THIP
Product Specifications
UNSPSC Description
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].
Target Antigen
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
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 Weight
140.14
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-10232/THIP-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-10232/THIP-SDS-MedChemExpress.pdf
Clinical Information
Phase 3
CAS Number
64603-91-4
Available Sizes
Curated Selection
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