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

Citation
Jg. Cannon et al., PREPARATION AND PHARMACOLOGICAL EVALUATION OF ENANTIOMERS OF CERTAIN NONOXYGENATED APORPHINES - (- AND (-)-APORPHINE AND (+)- AND (-)-10-METHYLAPORPHINE()), Journal of medicinal chemistry, 36(10), 1993, pp. 1316-1318
Citations number
11
Categorie Soggetti
Chemistry Medicinal
ISSN journal
00222623
Volume
36
Issue
10
Year of publication
1993
Pages
1316 - 1318
Database
ISI
SICI code
0022-2623(1993)36:10<1316:PAPEOE>2.0.ZU;2-S
Abstract
The subject compounds were prepared as a part of a continuing structur e-activity study of the contrasting actions (agonism-antagonism) of ()- and (-)-11-hydroxy-10-methylaporphine at serotonin (5-HT1A) recepto rs. None of the targeted nonoxygenated aporphine derivatives demonstra ted significant activity in assays for any effects at serotonin 5-HT1A receptors. It is concluded that, in the aporphine series, serotonergi c agonist or antagonism requires an alkyl group ortho to a phenolic OH group in the A ring.