184025-18-1 环丙基[4-[3-(1H-咪唑-5-基)丙氧基]苯基]甲酮

WGK Germany:3

• 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 [ 3 H]HA release from synaptosomes with K i of 0.5 nM. Ciproxifan inhibits the binding of [ 125 I]iodoproxyfan at the brain H3 receptor with K i of 0.7 nM. Ciproxifan displays high affinity at H 3 receptor but shows low apparent affinity at other receptor subtypes as evaluated in functional tests on isolated organs (histamine H 1 and H 2 , muscarinic M 3 , adrenergic α 1D and β 1 , serotonin 5-HT 1B , 5-HT 2A , 5-HT 3 and 5-HT 4 ).
• 体内研究 Ciproxifan intravenously injected at dose of 1 mg/kg decreases the H 3 -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 )

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