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Dopamine autoreceptor agonists: resolution and pharmacological activity of 2,6-diaminotetrahydrobenzothiazole and an aminothiazole analogue of apomorphine.

Abstract：

:The enantiomers of the aminothiazole analogues of the known dopaminergic agonists apomorphine (1) and 2-aminohydroxytetralin (2) have been prepared. The absolute configurations of the enantiomers of 2,6-diaminotetrahydrobenzothiazole have been established by X-ray crystallographic analysis. Dopamine (DA) autoreceptor agonist activities of the compounds were evaluated. Testing revealed (-)-5, the S enantiomer, to be the most active compound tested (inhibition of GBL accelerated dopamine synthesis and inhibition of alpha-methyltyrosine-induced decline of DA). In addition (-)-5 does not exhibit stereotyped behavior, suggesting a pronounced selectivity for DA autoreceptors.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Schneider CS,Mierau J

doi

10.1021/jm00386a009

subject

Has Abstract

pub_date

1987-03-01 00:00:00

pages

494-8

issue

3

eissn

0022-2623

issn

1520-4804

journal_volume

30

pub_type

杂志文章

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