RELATIVE ACTIVITY OF SOME INHIBITORS OF MONO-AMINE OXIDASE IN POTENTIATING ACTION OF TRYPTAMINE IN VITRO AND IN VIVO
RELATIVE ACTIVITY OF SOME INHIBITORS OF MONO-AMINE OXIDASE IN POTENTIATING ACTION OF TRYPTAMINE IN VITRO AND IN VIVO
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DOI：
10.1111/j.1476-5381.1961.tb01118.x
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发表时间：
1961-01-01
期刊：
影响因子：
--
通讯作者：
GRAY, WR
中科院分区：
文献类型：
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作者：
MAXWELL, DR;TAYLOR, EM;GRAY, WR
检测了几种已知的单胺氧化酶抑制剂（异丙肼、异羧肼甲酰胺、苯乙肼、非尼哌嗪和反苯环丙胺）（i）在体外抑制大鼠脑线粒体制备物的单胺氧化酶活性;（ii）增强色胺对分离的大鼠胃底带制备物的作用;和（iii）增强色胺在小鼠中的急性毒性。在三项试验中，药物的效力顺序之间存在一定的相关性，特别是在抑制瓦尔堡酶活性和小鼠色胺毒性试验中。除此之外，还有异卡波肼（isocarbonazid），它对大鼠眼底条制剂具有出乎意料的高活性，以及反苯环丙胺（transylcypromine），它对大鼠眼底制剂没有色胺增强作用，尽管它在体外抑制大鼠脑单胺氧化酶，并在体内增强色胺的作用。反苯环丙胺在体外对大鼠眼底单胺氧化酶的抑制活性低于大鼠脑组织，而异丙肼和异卡波肼对这两种组织的酶的抑制效力大致相同。
Several known inhibitors of mono-amine oxidase (iproniazid, isocarboxazid nialamide, phenelzine, pheniprazine and tranylcypromine) were tested for their ability to (i) inhibit the mono-amine oxidase activity of a rat brain mitochondrial preparation in vitro; (ii) potentiate the action of tryptamine on the isolated rat fundal strip preparation; and (iii) potentiate the acute toxicity of tryptamine in mice. There was some correlation between the order of potency of the drugs in the three tests, particularly in inhibiting the enzyme activity in the Warburg and in the tryptamine toxicity test in mice. Exceptions to this were isocarboxazid which had unexpectedly high activity on the rat fundal strip preparation, and tranylcypromine which was devoid of tryptamine-potentiation action on the rat fundus preparation although it inhibited rat brain mono-amine oxidase in vitro and potentiated the action of tryptamine in vivo. Tranylcypromine was considered less active in inhibiting the mono-amine oxidase of rat fundus than rat brain tissue in vitro, while iproniazid and isocarboxazid had about the same potency on the enzyme from the two tissues.