Alpha-adrenolytic and anti-serotonin activities of apogalanthamine analogs on the rat aortic strips.

Most of apogalanthamine analogs were more specific in alpha-adrenolytic activity than in anti-serotonin activity. In this report, 1,2,11-trimethoxy-N-methyl-5,6,7,8-tetrahydrodibenz[c,e]azocine(abbreviated as K-35) was found to be stronger in activity against serotonin (pA2 = 7.11 +/- 0.08) than against adrenaline (pA2 = 6.24 +/- 0.06). Apogalanthamine analogs have a tetrahydrodibenz[c,e]azocine structure, in which one benzene can be regarded as a part of benzylamine and other as a part of phenethylamine. From the pharmacological point of view, various azocine compounds were tested, the phenethylamine in the azocine structure is demonstrated to contribute toward the alpha-adrenolytic activity and the benzylamine having two methoxy groups contributes toward the anti-serotonin activity.