[CAS NO. 184025-19-2] Ciproxifanmaleate
PRODUCTS SPECIFICATIONS [184025-19-2]
DESCRIPTION [184025-19-2]
Overview
| MDL | MFCD06411563 |
|---|---|
| Molecular Weight | 386.40 |
| Molecular Formula | C20H22N2O6 |
| SMILES | O=C(C1CC1)C2=CC=C(OCCCC3=CNC=N3)C=C2.O=C(O)/C=C\C(O)=O |
Summary
Ciproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable and competitive antagonist of histamine H 3 -receptor , with an IC 50 of 9.2 nM. Ciproxifan maleate displays low apparent affinity at other receptor subtypes. Ciproxifan maleate can be used for the research of aging disorders and Alzheimer's disease [1] [3] .
IC50 & Target
|
H 3 receptor 9.2 nM (IC 50 ) |
In Vitro
Ciproxifan inhibits [
3
H]HA release from synaptosomes of rat cerebral cortex, with a K
i
of 0.5 nM
[1]
.
Ciproxifan (0.01 nM-1 μM; 60 min) inhibits the binding of [
125
I]iodoproxyfan with rat striatal membranes, with a K
i
of 0.7 nM
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Ciproxifan (1 mg/kg; a single p.o.) increases the t-MeHA level in mouse brain, with an ED
50
of 0.14 mg/kg
[1]
.
Ciproxifan (3 mg/kg, i.p.) improves the accuracy of responding in the five-choice task in rats only when the stimulus duration is 0.25 sec instead of 0.50 sec
[1]
.
Ciproxifan (0.15-2 mg/kg; p.o.) induces marked signs of neocortical electroencephalogram activation manifested by enhanced fast-rhythms density and an almost total waking state in cats
[1]
.
Ciproxifan (1 mg/kg; a single i.v.) decreases the H
3
-receptor ligand concentration in serum in mice, with the half-lives (t
1/2
) of 13 and 87 min for the distribution and elimination phases in mice, respectively
[1]
.
Ciproxifan (1 mg/kg; a single p.o.) exhibits oral bioavailability (F=62%) and maximal concentration (C
max
=420 nM) in mice
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 258.80 mM )
H 2 O : 3.57 mg/mL ( 9.24 mM ; ultrasonic and warming and heat to 60°C)
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5880 mL | 12.9400 mL | 25.8799 mL |
| 5 mM | 0.5176 mL | 2.5880 mL | 5.1760 mL |
| 10 mM | 0.2588 mL | 1.2940 mL | 2.5880 mL |
References
- [1] Ligneau X, et, al. Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist. J Pharmacol Exp Ther. 1998 Nov;287(2):658-66.
- [2] Motawaj M, Arrang JM. Ciproxifan, a histamine H3-receptorantagonist / 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.
- [3] 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.
- [4] 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.
- [5] 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.
- [6] 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.
