184025-18-1
184025-18-1 結(jié)構(gòu)式
基本信息
中文別名
化合物CIPROXIFAN環(huán)丙基[4-[3-(1H-咪唑-5-基)丙氧基]苯
環(huán)丙基[4-[3-(1H-咪唑-5-基)丙氧基]苯基]甲酮
英文別名
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]-
所屬類別
生物化工：Histamine Receptor 拮抗劑物理化學性質(zhì)
沸點526.9±35.0 °C(Predicted)
密度1.231
儲存條件2-8°C
溶解度H2O: insoluble
酸度系數(shù)(pKa)14.54±0.10(Predicted)
形態(tài)solid
顏色white
常見問題列表
生物活性
Ciproxifan是一種高效的，選擇性的histamin H3-receptor拮抗劑，IC50為9.2 nM，作用于其他受體亞型具有低親和力。體外研究
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).體內(nèi)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.靶點
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H 3 receptor 9.2 nM (IC 50 ) |