SELECTIVE ALPHA-ADRENOCEPTOR BLOCKING ACTIONS OF A NEW DERIVATIVE OF 2-HALOGENOETHYLAMINE : 6-(2-BROMOETHYL)-10, 11-METHYLENEDIOXY-5, 6, 7, 8-TETRAHYDRODIBENZ[c, e]AZOCINE

[摘要] References(20)Cited-By(1)A new compound, 6-(2-bromoethyl)-10, 11-methylenedioxy-5, 6, 7, 8-tetrahydrodibenz [c, e] azocine (DA-VIII-MBr) was found to have a more selective α-adrenergic blocking action than dibenamine or phenoxybenzamine. From dose-response curves for adrenaline and 5-hydroxytryptamine (5-HT) obtained in strips of rat aorta before and after incubation with each of the three blocking agents, the fractions of receptors remaining active for adrenaline and 5-HT, respectively, were estimated. After blockade with DA-VIII-MBr the receptors for adrenaline were blocked considerably, but those for 5-HT were little affected. Dibenamine blocked the receptors to adrenaline and 5-HT almost equally. The effective dose of phenoxybenzamine for adrenaline receptors was less than one hundredth that of dibenamine or DA-VIII-MBr, but specificity for these receptors was intermediate between those of dibenamine and DA-VIII-MBr. The structure of DA-VIII-MBr is an analog of apogalanthamine and its nitrogen atom bears the 2-halogenoethylamine group in part of an eight membered ring.

[学科分类] 药理学