184025-18-1

184025-18-1 structure

Name: Ciproxifan
Chemical Name: cyclopropyl-[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone
CAS Number: 184025-18-1
Molecular Formula: C₁₆H₁₈N₂O₂
Molecular Weight: 270.326
Catalog: Biochemical Inhibitor Neuronal Signaling Histamine Receptor Antagonist
Create Date: 2018-11-22 16:27:07
Modify Date: 2024-01-11 13:52:49
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.

Name	cyclopropyl-[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone
Synonyms	Ciproxifan cyclopropyl 4-(3-(1H-imidazol-4-yl)propyloxy)phenyl ketone Methanone, cyclopropyl[4-[3-(1H-imidazol-4-yl)propoxy]phenyl]- Cyclopropylpyrrol4-[3-(1H-imidazol-4-yl)propoxy] phenylmorphomethanone Cyclopropyl{4-[3-(1H-imidazol-4-yl)propoxy]phenyl}methanone FUB-359 cyclopropyl 4-(3-(1H-imidazol-4-yl)propyloxy)phenyl methanone

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.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Histamine Receptor Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Research Areas >> Neurological Disease
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.

Density	1.2±0.1 g/cm3
Boiling Point	526.9±35.0 °C at 760 mmHg
Molecular Formula	C₁₆H₁₈N₂O₂
Molecular Weight	270.326
Flash Point	272.5±25.9 °C
Exact Mass	270.136841
PSA	54.98000
LogP	2.29
Appearance	solid \| white
Vapour Pressure	0.0±1.4 mmHg at 25°C
Index of Refraction	1.613
Storage condition	-20℃
Water Solubility	H2O: insoluble