CAS 184025-19-2|Ciproxifan Maleate

Introduction：Basic information about CAS 184025-19-2|Ciproxifan Maleate, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Ciproxifan Maleate BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Articles1
6. Synonyms

Common Name	Ciproxifan Maleate
CAS Number	184025-19-2	Molecular Weight	386.398
Density	/	Boiling Point	743.6ºC at 760 mmHg
Molecular Formula	C₂₀H₂₂N₂O₆	Melting Point	/
MSDS	ChineseUSA	Flash Point	403.5ºC
Symbol	GHS07	Signal Word	Warning

Names

Name	(Z)-but-2-enedioic acid,cyclopropyl-[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone
Synonym	More Synonyms

Ciproxifan Maleate BiologicalActivity

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 ReceptorSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch 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.

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 ReceptorSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch 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.

Chemical & Physical Properties

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
InChIKey	RLQFKEYRALXXEJ-BTJKTKAUSA-N
SMILES	O=C(O)C=CC(=O)O.O=C(c1ccc(OCCCc2cnc[nH]2)cc1)C1CC1
Storage condition	-20℃

Safety Information

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

Articles1

Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist.

J. Pharmacol. Exp. Ther. 287 , 658-666, (1998)

Ciproxifan, i.e., cyclopropyl-(4-(3-1H-imidazol-4-yl)propyloxy) phenyl) ketone, belongs to a novel chemical series of histamine H3-receptor antagonists. In vitro, it behaved as a competitive antagonis...

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)

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