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Biological Activity for (RS)-Baclofen
(RS)-Baclofen is a selective GABAB receptor agonist. Skeletal muscle relaxant.
R-enantiomer also available.
Technical Data for (RS)-Baclofen
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for (RS)-Baclofen
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for (RS)-Baclofen
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References for (RS)-Baclofen
References are publications that support the biological activity of the product.
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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Keywords: (RS)-Baclofen, (RS)-Baclofen supplier, Selective, GABAB, agonists, Receptors, 0417, Tocris Bioscience
23 Citations for (RS)-Baclofen
Citations are publications that use Tocris products. Selected citations for (RS)-Baclofen include:
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
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
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
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
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
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
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
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
Doshina et al (2017) Cortical cells reveal APP as a new player in the regulation of GABAergic neurotransmission. Sci Rep 7 370 PMID: 28337033
Limó n et al (2019) Electrophysiological evaluation of extracellular spermine and alkaline pH on synaptic human GABAA receptors. Transl Psychiatry 9 218 PMID: 31488811
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
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
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
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
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
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
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
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Reviews for (RS)-Baclofen
Average Rating: 5 (Based on 1 Review.)
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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.
Literature in this Area
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GABA Receptors Scientific Review
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.
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