Befiradol hydrochloride (C09-1112-962)

Befiradol hydrochloride (NLX-112 hydrochloride) is a selective 5-HT 1A receptor agonist.In VivoBefiradol (F13640; NLX-112) reduces the activity of dorsal raphe serotonergic neurons at 0.2-18.2 μg/kg, i.v. (cumulative doses; ED 50 =0.69 μg/kg, i.v.) and increases the discharge rate of 80% of mPFC pyramidal neurons in the same dose range (ED 50 =0.62 μg/kg, i.v.). Both effects are reversed by the subsequent administration of the 5-HT 1A receptor antagonist (±)WAY100635. In microdialysis studies, Befiradol (F13640; NLX-112) (0.04-0.63 mg/kg, i.p.) dose-dependently decreases extracellular 5-HT in the hippocampus and mPFC. Likewise, Befiradol (F13640; NLX-112) (0.01-2.5 mg/kg, i.p.) dose-dependently increases extracellular DA in mPFC, an effect dependent on the activation of postsynaptic 5-HT 1A receptors in mPFC. Local perfusion of Befiradol in mPFC (1-1,000 μM) also increases extracellular DA in a concentration-dependent manner. Both the systemic and local effects of Befiradol are prevented by prior (±)WAY100635 administration . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:5-HT 1A Receptor. Molecular Formula: C20H23Cl2F2N3O Molecular Weight: 430.32