Synthesis and 5HT modulating activity of stereoisomers of 3-phenoxymethyl-4-phenylpiperidines

被引：25

作者：

Engelstoft, M

Hansen, JB

机构：

[1] Novo Nordisk A/S, Medicinal Chemistry, Novo Nordisk Park

来源：

ACTA CHEMICA SCANDINAVICA | 1996年 / 50卷 / 02期

关键词：

D O I：

10.3891/acta.chem.scand.50-0164

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of pairs of enantiomers of substituted 3-phenoxymethyl-4-phenylpiperidines has been prepared from arecoline or alpha-methylstyrene by a combination of stereospecific reactions and optical resolutions. The ability of the compounds to modulate serotonin (5HT) neurotransmission in vitro was determined. Several derivatives, among which is the antidepressant paroxetine, are very potent inhibitors of 5HT reuptake. These compounds exhibit a pronounced steric requirement for inhibition of 5HT reuptake and binding to 5HT(2A) and 5HT(2C) receptors.

引用

收藏

页码：164 / 169

页数：6

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