Gaboxadol (hydrochloride)

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].

Product Specifications

CAS Number

[85118-33-8]

Product Name Alternative

Lu 02-030 (hydrochloride) ; THIP (hydrochloride)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

GABA Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/gaboxadol-hydrochloride.html

Purity

99.95

Solubility

DMSO : 75 mg/mL (ultrasonic) |H2O : ≥ 100 mg/mL

Smiles

O=C1C2=C(CNCC2)ON1.Cl

Molecular Formula

C6H9ClN2O2

Molecular Weight

176.60

Precautions

H302, H315, H319, H335

References & Citations

[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.