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Derivatives of (R)-2-amino-5-methoxytetralin: Antagonists and inverse agonists at the dopamine D2a receptor
Institution:1. Department of Materials and Environmental Chemistry, Stockholm University, SE 106 91, Stockholm, Sweden;2. Institute of Biology, Karelian Research Center, Russian Academy of Sciences, Pushkinskaya 11, Petrozavodsk, 185910, Russian Federation
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]GTPγS binding assay.
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