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ID: ALA1130629
Journal: Bioorg Med Chem Lett
Title: Fused aminotetralins: novel antagonists with high selectivity for the dopamine D3 receptor.
Authors: Avenell KY, Boyfield I, Coldwell MC, Hadley MS, Healy MA, Jeffrey PM, Johnson CN, Nash DJ, Riley GJ, Scott EE, Smith SA, Stacey R, Stemp G, Thewlis KM.
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.
CiteXplore: 9873637