1189888-77-4

A major labelled metabolite of clozapine. A potent and selective 5-HT2C serotonin receptor antogonist.

N-Desmethylclozapine-d8 is intended for use as an internal standard for the quantification of N-desmethylclozapine by GC- or LC-MS. N-Desmethylclozapine is an active metabolite of the atypical antipsychotic clozapine .1 It was originally described as an antagonist of serotonin (5-HT) receptor subtype 5-HT2C (IC50 = 7.1 nM in rat choroid plexus) and later as an inverse agonist using human recombinant receptors.2,3 N-Desmethylclozapine is an antagonist at dopamine D4 receptors, an agonist at δ-opioid receptors, and a partial agonist at dopamine D2 and D3, M1 muscarinic acetylcholine, and 5-HT1A receptors.3,1,4 N-Desmethylclozapine (30 mg/kg) decreases exploratory locomotor activity and increases prepulse inhibiton of the acoustic startle response in mice.5

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1.Burstein, E.S., Ma, J., Wong, S., et al.Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: Identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonistJ. Pharmacol. Exp. Ther.315(3)1278-1287(2005) 2.Kuoppam?ki, M., Syv?lahti, E., and Hietala, J.Clozapine and N-desmethylclozapine are potent 5-HT1C receptor antagonistsEur. J. Pharmacol.245(2)179-182(1993) 3.Lameh, J., Burstein, E.S., Taylor, E., et al.Pharmacology of N-desmethylclozapinePharmacol. Ther.115(2)223-231(2007) 4.Odagaki, Y., Kinoshita, M., and Ota, T.Comparative analysis of pharmacological properties of xanomeline and N-desmethylclozapine in rat brain membranesJ. Psychopharmacol.30(9)896-912(2016) 5.Maehara, S., Hikichi, H., and Ohta, H.Behavioral effects of N-desmethylclozapine on locomotor activity and sensorimotor gating function in mice-Possible involvement of muscarinic receptorsBrain Res.1418111-119(2011)