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

Acylated and aroylated hydrazinoclozapines are highly potent dopamine D1 antagonists that show remarkable selectivity over other dopamine receptors. The most potent compound in this series is the 2,6-dimethoxybenzhydrazide 33 with a D1Ki of 1.6 nM and 212-fold selectivity over D2 receptor.

A series of potent and selective dopamine D1/D5 antagonists have been discovered based on the clozapine unit.Figure optionsDownload as PowerPoint slide