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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 |
|---|
| Dimethindene
Dimethindene is a potent, selective histamine H1 antagonist. |
| ABT-288
ABT-288 is a competitive, potent and selective histamine H3 receptor (H3R) antagonist. |
| A-349821
A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. |
| Betazole
Betazole (Ametazole), a pyrazole analogue of histamine, is an orally active histamine H2 receptor agonist. |
| Tiotidine
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). |
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