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芳香族氨基酸脱羧酶抑制剂NSD - 1015可增加多巴胺释放:反应特性

The aromatic amino acid decarboxylase inhibitor, NSD-1015, increases release of dopamine: response characteristics.

作者信息

Dluzen D, Reddy A, McDermott J

机构信息

Department of Anatomy, Northeastern Ohio Universities College of Medicine, Rootstown 44272-0095.

出版信息

Neuropharmacology. 1992 Dec;31(12):1223-9. doi: 10.1016/0028-3908(92)90050-y.

DOI:10.1016/0028-3908(92)90050-y
PMID:1470299
Abstract

Addition of the aromatic amino acid decarboxylase inhibitor, NSD-1015 (10 microM), to Krebs'-Ringer phosphate (KRP) superfusion medium, significantly increased the release of dopamine in vitro from superfused corpus striatum tissue fragments of male rats. A dose-dependent increase in release of dopamine was obtained in response to increasing concentrations of NSD-1015, with 1.0 microM being the minimally effective dose. In addition to the striatum, NSD-1015 also increased the release of dopamine from superfused hypothalamic tissue fragments. This capacity of NSD-1015 to increase release of dopamine was calcium-independent, appeared to be somewhat specific and could apparently increase the release of dopamine in vivo, as indicated by increases in the release of the metabolite of dopamine, DOPAC, under conditions of push-pull perfusion. Although the putative role of NSD-1015 is as an aromatic amino acid decarboxylase inhibitor, the present results demonstrate that, either as a result of this function and/or in addition to this role, NSD-1015 is a potent activator of the release of dopamine.

摘要

向磷酸克氏-林格(KRP)灌流培养基中添加芳香族氨基酸脱羧酶抑制剂NSD-1015(10微摩尔),可显著增加雄性大鼠体外灌流纹状体组织碎片中多巴胺的释放。随着NSD-1015浓度增加,多巴胺释放呈剂量依赖性增加,1.0微摩尔为最小有效剂量。除纹状体外,NSD-1015还可增加下丘脑组织碎片灌流中多巴胺的释放。NSD-1015增加多巴胺释放的能力不依赖于钙,似乎具有一定特异性,并且在推挽灌注条件下,多巴胺代谢产物DOPAC释放增加表明其显然可在体内增加多巴胺的释放。尽管NSD-1015的假定作用是作为芳香族氨基酸脱羧酶抑制剂,但目前结果表明,无论是由于该功能和/或除此作用之外,NSD-1015都是多巴胺释放的强效激活剂。

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