产品
编 号：F230170
分子式：C20H22N2O6
分子量：386.4
分子式：C20H22N2O6
分子量：386.4
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 184025-19-2
产品详情
生物活性：
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.
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 is 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.
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.
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.
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 is 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.
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.
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