Heterogeneity of mammalian alpha 2-adrenoceptors delineated by [3H]yohimbine binding.
[3H]Yohimbine binding to membrane preparations of human colon, cerebral cortex, kidney, spleen and platelets was compared with binding to preparations of animal tissues (rabbit spleen, kidney and cerebral cortex; rat cerebral cortex; guinea-pig and cat spleen). Specific binding to all preparations was saturable and indicative of binding to a uniform population of sites. The equilibrium dissociation constants (KD) of [3H]yohimbine ranged from 1.6 to 2.6 nM for human tissue and from 5.1 to 9.4 nM for the animal tissues. Binding to all tissues was displaced by drugs with an order of potency yohimbine greater than phentolamine greater than prazosin, indicating an alpha 2-adrenoceptor classification of the labelled sites. Whilst certain drugs (phentolamine, corynanthine) possessed similar affinities for all alpha 2-adrenoceptors, others (prazosin, idazoxan, WY 26392) exhibited differential potencies for alpha 2-adrenoceptors in certain species. The pharmacological characteristics of human alpha 2-adrenoceptors were conserved within the tissues examined. These results suggest that human alpha 2-adrenoceptors differ in a number of ways from those present in tissues from the other mammalian species examined. The possible existence of a spectrum of alpha 2-adrenoceptors is discussed in the light of these findings.
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001792:Blood Platelets / Q000378:metabolism; D002415:Cats; D002540:Cerebral Cortex / Q000378:metabolism; D006168:Guinea Pigs; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D008566:Membranes / Q000378:metabolism; D010646:Phentolamine / Q000494:pharmacology; D011506:Proteins / Q000378:metabolism; D011817:Rabbits; D051381:Rats; D011942:Receptors, Adrenergic, alpha / Q000378:metabolism*; D013045:Species Specificity; D013154:Spleen / Q000378:metabolism; D015016:Yohimbine / Q000378:metabolism*
D011506:Proteins; D011942:Receptors, Adrenergic, alpha; D015016:Yohimbine; D010646:Phentolamine