貨號	規(guī)格	價格	上海	北京	武漢	南京
S80834-5mg	98.2%	￥160.00 S80834-5mg ￥160.00 現(xiàn)貨	2 2	-	-	-
S80834-10mg	98.2%	￥304.00 S80834-10mg ￥304.00 現(xiàn)貨	2 2	-	-	-
S80834-25mg	98.2%	￥720.00 S80834-25mg ￥720.00 現(xiàn)貨	1 1	-	-	-

產(chǎn)品介紹

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

產(chǎn)品描述：

靶點：

mAChR1;δ Opioid Receptor/DOR;VirusProtease;DopamineReceptor;5-HTReceptor;OpioidReceptor;AChR;DrugMetabolite

體內(nèi)研究：

N-desmethylclozapine in rat and human at M2 and M4 mAChRs underlying presynaptic modulation of GABA and glutamate release, respectively. In particular, N-desmethylclozapine maybe a M2 mAChR antagonist in the rat but has no activity at this receptor in human neocortex. However, N-desmethylclozapine has an agonistic effect at M4 mAChR in the human but no such effect in the rat neocortex[4]

參考文獻：

1. 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. 2. 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 3. 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 4. 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 5. Himmerich H, et al. Impact of clozapine, N-desmethylclozapine and chlorpromazine on thromboxane production in vitro. Med Chem. 2012 Nov;8(6):1032-8. 6. Medigeshi GR, et al. N-Desmethylclozapine, Fluoxetine and Salmeterol inhibit post-entry stages of dengue virus life-cycle. Antimicrob Agents Chemother. 2016 Aug 29.

溶解性：

DMSO : ≥ 50 mg/mL (159.85 mM)

保存條件：

2-8℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	3.197 ml	15.985 ml	31.969 ml
5 mM	0.639 ml	3.197 ml	6.394 ml
10 mM	0.32 ml	1.598 ml	3.197 ml
50 mM	0.064 ml	0.32 ml	0.639 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻

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N-Desmethyl Clozapine