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Clozapine-N-oxide is a major metabolite of clozapine (Item No. 12059) and an activator of designer receptors exclusively activated by designer drugs (DREADDs) derived from human muscarinic acetylcholine receptors (EC50s = 16.7, 323, 17.4, 18.3, and 18.7 nM for PASMCs expressing hM1-5D receptors, respectively).1,2 It prevents action potential firing in cultured hippocampal neurons transiently expressing hM4D receptors.2 Clozapine-N-oxide increases glutamate in the nucleus accumbens core and inhibits cue-induced reinstatement of cocaine-seeking behavior in rats transfected with hM3Dq DREADD receptors.3
WARNING This product is not for human or veterinary use.
1. The involvement of CYP1A2 and CYP3A4 in the metabolism of clozapine. Br. J. Clin. Pharmacol. 44(5), 439-446 (1997).
2. Evolving the lock to fit the key to create a family of G protein-
3. Gq-