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184025-18-1

184025-18-1 structure
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
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
Hazard Codes Xn
Risk Phrases 22-36/37/38-43
Safety Phrases 26-36/37/39
WGK Germany 3