Ciproxifan (maleate)

Ciproxifan is a histamine H3 receptor antagonist (Ki = 0.5 nM for inhibition of histamine release in rat synaptosomal preparations).1 It is selective for histamine H3 over histamine H1 and H2, M3 muscarinic, and α1D- and β1-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-(–)-α-methylhistamine (Item No. 25601). In vivo, ciproxifan reduces R-(–)-α-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.WARNING This product is not for human or veterinary use.

A histamine H3 receptor antagonist

386.4

≥98%

Biochemicals/Receptor Pharmacology/Antagonists

Formal_Name:cyclopropyl[4-[3-(1H-imidazol-4-yl)propoxy]phenyl]-methanone (2Z)-2-butenedioate;Synonyms:FUB-359

O=C(C1CC1)C2=CC=C(OCCCC3=CN=CN3)C=C2.OC(/C=C\C(O)=O)=O

C16H18N2O2 • C4H4O4

184025-19-2

≥ 4 years

DMSO: soluble