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Hydrazides of clozapine: A new class of D1dopamine receptor subtype selective antagonists

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
16
Issue
17
Identifiers
DOI: 10.1016/j.bmcl.2006.06.022
Keywords
  • Clozapine
  • Hydrazinoclozapine
  • Dopamine D1

Abstract

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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