All AbMole products are for research use only, cannot be used for human consumption.
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.
| Molecular Weight | 386.4 |
| Formula | C16H18N2O2.C4H4O4 |
| CAS Number | 184025-19-2 |
| Solubility (25°C) | DMSO 50 mg/mL Ethanol 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Histamine Receptor Products |
|---|
| Antazoline hydrochloride
Antazoline hydrochloride is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine. |
| Azacyclonol
Azacyclonol, also known as γ-pipradol, which diminishes hallucinations in psychotic individuals. |
| Azatadine dimaleate
Azatadine dimaleate is an antihistamine and anticholinergic compound with IC50 of 6.5nM and 10nM, respectively. |
| Bepotastine Besilate
Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7. |
| Buclizine hydrochloride
Buclizine hydrochloride is an antihistamine and anticholinergic of the piperazine derivative family. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
