Hydrazides of Clozapine: a New Class of D1 Dopamine Receptor Subtype Selective Antagonists
Overview
Affiliations
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.
F-labeled radiotracers for in vivo imaging of DREADD with positron emission tomography.
Hu F, Morris P, Bonaventura J, Fan H, Mathews W, Holt D Eur J Med Chem. 2020; 213:113047.
PMID: 33280897 PMC: 7925357. DOI: 10.1016/j.ejmech.2020.113047.
Vogt I, Ahmed H, Auer J, Bajorath J Mol Divers. 2008; 12(1):25-40.
PMID: 18317941 DOI: 10.1007/s11030-008-9071-2.