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SKF 83959 hydrobromide
Dopamine D1-like receptor partial agonist (Ki values are 1.18, 7.56, 920 and 399 nM for rat D1, D5, D2 and D3 receptors respectively). May act as an antagonist in vivo, producing anti-Parkinsonian effects and antagonizing the behavioral effects of cocaine. Shown to potentiate agonist binding of the σ1 receptor.
|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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 398.73. 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|
|0.5 mM||5.02 mL||25.08 mL||50.16 mL|
|2.5 mM||1 mL||5.02 mL||10.03 mL|
|5 mM||0.5 mL||2.51 mL||5.02 mL|
|25 mM||0.1 mL||0.5 mL||1 mL|
References are publications that support the biological activity of the product.
Platt et al (2000) Dissociation of cocaine-antagonist properties and motoric effects of the D1 receptor partial agonists SKF 83959 and SKF 77434. J.Pharmacol.Exp.Ther. 293 1017 PMID: 10869406
Cools et al (2002) SKF 83959 is an antagonist of DA D1-like receptors in the prefrontal cortex and nucleus accumbens: a key to its antiparkinsonian effect in animals? Neuropharmacology 42 237 PMID: 11804620
Neumeyer et al (2003) Receptor affinities of DA D1 receptor-selective novel phenylbenzazepines. Eur.J.Pharmacol. 474 137 PMID: 12921854
Guo et al (2013) SKF83959 is a potent allosteric modulator of sigma-1 receptor. Mol.Pharmacol. 83 577 PMID: 23295385
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Keywords: SKF 83959 hydrobromide, SKF 83959 hydrobromide supplier, D1-like, partial, agonists, Dopamine, D1, Receptors, D5, dopaminergic, SKF83959, hydrobromide, and, Sigma1, 2074, Tocris Bioscience
6 Citations for SKF 83959 hydrobromide
Citations are publications that use Tocris products. Selected citations for SKF 83959 hydrobromide include:
Perreault et al (2015) Regulation of c-fos expression by the DA D1-D2 receptor heteromer. Neuroscience 285 194 PMID: 25446350
Perreault et al (2013) A physiological role for the DA D5 receptor as a regulator of BDNF and Akt signalling in rodent prefrontal cortex. Int J Neuropsychopharmacol 16 477 PMID: 22827965
Fuenzalida et al (2014) DA D1 and corticotrophin-releasing hormone type-2α receptors assemble into functionally interacting complexes in living cells. PLoS One 171 5650 PMID: 25073922
Huang et al (2012) SKF83959, an agonist of phosphatidylinositol-linked D(1)-like receptors, promotes ERK1/2 activation and cell migration in cultured rat astrocytes. Nat Chem Biol 7 e49954 PMID: 23185493
Cassar et al (2015) A DA receptor contributes to paraquat-induced neurotoxicity in Drosophila. Pharmacol Biochem Behav 24 197 PMID: 25158689
Shen et al (2015) The DA D1-D2 receptor heteromer exerts a tonic inhibitory effect on the expression of amphetamine-induced locomotor sensitization. Br J Pharmacol 128 33 PMID: 25444866
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Dopamine Receptors Scientific Review
Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. 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.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.