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可乐定的抗紧张症作用:其与多巴胺能、抗胆碱能及γ-氨基丁酸能药物的相互作用。

Anticatatonic effect of clonidine: its interaction with dopaminergic, anticholinergic and GABA-ergic drugs.

作者信息

Shukla V K, Garg S K, Kulkarni S K

出版信息

Arch Int Pharmacodyn Ther. 1986 Jul;282(1):33-43.

PMID:3021074
Abstract

Anticatatonic effects of systemic (50 micrograms/kg, i.p.) and intracerebroventricularly (5 micrograms/10 microliters/rat) administered clonidine was studied in rats against perphenazine-induced catatonia. Clonidine was found to possess anticatatonic actions in rats as it significantly blocked perphenazine-induced catatonia. When clonidine was administered simultaneously with dopaminergic (dopamine, bromocriptine), anticholinergic (scopolamine, diphenhydramine) and GABA-ergic (GABA, muscimol) agents there was a potentiation of the anticatatonic effect. However, clonidine-anticholinergic combination showed a better protective response as compared to clonidine-dopaminergic combination. The protective effect of clonidine and its modification by anticholinergic agents has been explained on the basis of direct central adrenergic as well as central anticholinergic actions of clonidine. Although higher dose of GABA-ergic agents was not studied due to toxicity, the combined effect of clonidine and GABA-ergic agents has been explained on neurotransmitter interactions.

摘要

研究了腹腔注射(50微克/千克)和脑室内注射(5微克/10微升/大鼠)可乐定对大鼠奋乃静诱导的紧张症的抗紧张症作用。发现可乐定在大鼠中具有抗紧张症作用,因为它能显著阻断奋乃静诱导的紧张症。当可乐定与多巴胺能药物(多巴胺、溴隐亭)、抗胆碱能药物(东莨菪碱、苯海拉明)和GABA能药物(GABA、蝇蕈醇)同时给药时,抗紧张症作用增强。然而,与可乐定-多巴胺能组合相比,可乐定-抗胆碱能组合表现出更好的保护反应。可乐定的保护作用及其被抗胆碱能药物修饰的作用已基于可乐定直接的中枢肾上腺素能以及中枢抗胆碱能作用得到解释。尽管由于毒性未研究更高剂量的GABA能药物,但可乐定和GABA能药物的联合作用已基于神经递质相互作用得到解释。

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