Befiradol (hydrochloride)

Befiradol (NLX-112) hydrochloride is a highly selective 5-HT₁A receptor agonist that acts on both presynaptic and postsynaptic sites. Befiradol hydrochloride attenuates sedative agent-induced respiratory depression in neonatal and adult rats. Befiradol reduces the duration of sedative agent-induced analgesia and sedation in adult rats. Befiradol hydrochloride can be used in studies related to opioid-induced respiratory depression^[1]. IC50 & Target:5-HT_1A receptor^[1]. In Vitro:Befiradol (1-30 μM) hydrochloride does not alleviate DAMGO-induced respiratory depression or alter baseline respiratory rhythm in vitro neonatal rat brainstem-spinal cord preparations^[1]. In Vivo:Befiradol (0.6 mg/kg; subcutaneous injection; single bolus) hydrochloride alleviates sedative agent-induced respiratory depression in neonatal rats by significantly increasing respiratory rate, tidal volume and minute ventilation, and exhibits a superior effect compared with the normal saline control group^[1].
Befiradol (0.1-0.4 mg/kg; intravenous injection; single bolus) hydrochloride dose-dependently attenuates sedative agent-induced respiratory depression and sedation in adult rats, but also significantly reduces sedative agent-induced analgesic effects at effective doses^[1].
Befiradol (0.2 mg/kg; subcutaneous injection; single bolus dose) hydrochloride induces hyperventilation, hyperalgesia and behavioral syndrome in normal adult rats^[1].