Ciproxifan (maleate)

Ciproxifan is a histamine H3 receptor antagonist (Ki = 0.5 nM for inhibition of histamine release in rat synaptosomal preparations). It is selective for histamine H3 over histamine H1 and H2, M3 muscarinic, and alpha1D- and beta1-adrenergic receptors (Kis = 3.15-25 µM), as well as the serotonin (5-HT) receptor subtypes 5-HT1B, 5-HT2A, 5-HT3, and 5-HT4 (Kis = 1.58-15 µM) in radioligand binding assays. Ciproxifan (3-300 nM) inhibits relaxation in precontracted isolated guinea pig ileal longitudinal muscle induced by R-(-)-alpha-methylhistamine (Cay-25601). In vivo, ciproxifan reduces R-(-)-alpha-methylhistamine-induced water consumption in rats (ED50 = 0.09 mg/kg). It increases wake episode duration and latency to fall asleep in rats when administered at a dose of 2 mg/kg.Formal Name: cyclopropyl[4-[3-(1H-imidazol-4-yl)propoxy]phenyl]-methanone (2Z)-2-butenedioate. CAS Number: 184025-19-2. Synonyms: FUB-359. Molecular Formula: C16H18N2O2 . C4H4O4. Formula Weight: 386.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble. lambdamax: 213, 272 nm. SMILES: O=C(C1CC1)C2=CC=C(OCCCC3=CN=CN3)C=C2.OC(/C=C\C(O)=O)=O. InChi Code: 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.