"目录号: HY-14567

GPCR/G ProteinImmunology/Inflammation-

Ciproxifan(FUB-359)是高活性的H3受体拮抗剂，IC50为9.2 nM，对其它亚型受体的亲和力较低。

Histamine Receptor

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生物活性

Description

Ciproxifan(FUB-359) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.IC50 value: 9.2 nM(Ki)Target: H3 receptorIn vitro, Ciproxifan behaved as a competitive antagonist at the H3 autoreceptor controlling 3H histamine release from synaptosomes and displayed similar Ki values (0.5-1.9 nM) at the H3 receptor controlling the electrically-induced contraction of guinea pig ileum or at the brain H3 receptor labeled with 125I-iodoproxyfan. This appears to be an orally bioavailable, extremely selective and potent H3-receptor antagonist whose vigilance- and attention-promoting effects are promising for therapeutic applications in aging disorders.

References

[1].Motawaj M, Arrang JM.  Ciproxifan, a histamine H?-receptor antagonist?/?inverse agonist, modulates methamphetamine-induced sensitization in mice.  Eur J Neurosci. 2011 Apr;33(7):1197-204. doi: 10.1111/j.1460-9568.2011.07618.x.

[2].Bardgett ME, et al.  Ciproxifan, an H3 receptor antagonist, alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimer's disease.  Neurobiol Learn Mem. 2011 Jan;95(1):64-72.

[3].Bardgett ME, et al.  The H3 antagonist, ciproxifan, alleviates the memory impairment but enhances the motor effects of MK-801 (dizocilpine) in rats.  Neuropharmacology. 2010 Nov;59(6):492-502.

[4].Day M, et al.  Differential effects of ciproxifan and nicotine on impulsivity and attention measures in the 5-choice serial reaction time test.  Biochem Pharmacol. 2007 Apr 15;73(8):1123-34.

[5].Pillot C, et al.  Ciproxifan, a histamine H3-receptor antagonist/inverse agonist, modulates the effects of methamphetamine on neuropeptide mRNA expression in rat striatum.  Eur J Neurosci. 2003 Jan;17(2):307-14.