THIP-d4

THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232) . 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

[2748778-97-2]

Product Name Alternative

Gaboxadol-d4

UNSPSC

12352005

Target

GABA Receptor; Isotope-Labeled Compounds

Type

Isotope-Labeled Compounds

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling; Others

Field of Research

Neurological Disease

Smiles

O=C1C2=C(ON1)CNC([2H])([2H])C2([2H])[2H]

Molecular Formula

C6H4D4N2O2

Molecular Weight

144.16

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.