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Ciproxifan maleate

Cat. No. M2088
Ciproxifan maleate Structure
Size Price Availability Quantity
10mg USD 120 In stock
50mg USD 456 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Ciproxifan maleate is a highly potent and selective H3-receptor antagonist with IC50 of 9.2 nM. In 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. Ciproxifan displayed at least 3-orders of magnitude lower potency at various aminergic receptors studied in functional or binding tests. In vivo, measurement of compound plasma levels, using a novel radioreceptor assay in mice receiving ciproxifan p.o. or i.v., led to an oral bioavailability ratio of 62%. Oral administration of ciproxifan to mice enhanced by approximately 100% histamine turnover rate and steady state level of tele-methylhistamine with an ED50 of 0.14 mg/kg. Ciproxifan reversed the H3-receptor agonist induced enhancement of water consumption in rats with and ID50 of 0.09 +/- 0.04 mg/kg, i.p. In cats, ciproxifan (0.15-2 mg/kg, p.o.) induced marked signs of neocortical electroencephalogram activation manifested by enhanced fast-rhythms density and an almost total waking state. In rats, ciproxifan enhanced attention as evaluated in the five-choice task performed using a short stimulus duration. Ciproxifan (3mg/kg i.p.) reduced premature responding, a measure of impulsivity.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 386.4
Formula C16H18N2O2.C4H4O4
CAS Number 184025-19-2
Purity >99%
Solubility DMSO 50 mg/mL
Ethanol 50 mg/mL
Storage at -20°C
References

Ciproxifan, an H3 receptor antagonist, alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimer's disease.
Bardgett ME, et al. Neurobiol Learn Mem. 2011 Jan;95(1):64-72. PMID: 21073971.

Differential effects of ciproxifan and nicotine on impulsivity and attention measures in the 5-choice serial reaction time test.
Day M, et al. Biochem Pharmacol. 2007 Apr 15;73(8):1123-34. PMID: 17214974.

Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist.
Ligneau X, et al. J Pharmacol Exp Ther. 1998 Nov;287(2):658-66. PMID: 9808693.

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Keywords: Ciproxifan maleate supplier, Histamine Receptor, inhibitors

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