Ciproxifan hydrochloride_product_DataBase

Bioactivity	Ciproxifan (FUB 359) hydrochloride is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan hydrochloride displays low apparent affinity at other receptor subtypes. Ciproxifan hydrochloride can be used for the research of aging disorders and Alzheimer's disease[1][3].
Invitro	Ciproxifan hydrochloride inhibits [3H]HA release from synaptosomes of rat cerebral cortex, with a Ki of 0.5 nM[1].Ciproxifan hydrochloride (0.01 nM-1 μM; 60 min) inhibits the binding of [125I]iodoproxyfan with rat striatal membranes, with a Ki of 0.7 nM[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Ciproxifan hydrochloride 相关抗体:
In Vivo	Ciproxifan hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride (1 mg/kg; a single i.v.) decreases the H3-receptor ligand concentration in serum in mice, with the half-lives (t1/2) of 13 and 87 min for the distribution and elimination phases in mice, respectively[1].Ciproxifan hydrochloride (1 mg/kg; a single p.o.) exhibits oral bioavailability (F=62%) and maximal concentration (Cmax=420 nM) in mice[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
CAS	1049741-81-2
Formula	C16H19ClN2O2
Molar Mass	306.79
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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. [2]. Motawaj M, Arrang JM. Ciproxifan, a histamine H₃-receptor antagonist / inverse agonist, modulates methamphetamine-induced sensitization in mice. Eur J Neurosci. 2011 Apr;33(7):1197-204. [3]. Mark E Bardgett, 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. [4]. Mark E Bardgett, 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. [5]. Mark Day, 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. [6]. Catherine Pillot, 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.

PeptideDB

Ciproxifan hydrochloride

CAS: 1049741-81-2 F: C16H19ClN2O2 W: 306.79