CLOZAPINE N-OXIDE

General description

Clozapine N-oxide (CNO), inactive from of clozapine drug, activates G-protein-coupled receptors (GPCRs). CNO serves as a synthetic ligand for engineered human muscarinic receptor. It elicits clozapine-like effects upon metabolic conversion. Clozapine conversion to CNO favors its passage through blood-brain barrier.

Application

Clozapine N-oxide has been used:

• for the activation of human M4 muscarinic (hM4Di) in primary motor cortex
• for inducing in vivo chemogenetic manipulation and impairing locomotor activity in Th-cre transgenic mice
• in behavioral testing in mice and for stimulating (HEK293) cells

Biochem/physiol Actions

5-HT₂ serotonin receptor antagonist; major metabolite of clopazine that can be monitored by HPLC.

Features and Benefits

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Molecular Weight: 342.82. Empirical Formula: C₁₈H₁₉ClN₄O. form: solid. Quality Level: 200. SMILES string: C[N+]1([O-])CCN(CC1)C2: Nc3cc(Cl)ccc3Nc4ccccc24. InChI: 1S/C18H19ClN4O/c1-23(24)10-8-22(9-11-23)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,20H,8-11H2,1H3. InChI key: OGUCZBIQSYYWEF-UHFFFAOYSA-N. Pictograms: GHS06. Signal Word: Danger. Hazard Statements: H301 - H336. Precautionary Statements: P301 + P310 + P330. Hazard Classifications: Acute Tox. 3 Oral - STOT SE 3. Target Organs: Central nervous system. Storage Class Code: 6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable. Personal Protective Equipment: dust mask type N95 (US), Eyeshields, Faceshields, Gloves.