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Clozapine N-oxide dihydrochloride
Biological Activity for Clozapine N-oxide dihydrochloride
Clozapine N-oxide dihydrochloride is a water-soluble salt of Clozapine N-oxide (Cat. No.4936). Activator of muscarinic DREADDs. Clozapine N-oxide dihydrochloride exhibits improved bioavailability (6 - 7-fold higher plasma concentration) compared with CNO, with less conversion to clozapine in animal studies.
Technical Data for Clozapine N-oxide dihydrochloride
|Storage||Desiccate at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Clozapine N-oxide dihydrochloride
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Clozapine N-oxide dihydrochloride
The following data is based on the product molecular weight 415.74. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.41 mL||12.03 mL||24.05 mL|
|5 mM||0.48 mL||2.41 mL||4.81 mL|
|10 mM||0.24 mL||1.2 mL||2.41 mL|
|50 mM||0.05 mL||0.24 mL||0.48 mL|
Product Datasheets for Clozapine N-oxide dihydrochloride
References for Clozapine N-oxide dihydrochloride
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for Clozapine N-oxide dihydrochloride, please let us know.
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Keywords: Clozapine N-oxide dihydrochloride, Clozapine N-oxide dihydrochloride supplier, Clozapine, N-oxide, 2HCl, metabolite, DREADDs, Ligands, muscarnic, designer, receptors, CNO, water, soluble, chemogenetics, (water-soluble), Multidrug, Transporters, Non-selective, Muscarinics, 6329, Tocris Bioscience
5 Citations for Clozapine N-oxide dihydrochloride
Citations are publications that use Tocris products. Selected citations for Clozapine N-oxide dihydrochloride include:
Khodai et al (2018) PACAP Neurons in the Ventromedial Hypothalamic Nucleus Are Glucose Inhibited and Their Selective Activation Induces Hyperglycaemia. Front Endocrinol (Lausanne) 9 632 PMID: 30425681
Fernandez et al (2018) Thalamic reticular control of local sleep in mouse sensory cortex. Elife 7 PMID: 30583750
Boender et al (2020) Striatal Astrocytes Shape Behavioral Flexibility via Regulation of the Glutamate Transporter EAAT2. Biol Psychiatry 89 1045 PMID: 33516457
Torre-Muruzabal et al (2019) Chronic nigral neuromodulation aggravates behavioral deficits and synaptic changes in an a-synuclein based rat model for Parkinson's disease. Acta Neuropathol Commun 7 160 PMID: 31640762
Chang et al (2019) The Ventral Hippocampus Controls Stress-Provoked Impulsive Aggression through the Ventromedial Hypothalamus in Post-Weaning Social Isolation Mice. Cell Rep 28 1195 PMID: 31365864
Do you know of a great paper that uses Clozapine N-oxide dihydrochloride from Tocris? Please let us know.
Reviews for Clozapine N-oxide dihydrochloride
Average Rating: 5 (Based on 1 Review.)
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Great water soluble version that worked beautifully in my hands. Used to stimulate virally-expressed hM4Di for behavioral neuroscience applications. CNO-induced activation of hM4Di significantly inhibited neuronal activation as confirmed via c-Fos staining.
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Chemogenetics Research Bulletin
Produced by Tocris, the chemogenetics research bulletin provides an introduction to chemogenetic methods to manipulate neuronal activity. It outlines the development of RASSLs, DREADDs and PSAMs, and the use of chemogenetic compounds. DREADD ligands and PSEMs available from Tocris are highlighted.
GPCR Efficacy and Biased Agonism Poster
GPCRs can interact with multiple distinct transducers or regulatory proteins and these can be preferentially engaged in an agonist-specific manner giving rise to biased agonism. This poster discusses cutting edge GPCR signaling pharmacology and highlights therapeutic applications of biased agonism.