产品
编 号：F230169
分子式：C16H18N2O2
分子量：270.33
分子式：C16H18N2O2
分子量：270.33
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CAS No: 184025-18-1
产品详情
生物活性：
Ciproxifan (FUB 359) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan displays low apparent affinity at other receptor subtypes. Ciproxifan 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 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.
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 (FUB 359) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan displays low apparent affinity at other receptor subtypes. Ciproxifan 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 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.
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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