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四氢嘧啶二酮-4,6新衍生物的中枢作用

Central action of new derivatives of tetrahydropirimidinedione-4,6.

作者信息

Wilimowski M, Witkowska M, Kedzierska L, Barczyńska J, Wojewódzki W, Felsztyńska J

出版信息

Arch Immunol Ther Exp (Warsz). 1979;27(3):397-405.

PMID:475560
Abstract

The central action and LD50 of 11 new 2,5-substituted derivates of tetrahydropirimidinedione-4,6 with an aryl group at C2 were investigated. The most favorable action was exerted by 2-furfurylamine derivatives with an alkil or benzyl group at C5. These compounds acted in doses of 0.0025--0.01 of their LD50 synergistically with chloral hydrate and strongly with hexobarbital, delayed convulsions induced with pentetrazole and potentiated the central action of DOPA in mice pargyline-inhibited MAO activity. They did not antagonize electrogenic convulsions, amphetamine potentiated motility and the action of reserpine, and had no analgetic action. Their LD50s were 670-- 1660 mg/kg.

摘要

对11种新的2,5-二取代四氢嘧啶二酮-4,6衍生物(C2位带有芳基)的中枢作用和半数致死量(LD50)进行了研究。最有利的作用是由C5位带有烷基或苄基的2-糠胺衍生物发挥的。这些化合物以其LD50的0.0025--0.01剂量与水合氯醛协同作用,与己巴比妥强烈协同作用,延迟戊四氮诱导的惊厥,并增强左旋多巴在小鼠中被帕吉林抑制的单胺氧化酶(MAO)活性时的中枢作用。它们不拮抗电源性惊厥,苯丙胺增强运动性和利血平的作用,且无镇痛作用。它们的LD50为670--1660毫克/千克。

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