Synthesis, characterization and pharmacological profile of tropicamide enantiomers

被引：25

作者：

Dei, S

Bellucci, C

Ghelardini, C

Romanelli, MN

Spampinato, S

机构：

[1] UNIV FLORENCE, DEPT PRECLIN & CLIN PHARMACOL, I-50134 FLORENCE, ITALY

[2] UNIV BOLOGNA, DEPT PHARMACOL, I-40126 BOLOGNA, ITALY

来源：

LIFE SCIENCES | 1996年 / 58卷 / 23期

关键词：

tropicamide enantiomers; M(4) selective muscarinic antagonist; M(1)-M(4) subtypes; analgesia;

D O I：

10.1016/0024-3205(96)00208-1

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

The synthesis, chemical characterization and antimuscarinic activity of the two enantiomers of tropicamide are reported. Functional (rabbit vas deferens, guinea pig heart (force) and ileum) as well as binding experiments (m(1) and m(4) human muscarinic receptors expressed in CHO-K1 cells; M(2) and M(3) receptors of rat heart and submaxillary gland membranes) were used to evaluate the antimuscarinic activity of the enantiomers. The results show that none of the enantiomers is able to significantly discriminate among the receptors studied and therefore do not support the proposal of tropicamide as an M(4) (m(4)) selective agent.

引用

页码：2147 / 2153

页数：7

共 27 条

[1] ALPHA-METHOXY-ALPHA-TRIFLUOROMETHYLPHENYLACETIC ACID, A VERSATILE REAGENT FOR DETERMINATION OF ENANTIOMERIC COMPOSITION OF ALCOHOLS AND AMINES [J].