N-Desmethylclozapine-d8(Synonyms: Norclozapine-d8; Desmethylclozapine-d8; Normethylclozapine-d8)

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N-Desmethylclozapine-d8 (Synonyms: Norclozapine-d8; Desmethylclozapine-d8; Normethylclozapine-d8)

N-Desmethylclozapine-d8 (Norclozapine-d8) 是 N-Desmethylclozapine 的氘代物。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。

N-Desmethylclozapine-d8(Synonyms: Norclozapine-d8; Desmethylclozapine-d8; Normethylclozapine-d8)

N-Desmethylclozapine-d8 Chemical Structure

CAS No. : 1189888-77-4

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生物活性

N-Desmethylclozapine-d8 (Norclozapine-d8) is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic drug Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

320.85

Formula

C17H9D8ClN4
CAS 号

1189888-77-4
中文名称

N-去甲基氯氮平 d8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Li Z, et al. N-desmethylclozapine, a major metabolite of clozapine, increases cortical acetylcholine and dopamine release in vivo via stimulation of M1 muscarinic receptors. Neuropsychopharmacology. 2005 Nov;30(11):1986-95.

    [3]. Odagaki Y, et al. Comparative analysis of pharmacological properties of xanomeline and N-desmethylclozapine in rat brain membranes. J Psychopharmacol. 2016 Sep;30(9):896-912

    [4]. Sugawara Y, et al. Electrophysiological evidence showing muscarinic agonist-antagonist activities of N-desmethylclozapine using hippocampal excitatory and inhibitory neurons. Brain Res. 2016 Jul 1;1642:255-62

    [5]. Gigout S, et al. Different pharmacology of N-desmethylclozapine at human and rat M2 and M 4 mAChRs in neocortex. Naunyn Schmiedebergs Arch Pharmacol. 2015 May;388(5):487-96

    [6]. Himmerich H, et al. Impact of clozapine, N-desmethylclozapine and chlorpromazine on thromboxane production in vitro. Med Chem. 2012 Nov;8(6):1032-8.

    [7]. Medigeshi GR, et al. N-Desmethylclozapine, Fluoxetine and Salmeterol inhibit post-entry stages of dengue virus life-cycle. Antimicrob Agents Chemother. 2016 Aug 29.

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