ciproxifan

Ciproxifan is a small molecule and potent, species-selective histamine H3 receptor inverse agonist/antagonist, originally developed as a pharmacological tool for research. It acts primarily by blocking H3 autoreceptors located on histaminergic nerve terminals, leading to increased release of histamine and potentially other neurotransmitters, with downstream effects including increased wakefulness, enhanced attention, and cognitive improvement in animal models. Ciproxifan shows very high affinity for rodent histamine H3 receptors (sub-nanomolar range) but only moderate affinity for human H3 receptors (Ki 46–180 nM). It has been studied as a potential treatment for sleep-wake disorders (including narcolepsy), cognitive dysfunction, Alzheimer's disease, and as an adjuvant in schizophrenia. Additionally, ciproxifan has been found to reversibly inhibit monoamine oxidase A (MAO A) and monoamine oxidase B (MAO B) at micromolar concentrations, an effect to consider at higher doses. While extensively used in research, ciproxifan is not approved for clinical use in humans.[1][3][4][5][7]

Other names

ciproxifancyclopropyl[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanoneMethanone cyclopropyl[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]-cyclopropyl-[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone184025-18-15EVQ7IRG99