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Clozapine N-oxide dihydrochloride

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  • 10mg
    ¥1225.00
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Clozapine N-oxide dihydrochloride 是 Clozapine 的主要代谢物和人类毒蕈碱设计受体 (DREADDs) 激动剂。

货号:ajcx27536
CAS:2250025-93-3
分子式:C18H19ClN4O.2HCl
分子量:415.74
溶解度:Soluble in DMSO
纯度:98%
存储:Store at -20°C
库存:现货

Background:

Water soluble salt of Clozapine N-oxide (Cat.No.4936). Activator of muscarinic DREADDs. Exhibits improved bioavailability (6 - 7-fold higher plasma concentration) compared with CNO, with less conversion to clozapine in animal studies.



Eiermann et al (1997) The involvement of CYP1A2 and CYP3A4 in the metabolism of cloz. Br.J.Clin.Pharmacol. 44 439 PMID:9384460 |Ambruster et al (2007) Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand. Proc.Natl.Acad.Sci.U.S.A. 104 5163 PMID:17360345 |Zaman et al (2014) LMO4 is essential for paraventricular hypothalamic neuronal activity and calcium channel expression to prevent hyperphagia. J.Neurosci. 34 140 PMID:24381275 |Gomez et al (2017) Chemogenetics revealed: DREADD occupancy and activation via converted cloz. Science 357 503 PMID:28774929 |Roth et al (2016) DREADDs for Neuroscientists. Neuron 89 683 PMID:26889809 |Nakajima et al (2016) Gs-coupled GPCR signalling in AgRP neurons triggers sustained increase in food intake. Nat.Commun. 8 10268 PMID:26743492 |Allen et al (2019) A comparative study of the pharmacokinetics of cloz. N-oxide and cloz. N-oxide hydrochloride salt in rhesus macaques. J.Pharmacol.Exp.Ther. 368 199 PMID:30523062

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