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Bioorg Med Chem Lett. 1998 Oct 20;8(20):2859-64.

Fused aminotetralins: novel antagonists with high selectivity for the dopamine D3 receptor.

Author information

1
SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK.

Abstract

Starting from a series of 2-aminotetralins 1, a novel series of N-[4-(4-phenylbenzoylamino)butyl]-octahydrobenzoquinolines and hexahydrobenzoindoles with high potency and selectivity for the dopamine D3 receptor has been designed. The effect of ligand chirality on binding affinity has been established. Selected derivatives (e.g. 2o, 2p) show high functional selectivity and enhanced in vivo properties compared to 1.

PMID:
9873637
DOI:
10.1016/s0960-894x(98)00512-5
[Indexed for MEDLINE]

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