THIP-d4
THIP-d4 (Gaboxadol-d4) is the deuterated-labeled THIP (HY-10232). THIP (Gaboxadol) is a blood-brain barrier-penetrant, orally active selective GABAA receptor agonist. THIP exhibits EC50 values of 33 μM and 130 μM for α4β2δ and α4β1δ receptors, respectively. THIP activates extrasynaptic GABAA receptors to produce tonic inhibition and inhibits GABAergic interneurons to cause disinhibition. THIP is used in research on insomnia, sleep disorders, and addictive behaviors.
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- CAS. Nr.: 2748778-97-2
- Formel: C6H4D4N2O2
- Molecular Weight:144.16
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
[3]|
α4β2δ 33 μM (EC50) |
α4β1δ 130 μM (EC50) |
Anwendung
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS. Nr. 2748778-97-2
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Unlabeled CAS 64603-91-4
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Molecular Weight 144.16
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Formel C6H4D4N2O2
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SMILES
O=C1C2=C(ON1)CNC([2H])([2H])C2([2H])[2H]
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Synonyms
Gaboxadol-d4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Drasbek KR, et al. THIP, a hypnotic and antinociceptive drug, enhances an extrasynaptic GABAA receptor-mediated conductance in mouse neocortex. Cerebral cortex (New York, N.Y. : 1991). 2006 Aug;16(8):1134-41. [Content Brief]
[2]. Larsen M, et al. 5-Hydroxy-L-tryptophan alters gaboxadol pharmacokinetics in rats: involvement of PAT1 and rOat1 in gaboxadol absorption and elimination. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 2010 Jan 31;39(1-3):68-75. [Content Brief]
[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.
[Content Brief]
[6]. Silverman NS, et al. Effects of gaboxadol on the expression of cocaine sensitization in rats. Experimental and clinical psychopharmacology. 2016 Apr;24(2):131-41. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)