Ciproxifan

Ciproxifan (FUB 359) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan displays low apparent affinity at other receptor subtypes. Ciproxifan can be used for the research of aging disorders and Alzheimer's disease[1][3].

Product Specifications

CAS Number

[184025-18-1]

Product Name Alternative

FUB-359

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Histamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Neurological Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/ciproxifan.html

Purity

99.26

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1CC1)C(C=C2)=CC=C2OCCCC3=CN=CN3

Molecular Formula

C16H18N2O2

Molecular Weight

270.33

Precautions

H302, H315, H319, H335

References & Citations

[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.|[6]Ligneau X, et, al. Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist. J Pharmacol Exp Ther. 1998 Nov;287 (2) :658-66.