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

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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. Part 2: asymmetric synthesis and biological evaluation.

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

PubMed ID

12372513 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Clozapine	Dopamine D2 receptor	Ki (nM)	138000	N/A	N/A	Details
Clozapine	Dopamine D4 receptor	Ki (nM)	9000	N/A	N/A	Details
Haloperidol	Dopamine D2 receptor	Ki (nM)	1000	N/A	N/A	Details