Ciproxifan  ≥98%

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包装规格:1mg 5mg 10mg 25mg 50mg in glass bottle
产品简介:一种有效的,选择性的,具有口服活性和竞争性的组胺 H3 受体拮抗剂,IC50值为9.2nM。Ciproxifan 对其他受体亚型的表观亲和力低。Ciproxifan 可用于研究衰老性疾病和阿尔兹海默症。
靶点:H3 receptor:9.2 nM (IC50)
体外研究: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.
体内研究: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.
保存条件:-20℃
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