Description
A histamine H3 receptor antagonist (Ki = 0.5 nM for inhibition of histamine release in rat synaptosomal preparations); 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 5-HT1B, 5-HT2A, 5-HT3, and 5-HT4 (Kis = 1.58-15 µM) in radioligand binding assays; inhibits R-(–)-α-methylhistamine-induced relaxation in precontracted isolated guinea pig ileal longitudinal muscle from 3-300 nM; reduces R-(–)-α-methylhistamine-induced water consumption in rats (ED50 = 0.09 mg/kg); 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
Synonyms: FUB-359
Molecular weight: 386.4
CAS: 184025-19-2
Purity: ≥98%
Formulation: A crystalline solid
