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Submit ReviewA 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
分子量 | 485.63 |
公式 | C30H35N3O3 |
储存 | 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 |
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.
参考文献是支持产品生物活性的出版物。
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
关键词: GR 103691, GR 103691 supplier, selective, D3, antagonists, Dopamine, Receptors, dopaminergic, GR103691, GlaxoSmithKline, GSK, 1109, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 GR 103691 的部分引用包括:
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
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
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
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
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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