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关于麦角棒麦角碱的某些中枢效应。

On some central effects of elymoclavine.

作者信息

Roussinov K, Georgiev V, Petkov V, Lazarova M, Petkova B, Shopova S, Markovska V, Getova D, Draganova S

出版信息

Acta Physiol Pharmacol Bulg. 1984;10(4):28-35.

PMID:6442955
Abstract

The pharmacological investigation of the ergot alkaloid of the group of clavines elymoclavine isolated from Claviceps sp. cp. II showed the following: LD50 for mice for 24 hours was 350 (228 divided by 535) mg/kg and for rats--145 (81 divided by 258) mg/kg; elymoclavine induced a dose-dependent stereotypy in rats and mice which was antagonized by haloperidol and pimozide; it prevented the development of haloperidol catalepsy in rats and produced rotations contralateral to the striatal lesions with 6-OHDA which were antagonized by pimozide and partly by cyproheptadine. Elymoclavine increased the exploratory activity of rats in open field as this effect was antagonized by haloperidol and was essentially influenced by many substances acting on different transmitter systems (NA, DA, GABA). Elymoclavine inhibited the picroroxin and electroshock convulsive seizures but potentiated the pentylenetetrazol ones in mice as these effects were differently influenced by pimozide, haloperidol, 5-HT, atropine and phentolamine. The observed effects of elymoclavine are mainly due to its DAergic agonistic action. It seems, however, that influences on other transmitter receptors also underlie the mechanism of action of this ergot alkaloid.

摘要

对从麦角菌属cp. II中分离出的棒麦角碱类麦角生物碱elymoclavine进行的药理学研究结果如下:小鼠24小时的半数致死量为350(228至535)mg/kg,大鼠为145(81至258)mg/kg;elymoclavine在大鼠和小鼠中诱导出剂量依赖性刻板行为,这种行为可被氟哌啶醇和匹莫齐特拮抗;它可预防大鼠氟哌啶醇僵住症的发生,并在6-羟基多巴胺造成的纹状体损伤对侧产生旋转行为,该行为可被匹莫齐特部分拮抗,被赛庚啶部分拮抗。Elymoclavine增加了大鼠在旷场中的探究活动,因为这种作用可被氟哌啶醇拮抗,且基本上受到许多作用于不同递质系统(去甲肾上腺素、多巴胺、γ-氨基丁酸)的物质影响。Elymoclavine抑制了小鼠中的苦味毒和电休克惊厥发作,但增强了戊四氮引起的惊厥发作,因为这些作用受到匹莫齐特、氟哌啶醇、5-羟色胺、阿托品和酚妥拉明的不同影响。观察到的elymoclavine的作用主要归因于其多巴胺能激动作用。然而,似乎对其他递质受体的影响也是这种麦角生物碱作用机制的基础。

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