ENANTIOMERS OF 11-HYDROXY-10-METHYLAPORPHINE HAVING OPPOSING PHARMACOLOGICAL EFFECTS AT 5-HT1A RECEPTORS

被引：29

作者：

CANNON, JG ^{[1
]}

MOE, ST ^{[1
]}

LONG, JP ^{[1
]}

机构：

[1] UNIV IOWA,COLL MED,DEPT PHARMACOL,IOWA CITY,IA 52246

来源：

CHIRALITY | 1991年 / 3卷 / 01期

关键词：

APORPHINE ENANTIOMERS; SEROTONIN 5-HT1A RECEPTORS;

D O I：

10.1002/chir.530030105

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The two enantiomers of the title compound have been prepared by different synthetic routes. Both bind strongly to 5-HT(1A) receptors from rat forebrain membrane tissue. However, in a guinea pig ileum preparation, the (R)-enantiomer exhibits properties consistent with its being an agonist, whereas the (S)-enantiomer shows no agonist effect, but it blocks the actions of the (R)-enantiomer and of 8-hydroxy-2-di-n-propylaminotetralin (8-OH-DPAT), a 5-HT(1A) agonist. These data are presented as a rare example of enantiomers which demonstrate opposite pharmacological effects at the same receptor.

引用

页码：19 / 23

页数：5

共 11 条

[1] (R)-(-)-10-METHYL-11-HYDROXYAPORPHINE - A HIGHLY SELECTIVE SEROTONERGIC AGONIST [J].