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Submit ReviewTHIP hydrochloride
说明： GABAA agonist
别名： Gaboxadol
化学名： 4,5,6,7-Tetrahydroisoxazolo[5,4-c]pyridin-3-ol hydrochloride
纯度： ≥98% (HPLC)
生物活性 for THIP hydrochloride
THIP hydrochloride is a systemically active GABAA receptor agonist and GABAA-ρ receptor antagonist. Displays antinociceptive, anticonvulsant and sedative effects. Hypnotic agent that enhances delta activity within non-REM sleep in rats.
化合物库 for THIP hydrochloride
THIP hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for THIP hydrochloride
| 分子量 | 176.6 |
| 公式 | C6H8N2O2.HCl |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 85118-33-8 |
| PubChem ID | 5702253 |
| InChI Key | ZDZDSZQYRBZPNN-UHFFFAOYSA-N |
| Smiles | Cl.OC1=NOC2=C1CCNC2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for THIP hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 17.66 | 100 | |
| DMSO | 17.66 | 100 |
制备储备液 for THIP hydrochloride
以下数据基于产品分子量 176.6。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 5.66 mL | 28.31 mL | 56.63 mL |
| 5 mM | 1.13 mL | 5.66 mL | 11.33 mL |
| 10 mM | 0.57 mL | 2.83 mL | 5.66 mL |
| 50 mM | 0.11 mL | 0.57 mL | 1.13 mL |
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产品说明书 for THIP hydrochloride
参考文献 for THIP hydrochloride
参考文献是支持产品生物活性的出版物。
Huckle (2004) Gaboxadol. Lundbeck/Merck Curr.Opin.Investig.Drugs 5 766 PMID: 15298075
Johnston (1996) GABAC receptors: relatively simple transmitter-gated ion channels? TiPS 17 319 PMID: 8885697
Krogsgaard-Larson (1983) 4,5,6,7-Tetrahydroisothiazolo[5,4-c]pyridin-3-ol and related analogues of THIP. Synthesis and biological activity. J.Med.Chem. 26 895 PMID: 6304315
Krogsgaard-Larson (1984) Chemistry and pharmacology of the GABA antagonists THIP (Gaboxadol) and isoguvacine. Drugs Future. 9 597
If you know of a relevant reference for THIP hydrochloride, please let us know.
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关键词: THIP hydrochloride, THIP hydrochloride supplier, GABAC, antagonists, GABAA, agonists, Receptors, Gaboxadol, GABAA-rho, 0807, Tocris Bioscience
13 篇 THIP hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 THIP hydrochloride 的部分引用包括：
Glykys (2006) Hippocampal network hyperactivity after selective reduction of tonic inhibition in GABA A receptor alpha5 subunit-deficient mice. J Neurophysiol 95 2796 PMID: 16452257
Schmid et al (2010) Blindsight depends on the lateral geniculate nucleus. PLoS One 466 373 PMID: 20574422
Patel et al (2016) Context-Dependent Modulation of GABAAR-Mediated Tonic Currents. J Neurophysiol 36 607 PMID: 26758848
Krook-Magnuson et al (2008) Tonically active inhibition selectively controls feedforward circuits in mouse barrel cortex. J Neurosci 100 932 PMID: 18509076
Green and Thayer et al (2019) HIV gp120 upregulates tonic inhibition through α5-containing GABAARs. Neuropharmacology 149 161 PMID: 30797029
Seifi et al (2014) Molecular and functional diversity of GABA-A receptors in the enteric nervous system of the mouse colon. Nature 34 10361 PMID: 25080596
Szemes et al (2013) Weaker control of the electrical properties of cerebellar granule cells by tonically active GABAA receptors in the Ts65Dn mouse model of Down's syndrome. Mol Brain 6 33 PMID: 23870245
Yue et al (2011) Potentiating action of PropF. at GABAA receptors of retinal bipolar cells. Invest Ophthalmol Vis Sci 52 2497 PMID: 21071744
Ki and Lim (2019) Sleep-promoting effects of threonine link amino acid metabolism in Drosophila neuron to GABAergic control of sleep drive. Elife 8 PMID: 31313987
Tong et al (2015) Ectopic Expression of α6 and δ GABAA Receptor Subunits in Hilar Somatostatin Neurons Increases Tonic Inhibition and Alters Network Activity in the Dentate Gyrus. J Neurosci 35 16142 PMID: 26658866
Montandon (2017) δ-subunit containing GABAA receptors modulate respiratory networks. Sci Rep 7 18105 PMID: 29273726
Asiedu et al (2012) Modulation of spinal GABAergic analgesia by inhibition of chloride extrusion capacity in mice. J Pain 13 546 PMID: 22537560
Ramaker et al (2012) Effect of ganaxolone and THIP on operant and limited-access ethanol self-administration. Neuropharmacology 63 555 PMID: 22613838
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THIP hydrochloride 的评论
平均评分: 5 (Based on 1 Review.)
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THIP and in vivo chloride signals.
By
Anonymous on 05/23/2019
分析类型： In Vivo
种属： Mouse
细胞系/组织： c57Bl6J
used with fiber photometry to validate chloride sensor in vivo. response to footshock was measured at baseline and at 20 min intervals post-injection
injected 8mg/kg I.p. at 1mg/ml in saline
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