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Submit ReviewMore active enantiomer of (RS)-Baclofen, a selective GABAB agonist.
Racemate also available.
分子量 | 213.66 |
公式 | C10H12ClNO2 |
储存 | Store at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 69308-37-8 |
PubChem ID | 44602 |
InChI Key | KPYSYYIEGFHWSV-QMMMGPOBSA-N |
Smiles | NC[C@@](CC(O)=O)([H])C1=CC=C(Cl)C=C1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 4.27 | 20 温和加热 |
以下数据基于产品分子量 213.66。 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 |
---|---|---|---|
0.2 mM | 23.4 mL | 117.01 mL | 234.02 mL |
1 mM | 4.68 mL | 23.4 mL | 46.8 mL |
2 mM | 2.34 mL | 11.7 mL | 23.4 mL |
10 mM | 0.47 mL | 2.34 mL | 4.68 mL |
参考文献是支持产品生物活性的出版物。
Falch et al (1986) Comparative stereostructure-activity studies on GABAA and GABAB receptor sites and GABA uptake using rat brain membrane preparations. J.Neurochem. 47 898 PMID: 3016189
Hong et al (1991) Effects of phaclofen and the enantiomers of bac. on cardiovascular responses to intrathecal administration of L- and D-baclofen in the rat. Eur.J.Pharmacol. 196 267 PMID: 1654254
If you know of a relevant reference for (R)-Baclofen, please let us know.
关键词: (R)-Baclofen, (R)-Baclofen supplier, Selective, GABAB, agonists, Receptors, STX209, STX, 209, 0796, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 (R)-Baclofen 的部分引用包括:
Styr et al (2019) Mitochondrial Regulation of the Hippocampal Firing Rate Set Point and Seizure Susceptibility. Neuron 102 1009 PMID: 31047779
Zhang et al (2015) GABAB receptor upregulates fragile X mental retardation protein expression in neurons. Front Cell Neurosci 5 10468 PMID: 26020477
Wang et al (2015) Neuronal γ-aminobutyric acid (GABA) type A receptors undergo cognate ligand chaperoning in the endoplasmic reticulum by endogenous GABA. Mol Cell Neurosci 9 188 PMID: 26041994
Kirwan et al (2015) Development and function of human cerebral cortex neural networks from pluripotent stem cells in vitro. J Pharmacol Exp Ther 142 3178 PMID: 26395144
Hensler et al (2012) GABAB receptor-positive modulators: brain region-dependent effects. J Pharmacol Exp Ther 340 19 PMID: 21954301
Lobb et al (2010) A dynamic role for GABA receptors on the firing pattern of midbrain DArgic neurons. J Neurophysiol 104 403 PMID: 20445035
Bartoi et al (2010) GABAB receptor constituents revealed by tandem affinity purification from transgenic mice. J Biol Chem 285 20625 PMID: 20406808
Pacey et al (2011) Subchronic administration and combination metabotropic glutamate and GABAB receptor drug therapy in fragile X syndrome. Sci Rep 338 897 PMID: 21636656
Bragina et al (2015) Differential expression of metabotropic glutamate and GABA receptors at neocortical glutamatergic and GABAergic axon terminals. Front Cell Neurosci 9 345 PMID: 26388733
Chai et al (2017) Neural Circuit-Specialized Astrocytes: Transcriptomic, Proteomic, Morphological, and Functional Evidence. Neuron 95 531 PMID: 28712653
Xia et al (2014) Regulation of action potential waveforms by axonal GABAA receptors in cortical pyramidal neurons. PLoS One 9 e100968 PMID: 24971996
Messer and Levine (2012) Epileptiform activity in the CA1 region of the hippocampus becomes refractory to attenuation by cannabinoids in part because of endogenous γ-aminobutyric acid type B receptor activity. J Neurosci Res 90 1454 PMID: 22388975
Klug et al (2012) Genetic inhibition of CaMKII in dorsal striatal medium spiny neurons reduces functional excitatory synapses and enhances intrinsic excitability. PLoS One 7 e45323 PMID: 23028932
Piqueras and Martínez (2004) Peripheral GABAB agonists stimulate gastric acid secretion in mice. Br J Pharmacol 142 1038 PMID: 15210585
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Used to activate GABAb, direct application. Although it did not trigger any response, neither did GABA and this was expected, used it to confirm GABAb is not involved in our assay.
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.