マレイン酸シプロキシファン

説明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 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 . 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.

使用Ciproxifan is a potent histamine H3 receptor antagonist which affects histamine levels in the brain. It may be used in treatments for sleep and neurological disorders.