Ciproxifan maleate is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.
iproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable, and competitive antagonist of the histamine H3 receptor, demonstrating an IC50 of 9.2 nM. It exhibits low apparent affinity at other receptor subtypes and is applicable for research into aging disorders and Alzheimer's disease [1][3].
体内研究
A single oral dose of Ciproxifan (1 mg/kg) increases t-MeHA levels in the mouse brain, with an ED50 of 0.14 mg/kg [1].
When administered intraperitoneally at 3 mg/kg, Ciproxifan enhances the accuracy of responding in the five-choice task in rats but only when the stimulus duration is 0.25 sec instead of 0.50 sec [1].
Oral administration of Ciproxifan at doses ranging from 0.15 to 2 mg/kg induces significant signs of neocortical electroencephalogram activation, characterized by enhanced fast-rhythms density and an almost complete waking state in cats [1].
Following a single intravenous dose of 1 mg/kg, Ciproxifan reduces H3-receptor ligand concentration in the serum in mice, with half-lives (t1/2) of 13 and 87 min for the distribution and elimination phases, respectively [1].
A single oral dose of Ciproxifan at 1 mg/kg demonstrates oral bioavailability (F=62%) and reaches maximal concentration (Cmax=420 nM) in mice [1].
体外研究
Ciproxifan inhibits [3H]HA release from synaptosomes of the rat cerebral cortex, with a Ki of 0.5 nM [1].
At concentrations ranging from 0.01 nM to 1 μM for 60 minutes, Ciproxifan inhibits the binding of [125I].iodoproxyfan with rat striatal membranes, with a Ki of 0.7 nM [1].
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