Ciproxifan CAS#: 184025-18-1

微信扫码

Ciproxifan

生物活性体外研究体内研究靶点

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	CS-757;Ciproxifan (FUB-359);Cyclopropyl[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone;FUB 359;Methanone, cyclopropyl[4-[3-(1H-iMidazol-4-yl)propoxy]phenyl]-;Ciproxifan, >=99%;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 性质

Ciproxifan 用途与合成方法

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 K_i of 0.5 nM. Ciproxifan inhibits the binding of [¹²⁵I]iodoproxyfan at the brain H3 receptor with K_i 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 α_1D and β₁, serotonin 5-HT_1B, 5-HT_2A, 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

安全信息

MSDS信息

Ciproxifan 上下游产品信息

上游原料

3-(1-三苯甲基-1H-咪唑-4-基)丙烷-1-醇4-羟基苯基环丙酮4-氟苯基环丙基甲酮4-氯-4'-氟苯丁酮