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二乙吡啶二酮的两种N-氨甲基衍生物的中枢抑制作用

Central depressive action of two N-aminomethyl derivatives of diethylpyridinedione.

作者信息

Beltcheva I, Stoytchev T

出版信息

Acta Physiol Pharmacol Bulg. 1983;9(1):35-43.

PMID:6684873
Abstract

The central depressive action of N-aminomethylmorpholine-3,3-diethyl-2,4-pyridinedione (DKMM) and N-aminomethylpiperazine-3,3-diethyl-2,4-pyridinedione (DKMP), compounds having a marked anticonvulsive effect, has been studied applying a set of methods characterizing this action. DKMM and DKMP are found to prolong hexobarbital, chlorhydrate and alcohol sleeping time. Investigated by the modified jumping test, the two substances inhibit the central nervous system to the same degree. They show at the same time properties of hypnosedatives and neuroleptics as well. DKMM and DKMP manifest motor-incoordination activity in doses nearly 3.5 times higher than the doses inhibiting corazol convulsions. The compounds have a marked antiaggressive effect in the case of isolation syndrome, particularly pronounced for DKMP in a dose of 1/12 of LD50. The results obtained show that DKMM and DKMP are central depressants with marked sedative-tranquillizing action.

摘要

对具有显著抗惊厥作用的化合物N-氨甲基吗啉-3,3-二乙基-2,4-吡啶二酮(DKMM)和N-氨甲基哌嗪-3,3-二乙基-2,4-吡啶二酮(DKMP)的中枢抑制作用,已采用一系列表征该作用的方法进行了研究。发现DKMM和DKMP可延长己巴比妥、盐酸盐和酒精的睡眠时间。通过改良跳跃试验研究,这两种物质对中枢神经系统的抑制程度相同。它们同时还表现出催眠药和抗精神病药的特性。DKMM和DKMP在剂量比抑制戊四氮惊厥的剂量高近3.5倍时表现出运动不协调活性。在隔离综合征的情况下,这些化合物具有显著的抗攻击作用,对于剂量为LD50的1/12的DKMP尤为明显。所得结果表明,DKMM和DKMP是具有显著镇静安定作用的中枢抑制剂。

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