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Preparation and pharmacological evaluation of enantiomers of certain nonoxygenated aporphines: (+)- and (-)-aporphine and (+)- and (-)-10-methylaporphine.

Abstract：

: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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Cannon JG,Raghupathi R,Moe ST,Johnson AK,Long JP

doi

10.1021/jm00062a002

subject

Has Abstract

pub_date

1993-05-14 00:00:00

pages

1316-8

issue

10

eissn

0022-2623

issn

1520-4804

journal_volume

36

pub_type

杂志文章

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