Ciproxifan

Ciproxifan

中文名称Ciproxifan
中文同义词环丙基[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;化合物CIPROXIFAN
英文名称Ciproxifan
英文同义词Cyclopropyl[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone;FUB 359;Methanone, cyclopropyl[4-[3-(1H-iMidazol-4-yl)propoxy]phenyl]-;Ciproxifan, >=99%;CS-757;Ciproxifan (FUB-359);Methanone, cyclopropyl[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]-;Ciproxifan USP/EP/BP
CAS号184025-18-1
分子式C16H18N2O2
分子量270.33
EINECS号
相关类别神经信号;小分子抑制剂,天然产物;Inhibitors
Mol文件184025-18-1.mol
结构式Ciproxifan 结构式

Ciproxifan 性质

沸点526.9±35.0 °C(Predicted)
密度1.231
储存条件2-8°C
溶解度不溶于水
酸度系数(pKa)14.54±0.10(Predicted)
形态固体
颜色白色

Ciproxifan 用途与合成方法

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。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).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.

H 3 receptor

9.2 nM (IC 50 )

安全信息

危险品标志Xn
危险类别码22-36/37/38-43
安全说明26-36/37/39
WGK Germany3

MSDS信息

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