Ciproxifan
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- CAS号:
- 184025-18-1
- 英文名:
- Ciproxifan
- 英文别名:
- CS-757;FUB 359;Ciproxifan, >=99%;Ciproxifan (FUB-359);Ciproxifan USP/EP/BP;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]-
- 中文名:
- Ciproxifan
- 中文别名:
- 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
- CBNumber:
- CB2503297
- 分子式:
- C16H18N2O2
- 分子量:
- 270.33
- MOL File:
- 184025-18-1.mol
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Ciproxifan化学性质
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沸点:
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526.9±35.0 °C(Predicted)
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密度:
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1.231
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储存条件:
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2-8°C
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溶解度:
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H2O: insoluble
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酸度系数(pKa):
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14.54±0.10(Predicted)
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形态:
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solid
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颜色:
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white
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Ciproxifan性质、用途与生产工艺
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。
Ciproxifan inhibits [
3H]HA release from synaptosomes with K
i of 0.5 nM. Ciproxifan inhibits the binding of [
125I]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).
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.
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H
3
receptor
9.2 nM (IC
50
)
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Ciproxifan
上下游产品信息
上游原料
下游产品
184025-18-1, Ciproxifan 相关搜索:
- Inhibitors
- 小分子抑制剂，天然产物
- 神经信号
- 化合物CIPROXIFAN
- 环丙基[4-[3-(1H-咪唑-5-基)丙氧基]苯基]甲酮
- 环丙基[4-[3-(1H-咪唑-5-基)丙氧基]苯
- 184025-18-1
- Ciproxifan USP/EP/BP
- Methanone, cyclopropyl[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]-
- Ciproxifan (FUB-359)
- CS-757
- Ciproxifan, >=99%
- Methanone, cyclopropyl[4-[3-(1H-iMidazol-4-yl)propoxy]phenyl]-
- FUB 359
- Cyclopropyl[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone