Hydrazides of clozapine: a new class of D1 dopamine receptor subtype selective antagonists.

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Sasikumar TK, Burnett DA, Zhang H, Smith-Torhan A, Fawzi A, Lachowicz JE

Hydrazides of clozapine: a new class of D1 dopamine receptor subtype selective antagonists.

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4543-7. Epub 2006 Jun 30.

PubMed ID

16809034 [ View in PubMed

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Abstract

Acylated and aroylated hydrazinoclozapines are highly potent dopamine D(1) antagonists that show remarkable selectivity over other dopamine receptors. The most potent compound in this series is the 2,6-dimethoxybenzhydrazide 33 with a D(1)K(i) of 1.6 nM and 212-fold selectivity over D(2) receptor.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Clozapine	Dopamine D1 receptor	Ki (nM)	132	N/A	N/A	Details
Clozapine	Dopamine D2 receptor	Ki (nM)	208	N/A	N/A	Details