Abstract
Apogalanthamine analogs were synthesized, and their α-adrenolytic and anti-5-HT activities and those of related compounds on rat aortic strips were compared with those of well known antagonists. It was found that N-alkylated 5, 6, 7, 8-tetrahydrodibenz [c, e]-azocines (I-III) and N-alkylated 10, 11-methylenedioxy-5, 6, 7, 8-tetrahydrodibenz [c, e]-azocines (V-VII) had reversible α-adrenolytic activities ; their activities were as great as those of phentolamine and benzylimidazoline. Of the compounds tested, DA-VIII-Me (II) had the strongest α-adrenolytic activity (pA2=8.76±0.07) / its activity was more than that of phentolamine.
