184025-18-1
184025-18-1 结构式
基本信息
中文别名
化合物CIPROXIFAN环丙基[4-[3-(1H-咪唑-5-基)丙氧基]苯
环丙基[4-[3-(1H-咪唑-5-基)丙氧基]苯基]甲酮
英文别名
CS-757FUB 359
Ciproxifan, >=99%
Ciproxifan USP/EP/BP
Ciproxifan (FUB-359)
Cyclopropyl[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone
Methanone, cyclopropyl[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]-
Methanone, cyclopropyl[4-[3-(1H-iMidazol-4-yl)propoxy]phenyl]-
所属类别
生物化工：Histamine Receptor 拮抗剂物理化学性质
沸点526.9±35.0 °C(Predicted)
密度1.231
储存条件2-8°C
溶解度H2O: insoluble
酸度系数(pKa)14.54±0.10(Predicted)
形态solid
颜色white
常见问题列表
生物活性
Ciproxifan是一种高效的，选择性的histamin H3-receptor拮抗剂，IC50为9.2 nM，作用于其他受体亚型具有低亲和力。体外研究
Ciproxifan inhibits [3H]HA release from synaptosomes with Ki of 0.5 nM. Ciproxifan inhibits the binding of [125I]iodoproxyfan at the brain H3 receptor with Ki of 0.7 nM. Ciproxifan displays high affinity at H3 receptor but shows low apparent affinity at other receptor subtypes as evaluated in functional tests on isolated organs (histamine H1 and H2, muscarinic M3, adrenergic α1D and β1, serotonin 5-HT1B, 5-HT2A, 5-HT3 and 5-HT4).体内研究
Ciproxifan intravenously injected at dose of 1 mg/kg decreases the H3-receptor ligand concentration in serum in Male Swiss mice, with half-times of distribution phase of 13min and elimination phase of 87 min, respectively. Ciproxifan (1 mg/kg, p.o.) rises brain t-MeHA level rapidly in Male Swiss mice, being already significantly increased after 30 min, reaching a plateau between 90 and 180 min and still remaining enhanced after 270 min. Ciproxifan leads to ED50 values of 0.23 mg/kg in cerebral cortex, 0.28 mg/kg in striatum and 0.30 mg/kg in hypothalamus in Male Wistar rats. Ciproxifan (3 mg/kg, i.p.) significantly increases choice accuracy as evaluated in the five-choice task performed using a short stimulus duration. 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 (10 mg/kg i.p.) enhances prepulse inhibition in the DBA/2 strain mice. Ciproxifan (3 mg/kg i.p.) alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimer's disease. Ciproxifan (3 mg/kg i.p.) improves accuracy and decreased impulsivity in adult male hooded Lister rats.靶点
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H 3 receptor 9.2 nM (IC 50 ) |