Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377711 | Bioorganic & Medicinal Chemistry Letters | 2006 | 5 Pages |
Abstract
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.
Graphical abstractA series of potent and selective dopamine D1/D5 antagonists have been discovered based on the clozapine unit.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
T.K. Sasikumar, D.A. Burnett, H. Zhang, A. Smith-Torhan, A. Fawzi, J.E. Lachowicz,