Ciproxifan

Research use only, not for human use.

Ciproxifan is a highly effective and specific histamin H3-receptor antagonist (IC50: 9.2 nM).

Ciproxifan is a highly effective and specific histamin H3-receptor antagonist (IC50: 9.2 nM).

Ciproxifan inhibits [3H]HA release from synaptosomes of rat cerebral cortex, with a Ki of 0.5 nM.Ciproxifan (0.01 nM-1 μM; 60 min) inhibits the binding of [125I]iodoproxyfan with rat striatal membranes, with a Ki of 0.7 nM.

Ciproxifan (1 mg/kg; a single p.o.) increases the t-MeHA level in mouse brain, with an ED50 of 0.14 mg/kg.Ciproxifan (3 mg/kg, i.p.) improves the accuracy of responding in the five-choice task in rats only when the stimulus duration was 0.25 sec instead of 0.50 sec.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.Ciproxifan (1 mg/kg; a single i.v.) decreases the H3-receptor ligand concentration in serum in mice, with the half-lives (t1/2) of 13 and 87 min for the distribution and elimination phases in mice, respectively.Ciproxifan (1 mg/kg; a single p.o.) exhibits oral bioavailability (F=62%) and maximal concentration (Cmax=420 nM) in mice.

FUB-359

Others

Other Targets

H3 receptor

Neurological Disease

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184025-18-1

386.4

C16H18N2O2·C4H4O4

>98% (HPLC)

——

C1CC1C(=O)c1ccc(cc1)OCCCc1cnc[nH]1

——

(-20℃)

With Ice Pack

≥ 2 years