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[5-羟色胺摄取抑制剂吲达品在猫脑中结合位点的生化特性及定量放射自显影研究]

[Biochemical characterization and study by quantitative autoradiography of the binding sites of indalpine, a 5-HT uptake inhibitor, in cat brain].

作者信息

Benavides J, Malgouris C, Daniel M, Savaki H, Uzan A, Gueremy C, Le Fur G

出版信息

Encephale. 1985 Nov-Dec;11(6):247-54.

PMID:3830692
Abstract

The [3H]indalpine binding sites have been characterized in slide-mounted cat brain sections. This inhibitor of 5-HT reuptake binds with a very high affinity to sites which have the pharmacological properties of the serotonin carrier. These sites can, however, be differentiated from the [3H]imipramine binding sites by their Na+ dependency and competitive inhibition by serotonin. Quantitative autoradiographic studies demonstrate that indalpine binding sites are localized in structures rich in serotonergic neurons. The widespread distribution of indalpine binding sites in limbic and associative areas is consisted with its well characterized antidepressant activity in human.

摘要

已在载玻片上的猫脑切片中对[3H]吲哚哌啶结合位点进行了表征。这种5-羟色胺再摄取抑制剂以非常高的亲和力与具有5-羟色胺载体药理学特性的位点结合。然而,这些位点可通过其对Na+的依赖性和5-羟色胺的竞争性抑制作用与[3H]丙咪嗪结合位点区分开来。定量放射自显影研究表明,吲哚哌啶结合位点定位于富含5-羟色胺能神经元的结构中。吲哚哌啶结合位点在边缘和联合区域的广泛分布与其在人体中已明确的抗抑郁活性相符。

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