Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: a novel series of mixed dopamine D2/D4 receptor antagonist.

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Zhao H, Zhang X, Hodgetts K, Thurkauf A, Hammer J, Chandrasekhar J, Kieltyka A, Brodbeck R, Rachwal S, Primus R, Manly C

Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: a novel series of mixed dopamine D2/D4 receptor antagonist.

Bioorg Med Chem Lett. 2003 Feb 24;13(4):701-4.

PubMed ID

12639562 [ View in PubMed

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Abstract

5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives were designed, synthesized, and identified as a new series of mixed dopamine D(2)/D(4) receptor antagonists. This series featured a rigid tricyclic ring system as an important pharmacophore core structure for high binding affinity. Molecular modeling studies are also described.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Clozapine	Dopamine D2 receptor	Ki (nM)	113	N/A	N/A	Details
Clozapine	Dopamine D4 receptor	Ki (nM)	17	N/A	N/A	Details