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Evidence in favor of a selective alpha 1 adrenoceptor blocking action of wb 4101 n 2 2 6 di methoxyphenoxyethyl 1 4 benzodioxan 2 methylamine in vivo


, : Evidence in favor of a selective alpha 1 adrenoceptor blocking action of wb 4101 n 2 2 6 di methoxyphenoxyethyl 1 4 benzodioxan 2 methylamine in vivo. Naunyn-Schmiedeberg's Archives of Pharmacology 319(3): 222-225

The .alpha.-adrenoceptor blocking potency of WB 4101 at .alpha.1- and .alpha.2-adrenoceptors was investigated in pithed rats. WB 4101 was .apprx. 97 times more potent at antagonizing the vasopressor responses produced by the selective .alpha.1-adrenoceptor agonist phenylephrine, than those produced by the selective .alpha.2-adrenoceptor agonist M-7 [2-N,N-dimethylamino-5,6-dihydroxy-1,2,3,4-tetrahydronaphthalene]. A dose of WB 4101 (3 mg/kg) that caused extensive blockade of vascular .alpha.1-adrenoceptors, but little or no blockade of vascular .alpha.2-adrenoceptors,exerted no significant blockade of the presynaptic .alpha.2-adrenoceptors in the rat heart. WB 4101 is apparently is highly selective antagonist at .alpha.1-adrenoceptors in vivo.

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