THIP

CAT: 0804-HY-10232-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-10232-01Size:5 mg
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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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3

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