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19 April 2024 |
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Article overview
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Beta-adrenergic receptor: stereospecific interaction of iodinated beta-blocking agent with high affinity site | | G D Aurbach
; S A Fedak
; C J Woodard
; J S Palmer
; D Hauser
; F Troxler
; | | Date: |
27 Dec 1974 | | Journal: | Science, 186 (4170), 1223-4 | | Abstract: | An iodine-labeled beta-adrenergic inhibitor ((125)l-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. | | Source: | PubMed, pmid4154497 | | Services: | Forum | Review | Favorites | |
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