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Ciproxifan maleate

CAS No. : 184025-19-2

MCE 站：Ciproxifan maleate

产品活性：Ciproxifan maleate (FUB 359 maleate) 是一种有效的，选择性的，具有口服活性和竞争性的组胺 H₃ 受体拮抗剂，IC₅₀ 值为 9.2 nM。Ciproxifan maleate 对其他受体亚型的表观亲和力低。Ciproxifan maleate 可用于研究衰老性疾病和阿尔兹海默症。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation

作用靶点：Histamine Receptor

In Vitro: Ciproxifan inhibits [³H]HA release from synaptosomes of rat cerebral cortex, with a K_i of 0.5 nM.
Ciproxifan (0.01 nM-1 μM; 60 min) inhibits the binding of [¹²⁵I]iodoproxyfan with rat striatal membranes, with a K_i of 0.7 nM.

In Vivo: Ciproxifan (1 mg/kg; a single p.o.) increases the t-MeHA level in mouse brain, with an ED₅₀ of 0.14 mg/kg.
Ciproxifan (3 mg/kg, i.p.) improves the accuracy of responding in the five-choice task in rats only when the stimulus duration is 0.25 sec instead of 0.50 sec.
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 (1 mg/kg; a single i.v.) decreases the H₃-receptor ligand concentration in serum in mice, with the half-lives (t_1/2) of 13 and 87 min for the distribution and elimination phases in mice, respectively.
Ciproxifan (1 mg/kg; a single p.o.) exhibits oral bioavailability (F=62%) and maximal concentration (C_max=420 nM) in mice.

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