Gaboxadol (hydrochloride)

Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABA_A receptor and an antagonist of GABA_C receptors (IC₅₀=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED₅₀ value of 143 μM, a full agonist efficacy at α5 subunit (ED₅₀=28-129 μM) and a superagonist efficacy at α4β3δ (ED₅₀=6 μM). Gaboxadol hydrochloride is a non-opioid agent^[1][2]. IC50 & Target: GABA_A receptor; GABA_C receptor^[1] In Vitro: Gaboxadol hydrochloride (0.34, 3.5 and 7.0 μM) decreses permeability across Caco-2 cell monolayers with a dose dependent manner, shows the mean P_app values with 8.1 × 10^-6 cm·s^-1, 6.1 × 10^-1 cm·s^-6 and 5.6 × 10^-6 cm·s^-1 for 0.34, 3.5 and 7 μM gaboxadol, respectively^[3].
In Vivo: Gaboxadol hydrochloride (intraperitoneal injection; 0.5, 1, 1.5, 2, 3, 4, or 5 mg/kg; once daily; three-day interval) normalizes the distance traveled by Fmr1 KO2 mice to WT activity levels at 0.5 mg/kg, additionally, this compound has no effect on locomotor activity in Fmr1 KO2 mice^[2].