| Bioactivity | 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]. | ||||||||||||
| Invitro | THIP (1 µM; 5 s) induces a robust tonic GABAA-mediated current in layer 2/3 neurons[1].THIP (1 µM; 1 s) shows no affect miniature IPSCs in layer 2/3 neurons[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| In Vivo | THIP (Gaboxadol) (0.5, 5.0 mg/kg; p.o.; single) shws a good oral utilization, with Fa values of 110% and 83% for dosage of 0.5 and 5.0 mg/kg, respectively[2]. Animal Model: | ||||||||||||
| Name | THIP | ||||||||||||
| CAS | 64603-91-4 | ||||||||||||
| Formula | C6H8N2O2 | ||||||||||||
| Molar Mass | 140.14 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |