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Submit ReviewGR 103691
Description: Highly selective D3 antagonist
Chemical Name: 4'-Acetyl-N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-[1,1'-biphenyl]-4-carboxamide
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.
Licensing Information
Sold with the permission of GlaxoSmithKline
Technical Data for GR 103691
| M. Wt | 485.63 |
| Formula | C30H35N3O3 |
| Storage | Store at RT |
| CAS Number | 162408-66-4 |
| Smiles | COC1=CC=CC=C1N1CCN(CCCCNC(=O)C2=CC=C(C=C2)C2=CC=C(C=C2)C(C)=O)CC1 |
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.
Product Datasheets for GR 103691
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:
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
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
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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!
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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.
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