中文名 | Ciproxifan |
英文名 | Ciproxifan |
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-757 FUB 359 Ciproxifan 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]- |
CAS | 184025-18-1 |
化学式 | C16H18N2O2 |
分子量 | 270.33 |
密度 | 1.231 |
沸点 | 526.9±35.0 °C(Predicted) |
溶解度 | H2O: 不溶物 |
酸度系数 | 14.54±0.10(Predicted) |
存储条件 | 2-8°C |
外观 | 固体 |
颜色 | white |
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. |
危险品标志 | Xn - 有害物品 |
风险术语 | R22 - 吞食有害。 R36/37/38 - 刺激眼睛、呼吸系统和皮肤。 R43 - 与皮肤接触可能致敏。 |
安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S36/37/39 - 穿戴适当的防护服、手套和护目镜或面具。 |
WGK Germany | 3 |
上游原料 | 4-羟基苯基环丙酮 4-氟苯基环丙基甲酮 4-氯-4'-氟苯丁酮 |
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