FUB-359

Cas 184025-18-1

Synobyms Ciproxifan; Cyclopropyl[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone

MF C16H18N2O2

MW 270.33

Density 1.231

Ciproxifan maleate

Cas 184025-19-2

Ciproxifan maleate salt

FUB 359

MF C16H18N2O2

MW 270.33

Abstract

Ciproxifan is an extremely potent histamine H3 inverse agonist/antagonist.

The histamine H3 receptor is an inhibitory autoreceptor located on histaminergic nerve terminals, and is believed to be involved in modulating the release of histamine in the brain. Histamine has an excitatory effect in the brain via H1 receptors in the cerebral cortex, and so drugs such as ciproxifan which block the H3 receptor and consequently allow more histamine to be released have an alertness-promoting effect.

Ciproxifan produces wakefulness and attentiveness in animal studies, and produced cognitive enhancing effects without prominent stimulant effects at relatively low levels of receptor occupancy, and pronounced wakefulness at higher doses. It has therefore been proposed as a potential treatment for sleep disorders such as narcolepsy and to improve vigilance in old age, particularly in the treatment of conditions such as Alzheimer's disease. It also potentiated the effects of antipsychotic drugs, and has been suggested as an adjuvant treatment for schizophrenia

Ciproxifan hydrochloride

Cas 1049741-81-2

Application A novel chemical series of histamine H3-receptor antagonists

MF C16H18N2O2 HCl

Mw 306.79

Purity 98%

Abstact Ciproxifan belongs to a novel chemical series of histamine H3-receptor antagonists. In vitro, it 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. This appears to be an orally bioavailable, extremely selective and potent H3-receptor antagonist whose vigilance- and attention-promoting effects are promising for therapeutic applications in aging disorders.

Form Solid

Solubility Soluble in DMSO: 30 mg/mL: water, high purity: 30 mg/mL

Storage Desiccate at 4° C

Reference Ligneau, X., et al.,, Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist. J. Pharmacol. Exp. Ther. 287, 658-666, (1998)