Ciproxifan  (Synonyms: FUB-359)

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].

Ciproxifan inhibits [³H]HA release from synaptosomes of rat cerebral cortex, with a K_i of 0.5 nM^[1].
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^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Ciproxifan (1 mg/kg; a single p.o.) increases the t-MeHA level in mouse brain, with an ED₅₀ of 0.14 mg/kg^[1].
Ciproxifan (3 mg/kg, i.p.) improves the accuracy of responding in the five-choice task in rats only when the stimulus duration was 0.25 sec instead of 0.50 sec^[1].
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^[1].
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^[1].
Ciproxifan (1 mg/kg; a single p.o.) exhibits oral bioavailability (F=62%) and maximal concentration (C_max=420 nM) in mice^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

270.33

C₁₆H₁₈N₂O₂

184025-18-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. 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.  [Content Brief]

  [2]. 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.  [Content Brief]

  [3]. 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.  [Content Brief]

  [4]. 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.  [Content Brief]

  [5]. 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.  [Content Brief]

  [6]. 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.  [Content Brief]