PREPARATION AND PHARMACOLOGICAL EVALUATION OF ENANTIOMERS OF CERTAIN NONOXYGENATED APORPHINES - (+)- AND (-)-APORPHINE AND (+)- AND (-)-10-METHYLAPORPHINE

被引：14

作者：

CANNON, JG ^{[1
]}

RAGHUPATHI, R ^{[1
]}

MOE, ST ^{[1
]}

JOHNSON, AK ^{[1
]}

LONG, JP ^{[1
]}

机构：

[1] UNIV IOWA,COLL MED,DEPT PHARMACOL,IOWA CITY,IA 52242

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 36卷 / 10期

关键词：

D O I：

10.1021/jm00062a002

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The subject compounds were prepared as a part of a continuing structure-activity study of the contrasting actions (agonism-antagonism) of (+)- and (-)-11-hydroxy-10-methylaporphine at serotonin (5-HT1A) receptors. None of the targeted nonoxygenated aporphine derivatives demonstrated significant activity in assays for any effects at serotonin 5-HT1A receptors. It is concluded that, in the aporphine series, serotonergic agonist or antagonism requires an alkyl group ortho to a phenolic OH group in the A ring.

引用

页码：1316 / 1318

页数：3

共 11 条

[1] ENANTIOMERS OF 11-HYDROXY-10-METHYLAPORPHINE HAVING OPPOSING PHARMACOLOGICAL EFFECTS AT 5-HT1A RECEPTORS [J].