拟精神病药物的硫类似物。三甲氧苯乙胺和异三甲氧苯乙胺的单硫类似物。

Sulfur analogues of psychotomimetic agents. Monothio analogues of mescaline and isomescaline.

作者信息

Jacob P, Shulgin A T

出版信息

J Med Chem. 1981 Nov;24(11):1348-53. doi: 10.1021/jm00143a017.

Abstract

Two monothio analogues of mescaline and three monothio analogues of 2,3,4-trimethoxyphenethylamine (isomescaline) have been synthesized and characterized. Only the two mescaline analogues (3-and 4-thiomescaline) were found to be psychotomimetics in man, being 6 and 12 times more potent than mescaline, respectively. All five compounds can serve as substrates for bovine plasma monoamine oxidase in vitro, but no positive correlation is apparent between the extent of enzymatic degradation and human psychotomimetic potency.

摘要

已合成并表征了麦司卡林的两种单硫代类似物以及2,3,4-三甲氧基苯乙胺（异麦司卡林）的三种单硫代类似物。仅发现两种麦司卡林类似物（3-硫代麦司卡林和4-硫代麦司卡林）对人具有拟精神病活性，效力分别比麦司卡林高6倍和12倍。所有这五种化合物在体外均可作为牛血浆单胺氧化酶的底物，但酶促降解程度与人类拟精神病活性之间未显示出明显的正相关。