GEY K F, PLETSCHER A
Br J Pharmacol Chemother. 1962 Aug;19(1):161-7. doi: 10.1111/j.1476-5381.1962.tb01437.x.
In rats, three alpha-alkylated tryptamine derivatives (alpha-methyl, alpha-ethyl, and alphaalpha-dimethyltryptamine) caused alterations of 5-hydroxytryptamine metabolism typical of monoamine-oxidase inhibitors with short duration of action, viz., an increase of endogenous 5-hydroxytryptamine in brain, enhancement of the increase of 5-hydroxytryptamine in brain and heart after 5-hydroxytryptophan administration, an inhibition of the decrease in 5-hydroxytryptamine in brain induced by a benzoquinolizine derivative and of the increase induced by iproniazid. The increase after iproniazid was antagonized to the same extent by all the tryptamine derivatives and by harmaline, whereas dexamphetamine showed less effect. In the other experiments with brain, the tryptamine derivatives were less potent than harmaline, but somewhat more active than dexamphetamine. alpha-Methyltryptamine and alpha-ethyltryptamine were relatively more effective in the heart than in the brain. Among the tryptamine derivatives alphaalpha-dimethyltryptamine had the weakest activity in brain and in heart.
在大鼠中，三种α-烷基化色胺衍生物（α-甲基、α-乙基和α,α-二甲基色胺）引起了单胺氧化酶抑制剂典型的5-羟色胺代谢变化，且作用持续时间较短，即：脑内内源性5-羟色胺增加，给予5-羟色氨酸后脑和心脏中5-羟色胺的增加增强，对苯并喹嗪衍生物诱导的脑内5-羟色胺减少以及异烟肼诱导的增加均有抑制作用。异烟肼后的增加被所有色胺衍生物和哈马灵以相同程度拮抗，而右旋苯丙胺的作用较小。在其他脑实验中，色胺衍生物的效力比哈马灵弱，但比右旋苯丙胺稍强。α-甲基色胺和α-乙基色胺在心脏中的作用相对比在脑中更有效。在色胺衍生物中，α,α-二甲基色胺在脑和心脏中的活性最弱。
