A GABAA receptor agonist and GABAC receptor antagonist
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Gaboxadol (hydrochloride)

Item No. 16355

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4,5,6,7-tetrahydro-isoxazolo[5,4-c]pyridin-3(2H)-one, monohydrochloride
CAS Number
85118-33-8
Synonyms
  • THIP
Molecular Formula
C6H8N2O2 • HCl
Formula Weight
176.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.1 mg/mlDMSO: 20 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
210 nm
SMILES
O=C(NO1)C2=C1CNCC2.Cl
InChi Code
InChI=1S/C6H8N2O2.ClH/c9-6-4-1-2-7-3-5(4)10-8-6;/h7H,1-3H2,(H,8,9);1H
InChi Key
ZDZDSZQYRBZPNN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $53

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    25 mg

    $95

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    50 mg

    $149

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    100 mg

    $241

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    Product Description

    Gaboxadol is a GABAA receptor agonist whose potency varies depending on the receptor subunit composition (partial agonist at α1β2γ2 (ED50 = 143 µM), full agonist at α5 (ED50 = 28-129 µM), and super agonist at α4β3δ (ED50 = 6 µM)).1 It also acts as an antagonist at ρ1 GABAC receptors (IC50 = 25 µM).1 Gaboxadol has been studied as a non-opioid analgesic and a novel hypnotic agent.2,3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Johnston, G.A.R., Chebib, M., Hanrahan, J.R., et al. Neurochemicals for the investigation of GABAC receptors. Neurochem. Res. 35(12), 1970-1977 (2010).

    2. Drasbek, K.R., and Jensen, K. THIP, a hypnotic and antinociceptive drug, enhances an extrasynaptic GABAA receptor-mediated conductance in mouse neocortex. Cereb. Cortex 16(8), 1134-1141 (2006).

    3. Vashchinkina, E., Panhelainen, A., Vekovischeva, O.Y., et al. GABA site agonist gaboxadol induces addiction-predicting persistent changes in ventral tegmental area dopamine neurons but is not rewarding in mice or baboons. J. Neurosci. 32(15), 5310-5320 (2012).

    4. Deacon, S., Staner, L., Staner, C., et al. Effect of short-term treatment with gaboxadol on sleep maintenance and initiation in patients with primary insomnia. Sleep 30(3), 281-287 (2007).