Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships.

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Zhao H, Thurkauf A, He X, Hodgetts K, Zhang X, Rachwal S, Kover RX, Hutchison A, Peterson J, 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 1: identification and structure-activity relationships.

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3105-9.

PubMed ID

12372512 [ View in PubMed

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Abstract

Optimization of the lead compound 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2,3-dihydro-indol-1-yl)-ethanone 1 by systematic structure-activity relation (SAR) studies lead to two potent compounds 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2-methy-2,3-dihydro-indol-1-yl)-ethano ne 2n and 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2-methy-2,3-dihydro-indol-1-yl)-ethano ne 7b. Their related synthesis was also reported.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Clozapine	Dopamine D2 receptor	Ki (nM)	138	N/A	N/A	Details
Clozapine	Dopamine D4 receptor	Ki (nM)	9	N/A	N/A	Details