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 |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
| Related Histamine Receptor Products |
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| Peptide 401
Peptide 401, a potent mast cell degranulating factor from bee venom, suppresses the increased vascular permeability due to intradermal injection of various smooth muscle spasmogens (histamine, and 5-HT). |
| Granuliberin R
Granuliberin R is a new mast cell degranulating peptide comes from amphibian, can be isolated from the skin of frog Rana rugosa. |
| Dimethindene maleate
Dimethindene maleate is a selective histamine H1 receptor antagonist with antihistamine activity.Dimethindene maleate may be used in studies related to allergic reactions. |
| 4-Methylhistamine
4-Methylhistamine is a potent agonist of histamine 4 receptor (H4R). |
| H4R antagonist 3
H4R antagonist 3 is a histamine-4 receptor antagonist with an EC50 of ＜10 mM. |
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