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5-羟色胺摄取抑制剂和单胺氧化酶抑制剂对大鼠L-5-羟色胺酸诱导兴奋的影响。

The effects of 5-HT uptake- and MAO-inhibitors on L-5-HTP-induced excitation in rats.

作者信息

Ortmann R, Waldmeier P C, Radeke E, Felner A, Delini-Stula A

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1980 Mar;311(2):185-92. doi: 10.1007/BF00510258.

Abstract

The behavioural syndrome caused by L-5-HTP in rats was used for the study of effects of selective 5-HT uptake inhibitors and inhibitors of MAO on central 5-HT receptors. A good correlation was found between the relative potencies of drugs in inhibiting the 5-HT uptake in the rat brain and in intensifying L-5-HTP-induced behavioural stimulation. The potentiation of the L-5-HTP syndrome by the MAO inhibitors correlated with the inhibition of the A- but not of the B-form of the brain monoamine oxidase. In rats treated with the maximally inhibiting dose of a 5-HT uptake inhibitor, MAO inhibitors were still able to increase the intensity of the L-5-HTP syndrome, while the combination of maximal doses of two 5-HT uptake inhibitors did not produce a more intense syndrome than that produced by one 5-HT uptake inhibitor alone. The L-5-HTP-induced behavioural syndrome in rats seems to afford an experimental model allowing the quantification and characterization of the interaction of drugs with serotonin metabolism in the brain.

摘要

利用L - 5 -羟色氨酸在大鼠中引起的行为综合征来研究选择性5 -羟色胺摄取抑制剂和单胺氧化酶抑制剂对中枢5 -羟色胺受体的作用。发现药物在抑制大鼠脑中5 -羟色胺摄取以及增强L - 5 -羟色氨酸诱导的行为刺激方面的相对效力之间存在良好的相关性。单胺氧化酶抑制剂对L - 5 -羟色氨酸综合征的增强作用与对脑单胺氧化酶A 型而非B型的抑制作用相关。在用最大抑制剂量的5 -羟色胺摄取抑制剂处理的大鼠中,单胺氧化酶抑制剂仍能增加L - 5 -羟色氨酸综合征的强度,而两种5 -羟色胺摄取抑制剂最大剂量的联合使用并未产生比单独一种5 -羟色胺摄取抑制剂更强烈的综合征。大鼠中L - 5 -羟色氨酸诱导的行为综合征似乎提供了一个实验模型,可用于定量和表征药物与脑中血清素代谢的相互作用。

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