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J Med Chem. 1993 Oct 15;36(21):3188-96.

Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.

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Department of Pharmacology, University of Göteborg, Sweden.


The (+)-and (-)-enantiomer of compounds 4 and 5 were synthesized and tested for central dopamine (DA) receptor stimulating activity, using biochemical and behavioral tests in rats. Based on the available data the (-)-enantiomers of 4 and 5 are characterized as centrally acting DA autoreceptor antagonists with oral activity. They display a similar pharmacological profile as the prototype DA autoreceptor antagonists (+)-1 and (+)-2 and show a certain preference for the D3 DA receptor antagonist binding site.

[Indexed for MEDLINE]

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