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Bioorg Med Chem Lett. 2002 Nov 4;12(21):3111-5.

Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation.

Author information

1
Neurogen Corporation, 35Northeast Industrial Road, Branford, CT 06405, USA. hzhao@nrgn.com

Abstract

A series of chiral benzylpiperazinyl-1-(2,3-dihydro-indol-1-yl)ethanone derivatives were prepared and examined for their affinity at dopamine D(2) and D(4) receptors. Three compounds having D(2)/D(4) affinity ratios approximating that found for the atypical neuroleptic clozapine were further evaluated in behavioral tests of antipsychotic efficacy and motor side effects.

PMID:
12372513
DOI:
10.1016/s0960-894x(02)00656-x
[Indexed for MEDLINE]

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