| Identification | Back Directory | [Name]
Labeled d8 Desmethyl Clozapine Hydrochloride | [CAS]
1189888-77-4 | [Synonyms]
[2H8]-N-Desmethyl Clozapine
Labeled d8 Desmethyl Clozapine Hydrochloride
N-DESMETHYLCLOZAPINE (D8, 98%) 100 UG/ML IN METHANOL | [Molecular Formula]
C17H17ClN4 | [MDL Number]
MFCD09840368 | [MOL File]
1189888-77-4.mol | [Molecular Weight]
312.8 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 5 mg/ml | [form ]
A solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
A major labelled metabolite of clozapine. A potent and selective 5-HT2C serotonin receptor antogonist. | [Biological Activity]
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 | [storage]
Store at -20°C | [References]
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)
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