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Biological Activity for GR 103691
A potent and selective dopamine D3 receptor antagonist, with a Ki value of 0.3 nM and > 100- fold selectivity over D2 and D4 sites.
Sold with the permission of GlaxoSmithKline
Technical Data for GR 103691
|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.
References for GR 103691
References are publications that support the biological activity of the product.
Audinot et al (1998) A comparative in vitro and in vivo pharmacological characterization of the novel DA D3 receptor antagonists (+)-S 14297, nafadotride, GR 103,691 and U 99194. J.Pharmacol.Exp.Ther. 287 187 PMID: 9765337
Hurley et al (1996) DA D3 receptors are not involved in the induction of c-fos mRNA by neuroleptic drugs: comparison of the DA D3 receptor antagonist GR 103691 with the typical and atypical neuroleptics. Eur.J.Pharmacol. 318 283 PMID: 9016916
Murray et al (1995) A novel series of arylpiperazines with high affinity and selectivity for the DA D3 receptor. Bioorg.Med.Chem.Lett. 5 219
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Keywords: GR 103691, GR 103691 supplier, selective, D3, antagonists, Dopamine, Receptors, dopaminergic, GR103691, GlaxoSmithKline, GSK, 1109, Tocris Bioscience
5 Citations for GR 103691
Citations are publications that use Tocris products. Selected citations for GR 103691 include:
Diaz et al (2014) Moderate Alcohol Exposure during the Rat Equivalent to the Third Trimester of Human Pregnancy Alters Regulation of GABAA Receptor-Mediated Synaptic Transmission by DA in the Basolateral Amygdala. Autophagy 2 46 PMID: 24904907
Chen et al (2006) DA D3 receptors regulate GABAA receptor function through a phospho-dependent endocytosis mechanism in nucleus accumbens. J Neurosci 26 2513 PMID: 16510729
Clemens and Hochman (2004) Conversion of the modulatory actions of DA on spinal reflexes from depression to facilitation in D3 receptor knock-out mice. J Neurosci 24 11337 PMID: 15601940
Wang et al (2015) A pivotal role of FOS-mediated BECN1/Beclin 1 upregulation in DA D2 and D3 receptor agonist-induced autophagy activation. Bone Res 11 2057 PMID: 26649942
Lee et al (2015) DArgic effects on in vitro osteogenesis. Mol Cancer 3 15020 PMID: 26558139
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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.
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.