基本属性 生物活性体外研究体内研究 用途与合成方法 供应商
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Ciproxifan

基本属性 生物活性体外研究体内研究 用途与合成方法 供应商
Ciproxifan
Ciproxifan 性质
  • 密度 1.231
  • 溶解度 H2O: insoluble
  • 形态solid
  • 颜色white
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 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.
安全信息
Ciproxifan供应商更多
  • 公司名称:上海波以尔化工有限公司
  • 联系电话:
  • 产品介绍: 中文名称:Ciproxifan
    英文名称:FUB359
    CAS:184025-18-1
    纯度:98%min
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  • 公司名称:上海佰世凯化学科技有限公司
  • 联系电话:+86(0)21-20908456
  • 产品介绍: 英文名称:FUB 359
    CAS:184025-18-1
    备注:C14471
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  • 公司名称:上海景颜化工科技有限公司
  • 联系电话:13817811078,021-50426030
  • 产品介绍: 英文名称:FUB359
    CAS:184025-18-1
    纯度:98%
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  • 公司名称:Hangzhou Sage Chemical Co., Ltd.
  • 联系电话:0571-86818502
  • 产品介绍: 英文名称:Methanone, cyclopropyl[4-[3-(1H-iMidazol-4-yl)propoxy]phenyl]-
    CAS:184025-18-1
    纯度:98% 包装信息:1g;5g;100g;Bulk
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  • 公司名称:上海遐瑞医药科技有限公司
  • 联系电话:+86 21 61551611
  • 产品介绍: 英文名称:fub 359;Ciproxifan; cyclopropyl(4-(3-(1h-imidazol-5-yl)propoxy)phenyl)methanone
    CAS:184025-18-1
    纯度:98% 包装信息:50kg;25kg;10kg;5kg;500g;500mg; 备注:工业级/医药级
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