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.
D000317:Adrenergic alpha-Antagonists; D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects; D004837:Epinephrine / Q000494:pharmacology; D005702:Galantamine / Q000031:analogs & derivatives* / Q000494:pharmacology; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects*; D051381:Rats; D012701:Serotonin / Q000494:pharmacology; D012702:Serotonin Antagonists
D000317:Adrenergic alpha-Antagonists; D012702:Serotonin Antagonists; D005702:Galantamine; D012701:Serotonin; D004837:Epinephrine