Ciproxifan (maleate)

Ciproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable and competitive antagonist of histamine H₃-receptor, with an IC₅₀ of 9.2 nM. Ciproxifan maleate displays low apparent affinity at other receptor subtypes. Ciproxifan maleate can be used for the research of aging disorders and Alzheimer's disease^[1][3]. IC50 & Target: IC50: 9.2 nM (histamine H3)^[1] In Vitro: Ciproxifan inhibits [³H]HA release from synaptosomes of rat cerebral cortex, with a K_i of 0.5 nM^[1].
Ciproxifan (0.01 nM-1 μM; 60 min) inhibits the binding of [¹²⁵I]iodoproxyfan with rat striatal membranes, with a K_i of 0.7 nM^[1]. In Vivo: Ciproxifan (1 mg/kg; a single p.o.) increases the t-MeHA level in mouse brain, with an ED₅₀ of 0.14 mg/kg^[1].
Ciproxifan (3 mg/kg, i.p.) improves the accuracy of responding in the five-choice task in rats only when the stimulus duration is 0.25 sec instead of 0.50 sec^[1].
Ciproxifan (0.15-2 mg/kg; p.o.) induces marked signs of neocortical electroencephalogram activation manifested by enhanced fast-rhythms density and an almost total waking state in cats^[1].
Ciproxifan (1 mg/kg; a single i.v.) decreases the H₃-receptor ligand concentration in serum in mice, with the half-lives (t_1/2) of 13 and 87 min for the distribution and elimination phases in mice, respectively^[1].
Ciproxifan (1 mg/kg; a single p.o.) exhibits oral bioavailability (F=62%) and maximal concentration (C_max=420 nM) in mice^[1].