Gaboxadol hydrochloride_product_DataBase

Bioactivity	Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC 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].
Target	GABAA receptor; GABAC receptor
Invitro	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 Papp 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]. Animal Model:
Name	Gaboxadol hydrochloride
CAS	85118-33-8
Formula	C6H9ClN2O2
Molar Mass	176.60
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Reference	[1]. Johnston GA, et al. Neurochemicals for the investigation of GABA(C) receptors. Neurochem Res. 2010 Dec;35(12):1970-7. [2]. Cogram P, et al. Gaboxadol Normalizes Behavioral Abnormalities in a Mouse Model of Fragile X Syndrome.Front Behav Neurosci. 2019 Jun 25;13:141. [3]. Larsen M, et al. Intestinal gaboxadol absorption via PAT1 (SLC36A1): modified absorption in vivo following co-administration of L-tryptophan.Br J Pharmacol. 2009 Aug;157(8):1380-9.

PeptideDB

Gaboxadol hydrochloride

CAS: 85118-33-8 F: C6H9ClN2O2 W: 176.60