Ciproxifan maleate - CAS 184025-19-2
Catalog number: 184025-19-2
Category: Inhibitor
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Molecular Formula:
C20H22N2O6
Molecular Weight:
386.40
COA:
Inquire
Targets:
Histamine Receptor
Description:
Ciproxifan maleate, also called as FUB-359 maleate, is a highly potent and strongly selective histamine H3 inverse agonist/antagonist (IC50 = 9.2 nM) which displays little affinity for other receptor subtypes.
Appearance:
White solid
Synonyms:
(Z)-but-2-enedioic acid;cyclopropyl-[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone Ciproxifan maleate Ciproxifan (maleate) FUB 359 maleate salt 184025-19-2 Cyclopropyl (4-[3-(1H-imidazol-4-yl)propyloxy]phenyl) ketone maleate salt ciproxifan?FUB359 FUB 3
Solubility:
Soluble in DMSO
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -65℃ for long term (months to years).
MSDS:
Inquire
Shelf Life:
2 years
InChIKey:
RLQFKEYRALXXEJ-BTJKTKAUSA-N
InChI:
1S/C16H18N2O2.C4H4O4/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14;5-3(6)1-2-4(7)8/h5-8,10-12H,1-4,9H2,(H,17,18);1-2H,(H,5,6)(H,7,8)/b;2-1-
Canonical SMILES:
C1CC1C(=O)C2=CC=C(C=C2)OCCCC3=CN=CN3.C(=CC(=O)O)C(=O)O
1.Loss of Melanopsin Photoreception and Antagonism of the Histamine H3 Receptor by Ciproxifan Inhibit Light-Induced Sleep in Mice.
Muindi F1, Colas D2, Ikeme J2, Ruby NF2, Heller HC2. PLoS One. 2015 Jun 17;10(6):e0128175. doi: 10.1371/journal.pone.0128175. eCollection 2015.
Light has direct effects on sleep and wakefulness causing arousal in diurnal animals and sleep in nocturnal animals. In the present study, we assessed the modulation of light-induced sleep by melanopsin and the histaminergic system by exposing mice to millisecond light flashes and continuous light respectively. First, we show that the induction of sleep by millisecond light flashes is dose dependent as a function of light flash number. We found that exposure to 60 flashes of light occurring once every 60 seconds for 1-h (120-ms of total light over an hour) induced a similar amount of sleep as a continuous bright light pulse. Secondly, the induction of sleep by millisecond light flashes was attenuated in the absence of melanopsin when animals were presented with flashes occurring every 60 seconds over a 3-h period beginning at ZT13. Lastly, the acute administration of a histamine H3 autoreceptor antagonist, ciproxifan, blocked the induction of sleep by a 1-h continuous light pulse during the dark period.
2.Ciproxifan improves working memory through increased prefrontal cortex neural activity in sleep-restricted mice.
Chauveau F1, Laudereau K1, Libourel PA2, Gervasoni D2, Thomasson J1, Poly B1, Pierard C1, Beracochea D3. Neuropharmacology. 2014 Oct;85:349-56. doi: 10.1016/j.neuropharm.2014.04.017. Epub 2014 May 4.
Histamine receptor type 3 (H3) antagonists are promising awakening drugs for treatment of sleep disorders. However, few works have tried to identify their cognitive effects after sleep restriction and their impact on associated neural networks. To that aim, Bl/6J male mice were submitted to acute sleep restriction in a shaker apparatus that prevents sleep by transient (20-40 ms) up and down movements. Number of stimulations (2-4), and delay between 2 stimulations (100-200 ms) were randomized. Each sequence of stimulation was also randomly administered (10-30 s interval) for 20 consecutive hours during light (8 h) and dark (12 h) phases. Immediately after 20 h-sleep restriction, mice were injected with H3 antagonist (ciproxifan 3 mg/kg ip) and submitted 30-min later to a working memory (WM) task using spatial spontaneous alternation behaviour. After behavioural testing, brains were perfused for Fos immunohistochemistry to assess neuronal brain activation in the dorsal dentate gyrus (dDG) and the prefrontal cortex.
3.The Effect of Subchronic Dosing of Ciproxifan and Clobenpropit on Dopamine and Histamine Levels in Rats.
Mahmood D1, Pillai KK1, Khanam R1, Jahan K1, Goswami D2, Akhtar M1. J Exp Neurosci. 2015 Aug 31;9:73-80. doi: 10.4137/JEN.S27244. eCollection 2015.
The present study was designed to investigate the effect of once daily for 7-day (subchronic treatment) dosing of histamine H3 receptor antagonists, ciproxifan (CPX) (3 mg/kg, i.p.), and clobenpropit (CBP) (15 mg/kg, i.p), including clozapine (CLZ) (3.0 mg/kg, i.p.) and chlorpromazine (CPZ) (3.0 mg/kg, i.p.), the atypical and typical antipsychotic, respectively, on MK-801(0.2 mg/kg, i.p.)-induced locomotor activity, and dopamine and histamine levels in rats. Dopamine and histamine levels were measured in striatum and hypothalamus, respectively, of rat brain. Atypical and typical antipsychotics were used to serve as clinically relevant reference agents to compare the effects of the H3 receptor antagonists. MK-801-induced increase of horizontal activity was reduced with CPX and CBP. The attenuation of MK-801-induced locomotor hyperactivity produced by CPX and CBP was comparable to CLZ and CPZ. MK-801 raised dopamine levels in the striatum, which was reduced in rats pretreated with CPX and CBP.
4.Ciproxifan differentially modifies cognitive impairment evoked by chronic stress and chronic corticosterone administration in rats.
Trofimiuk E1, Braszko JJ2. Behav Brain Res. 2015 Apr 15;283:145-53. doi: 10.1016/j.bbr.2015.01.038. Epub 2015 Jan 29.
Despite the development of neuroscience and spectacular discoveries, the clear functions and the role of histamine are still not fully understood, especially in the context of the negative impact of prolonged stress exposure on the cognition. The purpose of this study was to evaluate the participation of hypercortisolemia in the detrimental effect of stress on cognitive function and their preclusion by affecting the histaminergic system with ciproxifan. Specifically, we attempted to characterize the preventive action of a single dose of ciproxifan (3mg/kg, i.p.) against an impairment caused by chronic restraint stress as well as parallel exogenous corticosterone (equivalent to that seen in chronically stressed rats), and show differences in the interaction on reference and working memories tested in both aversive (Morris water maze - MWM) and appetitive (Barnes maze-BM) incentives. We found that administration of ciproxifan potently prevented equally deleterious effects of chronic restraint stress (p<0.
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CAS 184025-19-2 Ciproxifan maleate

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