Ciproxifan maleate is a potent, selective, orally bioavailable, and competitive antagonist of the histamine H3-receptor, with an IC50 of 9.2 nM. It shows low apparent affinity at other receptor subtypes and can be used for the research of aging disorders and Alzheimer's disease.
- Inhibits [3H]HA release from synaptosomes of rat cerebral cortex (Ki: 0.5 nM).
- Inhibits binding of [125I]iodoproxyfan with rat striatal membranes (Ki: 0.7 nM).
- Increases t-MeHA level in mouse brain (ED50: 0.14 mg/kg).
- Improves accuracy of responding in five-choice tasks in rats.
- Induces neocortical electroencephalogram activation and waking state in cats.
- Decreases H3-receptor ligand concentration in serum in mice.
- Exhibits oral bioavailability (F=62%) and maximal concentration (Cmax=420 nM) in mice.