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PubMed · 3019726

Differences between central and peripheral rat alpha-adrenoceptors revealed using binuclear ligands.

A Adams·B Jarrott·W A Denny·L P Wakelin
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Abstract

We have used two homologous series of binuclear ligands, diacridines and diquinolines, and the radioligand receptor assay to compare the topology of alpha 1- and alpha 2-adrenoceptors in rat cerebral cortex and kidney membranes. While the chain length-dependence of affinity of the diacridines, as well as that of the diquinolines, for the alpha 1-adrenoceptors of these central and peripheral tissues are similar, we find marked differences in affinity profiles for interaction with central and peripheral alpha 2-adrenoceptors. In the context of our previously proposed model for the binding of diacridines and diquinolines to alpha-adrenoceptors the results suggest that the surface features of central and peripheral alpha 2-adrenoceptors differ in the area surrounding the noradrenaline binding site. This difference may prove to be of therapeutic relevance.

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AcridinesAnimalsBinding, CompetitiveCerebral CortexFemaleIn Vitro TechniquesKidneyPrazosinQuinolinesRadioligand AssayRatsRats, Inbred StrainsReceptors, Adrenergic, alphaYohimbineComparative StudyJournal ArticleResearch Support, Non-U.S. Gov't

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A Adams, B Jarrott, W A Denny, L P Wakelin. 1986-08-07. Differences between central and peripheral rat alpha-adrenoceptors revealed using binuclear ligands.. https://doi.org/10.1016/0014-2999(86)90202-5

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