alpha2B-adrenoceptor agonist ST-91 antagonizes beta2-adrenoceptor-mediated relaxation in rat mesenteric artery rings.

We sought an isolated vascular preparation and experimental setting where the function of alpha2B-adrenoceptors could be demonstrated by non-recombinant technique. ST-91 (2-[2,6-diethylphenylamino]-2-imidazoline), an alpha 2B-adrenoceptor agonist with a mixed alpha adrenergic receptor type/subtype selection profile antagonized the relaxant effect of isoproterenol in endothelium-denuded rat mesenteric artery rings precontracted with phenylephrine. At 10(-7) M of ST-91, the antagonism was characterized by a rightward shift of isoproterenol dose-response curve (A50=6.81+/-1.40 e-7 (n=4) vs the control 1.29+/-0.25 e-7 M (n=4)) with no E(max) depression. At 10(-6) M the Emax depression was prevalent (36.1+/-7.0% (n=4) vs the control 79.9+/-5.1% (n=4)); both actions could be antagonized by the alpha2-adrenoceptor antagonist yohimbine. The not subtype-selective alpha(2)-adrenoceptor agonist xylazine (10(-7) M) did not affect the relaxant action of isoproterenol. Present findings are discussed in the light of previously reported hemodynamic effects attributed to alpha2B-adrenoceptors in receptor subtype-knockout animals.

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