CIPROXIFAN

Description

Ciproxifan is a histamine H₃ receptor antagonist (K_i = 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 α_1D- and β₁-adrenergic receptors (K_is = 3.15-25 μM), as well as the serotonin (5-HT) receptor subtypes 5-HT_1B, 5-HT_2A, 5-HT₃, and 5-HT₄ (K_is = 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.

The Uses of CIPROXIFAN

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.

What are the applications of Application

Ciproxifan maleate is a potent and selective H3 histamine receptor antagonist

Biochem/physiol Actions

Potent, selective H3 histamine receptor antagonist.