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

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Sonesson C, Waters N, Svensson K, Carlsson A, Smith MW, Piercey MF, Meier E, Wikstrom H

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

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

PubMed ID

8230107 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Haloperidol	Dopamine D3 receptor	Ki (nM)	6.4	N/A	N/A	Details