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Zhao H, He X, Thurkauf A, Hoffman D, Kieltyka A, Brodbeck R, Primus R, Wasley JW: Indoline and piperazine containing derivatives as a novel class of mixed D (2)/D (4) receptor antagonists. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3111-5.
Part 2: asymmetric synthesis and biological evaluation.. 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. |
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