SYNTHESIS AND BETA-ADRENERGIC ACTIVITY OF ATYPICAL BETA-ADRENERGIC PHENYLETHANOLAMINOTETRALIN STEREOISOMERS

被引：34

作者：

CECCHI, R

CROCI, T

BOIGEGRAIN, R

BOVERI, S

BARONI, M

BOCCARDI, G

GUIMBARD, JP

GUZZI, U

机构：

[1] SANOFI MIDY SPA,RES CTR,I-20137 MILAN,ITALY

[2] SANOFI RECH,F-34184 MONTPELLIER 04,FRANCE

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1994年 / 29卷 / 04期

关键词：

PHENYLETHANOLAMINOTETRALINS; SR; 58611A; BETA-ATYPICAL ADRENERGIC ACTIVITY; CHIRAL SEPARATION;

D O I：

10.1016/0223-5234(94)90095-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of substituted phenylethanolaminotetralins were synthesized as pure stereoisomers and their ability to stimulate atypical beta-adrenoceptors selectively was evaluated. The compounds in vitro relative potencies were assessed using the atypical beta response of inhibition of rat proximal colon motility and the typical beta 1 (increase in guinea-pig right atrial frequency) and beta 2 (guinea-pig tracheal relaxation and rat uterus motility inhibition) responses. Compound 42 (SR 58611A) was found to be the most potent and selective.

引用

页码：259 / 267

页数：9

共 25 条

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