-blocking agent and the correspondence between affinity for site and biological potency of analogs suggested that this interaction is involved in function of the beta-adrenergic receptor.


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