65202-63-3
Chemical Structure
THIP (hydrobromid)
Synonym(s): Gaboxadol (hydrobromid)
- CAS No.: 65202-63-3
- Formula:C6H9BrN2O2
- Molecular Weight:221.05
IUPAC Name: 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3(2H)-one hydrobromide
InChIKey: UPVZCNRBPOAABW-UHFFFAOYSA-N
SMILES: O=C1NOC2=C1CCNC2.Br
Biological Activity: THIP (Gaboxadol) hydrobromide is a blood-brain barrier-penetrant, orally active selective GABAA receptor agonist. THIP hydrobromide exhibits EC50 values of 33 μM and 130 μM for α4β2δ and α4β1δ receptors, respectively. THIP hydrobromide activates extrasynaptic GABAA receptors to produce tonic inhibition and inhibits GABAergic interneurons to cause disinhibition. THIP hydrobromide is used in research on insomnia, sleep disorders, and addictive behaviors[1][2][3][4][5][6].
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THIP (hydrobromid) | THIP (Gaboxadol) hydrobromide is a blood-brain barrier-penetrant, orally active selective GABAA receptor agonist. THIP hydrobromide exhibits EC50 values of 33 μM and 130 μM for α4β2δ and α4β1δ receptors, respectively. THIP hydrobromide activates extrasynaptic GABAA receptors to produce tonic inhibition and inhibits GABAergic interneurons to cause disinhibition. THIP hydrobromide is used in research on insomnia, sleep disorders, and addictive behaviors. | |||||||||||||||||||||
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References
- [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]
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[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] - [4]. Winsky-Sommerer R, et al. The EEG effects of THIP (Gaboxadol) on sleep and waking are mediated by the GABA(A)delta-subunit-containing receptors. The European journal of neuroscience. 2007 Mar;25(6):1893-9.
- [5]. Vashchinkina E, et al. GABA site agonist gaboxadol induces addiction-predicting persistent changes in ventral tegmental area dopamine neurons but is not rewarding in mice or baboons. The Journal of neuroscience : the official journal of the Society for Neuroscience. 2012 Apr 11;32(15):5310-20.
- [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]
