生物活性 体外研究 体内研究 靶点
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Ciproxifan

生物活性 体外研究 体内研究 靶点
Ciproxifan,184025-18-1,结构式
Ciproxifan
  • CAS号:184025-18-1
  • 英文名:Ciproxifan
  • 中文名:Ciproxifan
  • CBNumber:CB2503297
  • 分子式:C16H18N2O2
  • 分子量:270.33
  • MOL File:184025-18-1.mol
Ciproxifan化学性质
  • 沸点 :526.9±35.0 °C(Predicted)
  • 密度 :1.231
  • 储存条件 :2-8°C
  • 溶解度 :H2O: insoluble
  • 酸度系数(pKa) :14.54±0.10(Predicted)
  • 形态 :solid
  • 颜色 :white
安全信息

Ciproxifan性质、用途与生产工艺

  • 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.
  • 靶点

    H 3 receptor

    9.2 nM (IC 50 )

Ciproxifan上下游产品信息
上游原料
下游产品
Ciproxifan生产厂家
  • 公司名称：Hangzhou Sage Chemical Co., Ltd.
  • 联系电话：+86057186818502 13588463833
  • 电子邮件：info@sagechem.com
  • 国家：中国
  • 产品数：10269
  • 优势度：58
  • 公司名称：MedChemexpress LLC
  • 联系电话：021-58955995
  • 电子邮件：sales@medchemexpress.cn
  • 国家：美国
  • 产品数：4863
  • 优势度：58
  • 公司名称：AdooQ BioScience, LLC
  • 联系电话：+1 (866) 930-6790
  • 电子邮件：info@adooq.com
  • 国家：美国
  • 产品数：2784
  • 优势度：58
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