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[小檗碱型生物碱的行为药理学。(2) 四氢小檗碱 (THB) 及相关化合物的中枢抑制作用]

[Behavioral pharmacology of berberine-type alkaloids. (2) Central depressant effects of tetrahydroberberine (THB) and related compounds].

作者信息

Yamahara J

出版信息

Nihon Yakurigaku Zasshi. 1976 Oct;72(7):909-27.

PMID:1035192
Abstract

The behavioral effects of tetrahydroberberine (THB), tetrahydrocoptisine (THC), tetrahydropalmatine (THP) and tetrahydrojateorrhizine (THJ) were compared with those of chlorpromazine (CPZ) and benzodiazepines in mice and rats. Effects of THB were also determined by electroencephalography (EEG) in rabbits. THB was found to pharmacologically exert various actions similar to those of CPZ which is a major tranquilizer, however, the actions of THB were weaker than those of CPZ. Although THB alone did not induce catalepsy, it enhanced the cataleptogenic action of CPZ. At a dose over the effective levels, THB did not lower normal body temperature or induce muscle relaxation and loss of righting reflex. EEG activities in the frontal cortex areas were markedly affected by THB, e.g., fast waves in spontaneous EEG were converted to slow waves. THB and CPZ in a similar manner elicited a sustaining increase in hippocampal afterdischarge, but the action of THB was weaker than that of CPZ. The acute toxicity of THB was lower than that of CPZ and benzodiazepines and the depressant activity of THB almost equalled that of THC and THP, whereas the activity of 1-THB was 1.5 times as great as that of THB. These data indicate that THB, THC and THP may be a new type of tranquilizer.

摘要

在小鼠和大鼠中,比较了四氢小檗碱(THB)、四氢黄连碱(THC)、延胡索乙素(THP)和四氢非洲防己碱(THJ)与氯丙嗪(CPZ)和苯二氮䓬类药物的行为学效应。还通过脑电图(EEG)测定了THB对家兔的作用。发现THB在药理学上发挥与主要镇静剂CPZ类似的多种作用,然而,THB的作用比CPZ弱。虽然THB单独不诱发僵住症,但它增强了CPZ的致僵住症作用。在超过有效水平的剂量下,THB不会降低正常体温或诱导肌肉松弛和翻正反射丧失。THB显著影响额叶皮质区域的EEG活动,例如,自发EEG中的快波转变为慢波。THB和CPZ以类似方式引起海马后放电持续增加,但THB的作用比CPZ弱。THB的急性毒性低于CPZ和苯二氮䓬类药物,且THB的抑制活性几乎与THC和THP相当,而1-THB的活性是THB的1.5倍。这些数据表明,THB、THC和THP可能是一种新型镇静剂。

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