Ciproxifan (maleate)

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

Product Specifications

CAS Number

[184025-19-2]

Product Name Alternative

FUB 359 maleate

UNSPSC

12352005

Hazard Statement

H302, H315, H317, H319, H335

Target

Histamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/Ciproxifan-maleate.html

Purity

99.68

Solubility

DMSO : ≥ 100 mg/mL|H2O : 3.57 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C1CC1)C2=CC=C(OCCCC3=CNC=N3)C=C2.O=C(O)/C=C\C(O)=O

Molecular Formula

C20H22N2O6

Molecular Weight

386.40

Precautions

H302, H315, H317, H319, H335

References & Citations

[1]Motawaj M, Arrang JM. Ciproxifan, a histamine H3-receptorantagonist / 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, Davis NN, Schultheis PJ, Griffith MS. 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, Points M, Kleier J, Blankenship M, Griffith MS. 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, Héron A, Schwartz JC, Arrang JM. 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.