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Bioorg Med Chem Lett. 1999 Aug 2;9(15):2167-72.

Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.

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  • 1Organic Pharmaceutical Chemistry, Uppsala Biomedical Centre, Uppsala University, Sweden.

Abstract

A series of N-arylmethyl substituted (R)-5-methoxy-2-(propylamino)tetralins has been prepared and evaluated for affinity and efficacy at dopamine (DA) D2A receptors. The novel compounds appeared to be antagonists or inverse agonists. (R)-2-[(Benzyl)propylamino]-5-methoxytetralin (7) was characterized as a potent inverse agonists at DA D2A receptors in a [35S]GTPgammaS binding assay.

PMID:
10465538
[PubMed - indexed for MEDLINE]
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