COMPARISON OF APPARENT ANTIDEPRESSANT ACTIVITY OF (-) AND (+) TRANYLCYPROMINE IN AN ANIMAL-MODEL
COMPARISON OF APPARENT ANTIDEPRESSANT ACTIVITY OF (-) AND (+) TRANYLCYPROMINE IN AN ANIMAL-MODEL
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DOI：
10.1016/0006-2952(76)90150-7
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发表时间：
1976-01-01
影响因子：
5.8
通讯作者：
NEFF, NH
中科院分区：
文献类型：
--
作者：
FUENTES, JA;OLESHANSKY, MA;NEFF, NH
反苯环丙胺（TCP）的异构体在腹膜内给药后进入大脑，并在15分钟内达到峰值浓度。（-）TCP进入大脑的速度更快，达到的浓度略高于（+）TCP。在2.5 mg/kg（-）或（+）TCP剂量后，脑中的药物比报告的阻断突触体对胺的再摄取所需的药物多。这两种异构体在体内和体外阻断单胺氧化酶。（+）TCP的活性比（-）TCP高10至60倍，具体取决于所评估的胺底物，并且两种异构体都是比A型单胺氧化酶活性更好的B型单胺氧化酶活性抑制剂。（+）异构体在防止利血平诱导的镇静作用方面比（-）异构体更有效。预防利血平综合征的能力显然与药物阻断单胺氧化酶活性的能力有关，而不是阻断胺的再摄取。
The isomers of tranylcypromine (TCP) entered the brain after i.p. administration and reached peak concentrations within 15 min. (-) TCP entered the brain more rapidly and reached somewhat higher concentrations than (+) TCP. After a dose of 2.5 mg/kg of (-) or (+) TCP, there was more drug in brain than was reported necessary to block the re-uptake of amines by synaptosomes. Both isomers blocked monoamine oxidase in vivo and in vitro. (+) TCP was between 10 and 60 times more active than (-) TCP, depending on the amine substrate evaluated, and both isomers were better inhibitors of type-B monamine oxidase activity than type-A activity. The (+) isomer was more active in preventing reserpine-induced sedation in the rat than the (-) isomer. The ability to prevent the reserpine syndrome was apparently related to the ability of the drugs to block monoamine oxidase activity rather than to blockade of amine re-uptake.