184025-19-2

184025-19-2 structure

Name: Ciproxifan Maleate
Chemical Name: (Z)-but-2-enedioic acid,cyclopropyl-[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone
CAS Number: 184025-19-2
Molecular Formula: C₂₀H₂₂N₂O₆
Molecular Weight: 386.398
Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
Create Date: 2018-12-27 11:05:42
Modify Date: 2024-01-03 01:31:33
Ciproxifan maleate(FUB-359 maleate) 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: 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	(Z)-but-2-enedioic acid,cyclopropyl-[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone
Synonyms	FUB 359 maleate salt Ciproxifan maleate cc-128 Ciproxifan moleate cyclopropyl{4-[3-(1H-imidazol-4-yl)propoxy]phenyl}methanone (2Z)-but-2-enedioate (1:1) Cyclopropyl{4-[3-(1H-imidazol-5-yl)propoxy]phenyl}methanone (2Z)-2-butenedioate (1:1) Cyclopropyl (4-[3-(1H-imidazol-4-yl)propyloxy]phenyl) ketone maleate salt FUB 359 maleate salt methanone, cyclopropyl[4-[3-(1H-imidazol-4-yl)propoxy]phenyl]-, (2Z)-2-butenedioate (1:1) FUB359 maleate Methanone, cyclopropyl[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]-, (2Z)-2-butenedioate (1:1) Ciproxifan (maleate)

Description	Ciproxifan maleate(FUB-359 maleate) 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: 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, 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.

Boiling Point	743.6ºC at 760 mmHg
Molecular Formula	C₂₀H₂₂N₂O₆
Molecular Weight	386.398
Flash Point	403.5ºC
Exact Mass	386.147797
PSA	129.58000
LogP	2.72580
Vapour Pressure	3.22E-23mmHg at 25°C
Storage condition	-20℃

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302-H315-H317-H319-H335
Precautionary Statements	P261-P280-P305 + P351 + P338
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Faceshields;Gloves
Hazard Codes	Xn: Harmful;
Risk Phrases	R22
Safety Phrases	S26
RIDADR	NONH for all modes of transport

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