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Submit Review(RS)-Baclofen
说明： Selective GABAB agonist
化学名： (RS)-4-Amino-3-(4-chlorophenyl)butanoic acid
纯度： ≥99% (HPLC)
生物活性 for (RS)-Baclofen
(RS)-Baclofen is a selective GABAB receptor agonist. Skeletal muscle relaxant.
R-enantiomer also available.
技术数据 for (RS)-Baclofen
| 分子量 | 213.66 |
| 公式 | C10H12ClNO2 |
| 储存 | Store at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 1134-47-0 |
| PubChem ID | 2284 |
| InChI Key | KPYSYYIEGFHWSV-UHFFFAOYSA-N |
| Smiles | OC(CC(CN)C1=CC=C(Cl)C=C1)=O |
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 (RS)-Baclofen
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| 1eq. NaOH | 100 |
制备储备液 for (RS)-Baclofen
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 |
|---|---|---|---|
| 1 mM | 4.68 mL | 23.4 mL | 46.8 mL |
| 5 mM | 0.94 mL | 4.68 mL | 9.36 mL |
| 10 mM | 0.47 mL | 2.34 mL | 4.68 mL |
| 50 mM | 0.09 mL | 0.47 mL | 0.94 mL |
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产品说明书 for (RS)-Baclofen
参考文献 for (RS)-Baclofen
参考文献是支持产品生物活性的出版物。
Berthelot et al (1991) 3-Thienylaminobutyric acid and 3-furylaminobutyric acids - synthesis and GABAB receptor binding studies. J.Med.Chem. 34 2557 PMID: 1652022
Bowery et al (1993) GABAB receptor pharmacology. Annu.Rev.Pharmacol.Toxicol. 33 109 PMID: 8388192
Hill et al (1981) 3H-Baclofen and 3H-GABA bind to bicuculline-insensitive GABAB sites in rat brain. Nature 290 149 PMID: 6259535
If you know of a relevant reference for (RS)-Baclofen, please let us know.
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关键词: (RS)-Baclofen, (RS)-Baclofen supplier, Selective, GABAB, agonists, Receptors, 0417, Tocris Bioscience
23 篇 (RS)-Baclofen 的引用文献
引用文献是使用了 Tocris 产品的出版物。 (RS)-Baclofen 的部分引用包括：
Yang et al (2013) PropF. inhibits superoxide production, elastase release, and chemotaxis in formyl peptide-activated human neutrophils by blocking formyl peptide receptor 1. J Immunol 190 6511 PMID: 23670191
Limó n et al (2019) Electrophysiological evaluation of extracellular spermine and alkaline pH on synaptic human GABAA receptors. Transl Psychiatry 9 218 PMID: 31488811
Chen et al (2014) Prolonged adenosine A1 receptor activation in hypoxia and pial vessel disruption focal cortical ischemia facilitates clathrin-mediated AMPA receptor endocytosis and long-lasting synaptic inhibition in rat hippocampal CA3-CA1 synapses: differential regulat J Neurosci 34 9621 PMID: 25031403
Baloucoune et al (2012) GABAB receptor subunit GB1 at the cell surface independently activates ERK1/2 through IGF-1R transactivation. PLoS One 7 e39698 PMID: 22761875
Takesian et al (2010) Presynaptic GABA(B) receptors regulate experience-dependent development of inhibitory short-term plasticity. J Neurosci 30 2716 PMID: 20164356
Tu et al (2010) GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation. J Neurosci 30 749 PMID: 20071540
Jakubs et al (2006) Environment matters: synaptic properties of neurons born in the epileptic adult brain develop to reduce excitability. Neuron 52 1047 PMID: 17178407
Yu et al (2016) Dentate cannabinoid-sensitive interneurons undergo unique and selective strengthening of mutual synaptic inhibition in experimental epilepsy. Neurobiol Dis 89 23 PMID: 26804027
Olmos-Serrano et al (2010) Defective GABAergic neurotransmission and pharmacological rescue of neuronal hyperexcitability in the amygdala in a mouse model of fragile X syndrome. Neuropharmacology 30 9929 PMID: 20660275
Rubio et al (2015) Context-induced reinstatement of metha. seeking is associated with unique molecular alterations in Fos-expressing dorsolateral striatum neurons. J Neurosci 35 5625 PMID: 25855177
Maher and Westbrook (2008) Co-transmission of DA and GABA in periglomerular cells. J Neurosci 99 1559 PMID: 18216231
Miyazato et al (2008) GABA receptor activation in the lumbosacral spinal cord decreases detrusor overactivity in spinal cord injured rats. J Urol 179 1178 PMID: 18206170
Vergassola et al (2018) Presynaptic mGlu1 Receptors Control GABAB Receptors in an Antagonist-Like Manner in Mouse Cortical GABAergic and Glutamatergic Nerve Endings. Front Mol Neurosci 11 324 PMID: 30279647
Wojnicki et al (2013) Baclofen-induced reductions in optional food intake depend upon food composition. Appetite 64 62 PMID: 23321345
Zemoura et al (2013) Endoplasmic reticulum-associated degradation controls cell surface expression of γ-aminobutyric acid, type B receptors. J Biol Chem 288 34897 PMID: 24114844
Bray and Mynlieff (2009) Influx of calcium through L-type calcium channels in early postnatal regulation of chloride transporters in the rat hippocampus. Dev Neurobiol 69 885 PMID: 19777558
Petzold et al (2008) Coupling of neural activity to blood flow in olfactory glomeruli is mediated by astrocytic pathways. J Neurosci 58 897 PMID: 18579080
Won et al (2011) Identification and modulation of voltage-gated Ca2+ currents in zebrafish Rohon-Beard neurons. J Neurophysiol 105 442 PMID: 20962070
Terunuma et al (2015) Purinergic receptor activation facilitates astrocytic GABAB receptor calcium signalling. Front Cell Neurosci 88 74 PMID: 25261019
Bell et al (2015) Acetylcholine release in mouse hippocampal CA1 preferentially activates inhibitory-selective interneurons via α4β2* nicotinic receptor activation. J Neurophysiol 9 115 PMID: 25918499
Baquero et al (2015) Developmental changes in synaptic distribution in arcuate nucleus neurons. Neuropsychopharmacology 35 8558 PMID: 26041922
Kerkhof et al (2013) Social play behavior in adolescent rats is mediated by functional activity in medial prefrontal cortex and striatum. Neuropsychopharmacology 38 1899 PMID: 23568326
Doshina et al (2017) Cortical cells reveal APP as a new player in the regulation of GABAergic neurotransmission. Sci Rep 7 370 PMID: 28337033
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Baclofen effects on dopamine release.
By
Anonymous on 03/28/2018
分析类型： Ex Vivo
种属： Mouse
Effects of GABAB agonism on electrically stimulated dopamine release was measured using fast scan cyclic voltammetry. Baclofen (30uM) was bath applied. This is a maximal concentration.
Effect was pretty small on striatal dopamine release. This may be due to low expression on terminals.
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