C6848

Ciproxifan maleate

≥98% (HPLC), powder

• Synonym(s): Cyclopropyl (4-[3-(1H-imidazol-4-yl)propyloxy]phenyl) ketone maleate salt, FUB 359 maleate salt
• Empirical Formula (Hill Notation): C₁₆H₁₈N₂O₂ · C₄H₄O₄
• CAS Number: 184025-19-2
• Molecular Weight: 386.40
• NACRES: NA.77
• PubChem Substance ID: 24892901
• UNSPSC Code: 12352200
• MDL number: MFCD06411563
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 32 mg/mL, H₂O: insoluble
• SMILES string: OC(=O)\C=C/C(O)=O.O=C(C1CC1)c2ccc(OCCCc3c[nH]cn3)cc2
• InChI: 1S/C16H18N2O2.C4H4O4/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14;5-3(6)1-2-4(7)8/h5-8,10-12H,1-4,9H2,(H,17,18);1-2H,(H,5,6)(H,7,8)/b;2-1-
• InChI key: RLQFKEYRALXXEJ-BTJKTKAUSA-N

Description

Application

Ciproxifan maleate has been used as a selective H3R antagonist to investigate the antidepressant potential of ciproxifan in chronic unpredictable stress (CUS) model of depression in mice.[1] It has also been used as an H3R antagonist to develop in vivo receptor occupancy assay for histamine H3 receptors (H3R)/to determine the occupancy of exogenous H3R antagonists using non-radiolabeled GSK189254 as a tracer in the rat.[2]

Biochem/physiol Actions

Cyclopropyl 4-(3-(1H-imidazol-4-yl)propyloxy)phenyl methanone (Ciproxifan) is a species-specific histamine H3 receptor (H3R) inverse agonist. It is mainly used as a reference H3R antagonist in rodent models for neurological diseases, Alzheimer′s disease, attention deficit hyperactivity disorder (ADHD), and sleep-wake disorders. It can block monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B) enzyme isoforms reversibly in humans and rats.[3]

Potent, selective H₃ histamine receptor antagonist.

Features and Benefits

This compound is featured on the Histamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Safety Information

• pictograms: GHS07
• signalword: Warning
• hcodes: H302,H315,H317,H319,H335
• pcodes: P261 - P264 - P280 - P301 + P312 - P302 + P352 - P305 + P351 + P338
• Hazard Classifications: Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2 - Skin Sens. 1 - STOT SE 3
• target_organs: Respiratory system
• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable
• ppe: dust mask type N95 (US), Eyeshields, Faceshields, Gloves