(S)-8-CDI-N-PROPYLAMINO)-6,7,8,9-TETRAHYDRO-3H-BENZ[E]INDOLE-1-CARBALOEHYDE AND (R)-8-(DI-N-PROPYLAMINO)-6,7,8,9-TETRAHYDRO-3H-BENZ[E]INDOLE-1-CARBALDEHYDE - A NEW CLASS OF ORALLY-ACTIVE 5-HT1A-RECEPTOR AGONISTS

被引：22

作者：

STJERNLOF, P ^{[1
]}

GULLME, M ^{[1
]}

ELEBRING, T ^{[1
]}

ANDERSSON, B ^{[1
]}

WIKSTROM, H ^{[1
]}

LAGERQUIST, S ^{[1
]}

SVENSSON, K ^{[1
]}

EKMAN, A ^{[1
]}

CARLSSON, A ^{[1
]}

SUNDELL, S ^{[1
]}

机构：

[1] UNIV GOTEBORG,DEPT MED BIOCHEM,STRUCT CHEM UNIT,S-41390 GOTHENBURG,SWEDEN

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 36卷 / 15期

关键词：

D O I：

10.1021/jm00067a002

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The enantiomers of 6,7,8,9-tetrahydro-N,N-di-n-propyl-3H-benz[e]indol-8-amine (S-(-)-2b and R-(+)-2b) and their corresponding 1-formyl analogs (S-(-)-6 and R-(+)-6) were prepared and evaluated pharmacologically for serotonergic and dopaminergic activity. The introduction of a formyl group in the 1-position shifted the pharmacological profile of 2b from a mixed D2/5-HT1A agonists to a selective 5-HT1A agonist (6). The enantiomers of 6 were agonists with full intrinsic activity and had an affinity comparable to that of 8-hydroxy-2-(di-n-propylamino)tetrahydronaphthalene (8-OH-DPAT). In contrast to 8-OH-DPAT, the enantiomers of compound 6 were found to have good oral availability.

引用

页码：2059 / 2065

页数：7

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