THIP

THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders[1][2][3].

Product Specifications

CAS Number

[64603-91-4]

Product Name Alternative

Gaboxadol

UNSPSC

12352005

Hazard Statement

H315, H319, H320

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/thip.html

Concentration

10mM

Purity

99.93

Solubility

DMSO : 50 mg/mL (ultrasonic; adjust pH to 3 with HCl) |H2O : 23.33 mg/mL (ultrasonic)

Smiles

O=C1C2=C(CNCC2)ON1

Molecular Formula

C6H8N2O2

Molecular Weight

140.14

Precautions

H315, H319, H320

References & Citations

[1]Drasbek KR, et al. THIP, a hypnotic and antinociceptive drug, enhances an extrasynaptic GABAA receptor-mediated conductance in mouse neocortex. Cereb Cortex. 2006 Aug;16 (8) :1134-41. |[2]Larsen M, et al. 5-Hydroxy-L-tryptophan alters gaboxadol pharmacokinetics in rats: involvement of PAT1 and rOat1 in gaboxadol absorption and elimination. Eur J Pharm Sci. 2010 Jan 31;39 (1-3) :68-75. |[3]Hoestgaard-Jensen K, et al. Probing α4βδ GABAA receptor heterogeneity: differential regional effects of a functionally selective α4β1δ/α4β3δ receptor agonist on tonic and phasic inhibition in rat brain. J Neurosci. 2014 Dec 3;34 (49) :16256-72.