Ciproxifan (maleate)

Ciproxifan (maleate)

CAT N°: 29513
Price:

49.00 41.65

Ciproxifan is a histamine H3 receptor antagonist (Ki = 0.5 nM for inhibition of histamine release in rat synaptosomal preparations).{54037} It is selective for histamine H3 over histamine H1 and H2, M3 muscarinic, and ?1D- and ?1-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-(–)-?-methylhistamine (Item No. 25601). In vivo, ciproxifan reduces R-(–)-?-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.

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