具有中枢5-羟色胺模拟活性的哌嗪基吡嗪类化合物。

Piperazinylpyrazines with central serotoninmimetic activity.

作者信息

Lumma W C, Hartman R D, Saari W S, Engelhardt E L, Hirschmann R, Clineschmidt B V, Torchiana M L, Stone C A

出版信息

J Med Chem. 1978 Jun;21(6):536-42. doi: 10.1021/jm00204a007.

Abstract

A series of 2-(1-piperazinyl)pyrazines was synthesized and evaluated for central serotonin-like activity. The most interesting member of the series, 6-chloro-2(1-piperazinyl)pyrazine (3a), had pharmacological properties characteristic of potent central serotoninmimetic activity and only weak peripheral serotoninmimetic action. Structural similarities between 3a and serotonin are discussed.

摘要

合成了一系列2-(1-哌嗪基)吡嗪并对其进行中枢5-羟色胺样活性评估。该系列中最有趣的成员6-氯-2-(1-哌嗪基)吡嗪(3a)具有强效中枢5-羟色胺模拟活性的药理学特性，而外周5-羟色胺模拟作用较弱。讨论了3a与5-羟色胺之间的结构相似性。