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[人血浆中5-羟色胺摄取抑制剂及特定丙咪嗪结合抑制剂]

[Inhibitors of reverse serotonin uptake and of specific imipramine binding in human blood plasma].

作者信息

Brusov O S, Lideman R R, Fomenko A M, Katasonov A B

出版信息

Biull Eksp Biol Med. 1985 Jul;100(7):26-8.

PMID:4016237
Abstract

Human blood plasma contains low-molecular substances that inhibit in a dose-dependent manner both high-affinity specific binding of imipramine and reverse serotonin uptake by platelets. Incubation of human blood plasma with alumina was made use of to extract and study these imipramine-like inhibitors. The extract obtained from human blood plasma inhibited imipramine binding and reverse uptake of serotonin with median inhibitory concentrations of 0.18 +/- 0.1 and 0.36 +/- 0.15 mg/ml, respectively. After gel chromatography on Biogel P-2 the elution profile of the extract showed 2 major peaks of reverse serotonin uptake and imipramine binding inhibition and 3 additional peaks of reverse serotonin uptake inhibition, which did not have any considerable effect on imipramine specific binding. It is assumed that endogenous inhibitors of imipramine binding and reverse serotonin uptake are involved in the development of affective disorders.

摘要

人血浆中含有低分子物质,这些物质以剂量依赖的方式抑制丙咪嗪的高亲和力特异性结合以及血小板对5-羟色胺的反向摄取。利用氧化铝与人血浆孵育来提取和研究这些类丙咪嗪抑制剂。从人血浆中获得的提取物抑制丙咪嗪结合和5-羟色胺的反向摄取,其半数抑制浓度分别为0.18±0.1和0.36±0.15mg/ml。在Biogel P-2上进行凝胶色谱分析后,提取物的洗脱图谱显示出2个5-羟色胺反向摄取和丙咪嗪结合抑制的主要峰,以及3个额外的5-羟色胺反向摄取抑制峰,这些峰对丙咪嗪特异性结合没有任何显著影响。据推测,丙咪嗪结合和5-羟色胺反向摄取的内源性抑制剂与情感障碍的发生有关。

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