N-Desmethylclozapine
Cat. No.:YN321700
产品名称: | N-Desmethylclozapine |
CAS No.: | 6104-71-8 |
Chemical Name: | 8-chloro-11-(1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine |
Synonyms: | N-去甲基氯氮平; Norclozapine; Desmethylclozapine; Normethylclozapine |
分子量: | 312.80 |
分子式: | C₁₇H₁₇ClN₄ |
SMILES: | ClC1=CC=C2C(N=C(N3CCNCC3)C4=CC=CC=C4N2)=C1 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | N-Desmethylclozapine 是非典型抗精神病药 Clozapine 的主要活性代谢产物。N-Desmethylclozapine 是一种有效的、变构的部分M1受体激动剂 (EC50=115 nM),能通过 M1 受体激活增强海马 N-methyl-d-aspartate (NMDA) 受体电流。N-Desmethylclozapine 也是δ-opioid激动剂。 |
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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)
Kuoppamäki, M., Syvälahti, E., and Hietala, J.Clozapine and N-desmethylclozapine are potent 5-HT1C receptor antagonistsEur. J. Pharmacol.245(2),179-182(1993)
Lameh, J., Burstein, E.S., Taylor, E., et al.Pharmacology of N-desmethylclozapinePharmacol. Ther.115(2),223-231(2007)
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)
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.1418,111-119(2011)