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, 16 (17), 4543-7

Hydrazides of Clozapine: A New Class of D1 Dopamine Receptor Subtype Selective Antagonists

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Hydrazides of Clozapine: A New Class of D1 Dopamine Receptor Subtype Selective Antagonists

T K Sasikumar et al. Bioorg Med Chem Lett.

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.

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