Evidence for pharmacological similarity between α2,-adrenoceptors in the vas deferens and central nervous system of the rat

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Abstract
Seven .alpha.2-adrenoceptor antagonists with diverse chemical structures were examined for their effects at .alpha.2-adrenoceptors in the vas deferens and CNS of the rat. Antagonist potency assessed against the presynaptic .alpha.2-adrenoceptor agonist action of clonidine in the isolated vas deferens (RX 781094 [2-(2(1,4-benzodiozanyl))WY 26703-2-imidazoline hydrochloride] > Wy 26703 [N-methyl-N-(1,3,4,6,7,11 ba-hexahydro-2H-benzo(.alpha.)-quinolizin-2.beta.-yl) isobutanesulfonamide] > yohimbine > rauwolscine > piperoxan > mianserin > RS 21361 [2-(1-ethyl-2-imidazolyl methyl)-1,4-benzodioxan]) was highly correlated with the ability of these drugs to displace saturable [3H]-RX 781094 binding from cerebral cortex membranes. Antagonist potency in the vas deferens was highly correlated with antagonist activity in reversing the centrally-mediated mydriasis induced by the selective .alpha.2-adrenoceptor agonist, guanoxabenz, in pentobarbitone-anesthetized rats. The presynaptic .alpha.2-adrenoceptors in the vas deferens are evidently pharmacologically similar to characterize these .alpha.2-adrenoceptors in the CNS of the rat.

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