Befiradol (hydrochloride)

NLX-112 (hydrochloride); F 13640 (hydrochloride)

C20H23Cl2F2N3O

DMSO : 125 mg/mL (290.48 mM; Need ultrasonic)

Neuronal Signaling; GPCR/G Protein

Befiradol hydrochloride (NLX-112 hydrochloride) is a selective 5-HT_1A receptor agonist. IC50 & Target: 5-HT_1A receptor^[1]. In Vivo: Befiradol (F13640; NLX-112) reduces the activity of dorsal raphe serotonergic neurons at 0.2-18.2 ug/kg, i.v. (cumulative doses; ED₅₀=0.69 ug/kg, i.v.) and increases the discharge rate of 80% of mPFC pyramidal neurons in the same dose range (ED₅₀=0.62 ug/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 uM) also increases extracellular DA in a concentration-dependent manner. Both the systemic and local effects of Befiradol are prevented by prior (+/-)WAY100635 administration^[1].