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Submit ReviewGBR 12909 dihydrochloride
说明： Selective DA uptake inhibitor; also σ ligand
化学名： 1-[2-[Bis-(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride
纯度： ≥98% (HPLC)
生物活性 for GBR 12909 dihydrochloride
GBR 12909 dihydrochloride is a potent, competitive inhibitor of dopamine uptake (Ki = 1 nM for inhibition of striatal dopamine uptake). Has >100-fold lower affinity for the noradrenaline and 5-HT uptake carriers. Also a potent sigma ligand (IC50 = 48 nM). Centrally active following systemic administration.
化合物库 for GBR 12909 dihydrochloride
GBR 12909 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for GBR 12909 dihydrochloride
| 分子量 | 523.49 |
| 公式 | C28H32F2N2O.2HCl |
| 储存 | Desiccate at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 67469-78-7 |
| PubChem ID | 104920 |
| InChI Key | MIBSKSYCRFWIRU-UHFFFAOYSA-N |
| Smiles | Cl.Cl.FC1=CC=C(C=C1)C(OCCN1CCN(CCCC2=CC=CC=C2)CC1)C1=CC=C(F)C=C1 |
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.
溶解性数据 for GBR 12909 dihydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 2.62 | 5 温和加热 | |
| DMSO | 26.17 | 50 |
制备储备液 for GBR 12909 dihydrochloride
以下数据基于产品分子量 523.49。 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.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 3.82 mL | 19.1 mL | 38.21 mL |
| 2.5 mM | 0.76 mL | 3.82 mL | 7.64 mL |
| 5 mM | 0.38 mL | 1.91 mL | 3.82 mL |
| 25 mM | 0.08 mL | 0.38 mL | 0.76 mL |
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产品说明书 for GBR 12909 dihydrochloride
参考文献 for GBR 12909 dihydrochloride
参考文献是支持产品生物活性的出版物。
Andersen (1989) The DA uptake inhibitor GBR12909: selectivity and molecular mechanism of action. Eur.J.Pharmacol. 166 493 PMID: 2530094
Contreras et al (1990) GBR-12909 and fluspirilene potently inhibited binding of [3H] (+)3-PPP to sigma receptors in rat brain. Life Sci. 47 PL133 PMID: 1980329
Heikkila and Manzino (1984) Behavioral properties of GBR 12909, GBR 13069 and GBR 13098: specific inhibitors of DA uptake. Eur.J.Pharmacol. 103 241 PMID: 6237922
Spealman and Melia (1991) Pharmacological characterization of the discriminative-stimulus effects of GBR 12909. J.Pharmacol.Exp.Ther. 258 626 PMID: 1678014
If you know of a relevant reference for GBR 12909 dihydrochloride, please let us know.
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关键词: GBR 12909 dihydrochloride, GBR 12909 dihydrochloride supplier, Potent, σ, sigma, ligand, DA, uptake, inhibitors, inhibits, Selective, General, Receptors, DAT, Dopamine, Transporters, Monoamine, Neurotransmitter, GBR12909, dihydrochloride, Sigma-Related, 0421, Tocris Bioscience
12 篇 GBR 12909 dihydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GBR 12909 dihydrochloride 的部分引用包括：
Wang et al (2014) Enhanced synthesis and release of DA in transgenic mice with gain-of-function α6* nAChRs. J Neurochem 129 315 PMID: 24266758
Squillace et al (2014) Dysfunctional DArgic neurotransmission in asocial BTBR mice. Transl Psychiatry 4 e427 PMID: 25136890
Koprich et al (2011) Progressive neurodegeneration or endogenous compensation in an animal model of Parkinson's disease produced by decreasing doses of alpha-synuclein. PLoS One 6 e17698 PMID: 21408191
Navaroli et al (2011) The plasma membrane-associated GTPase Rin interacts with the DA transporter and is required for protein kinase C-regulated DA transporter trafficking. J Neurosci 31 13758 PMID: 21957239
Costa et al (2008) Electrophysiology and pharmacology of striatal neuronal dysfunction induced by mitochondrial complex I inhibition. J Neurosci 28 8040 PMID: 18685029
Visanji et al (2008) PYM50028, a novel, orally active, nonpeptide neurotrophic factor inducer, prevents and reverses neuronal damage induced by MPP+ in mesencephalic neurons and by MPTP in a mouse model of Parkinson's disease. FASEB J 22 2488 PMID: 18364399
Abdallah et al (2009) Impact of serotonin 2C receptor null mutation on physiology and behavior associated with nigrostriatal DA pathway function. Br J Pharmacol 29 8156 PMID: 19553455
Patel et al (2012) Soluble interleukin-6 receptor induces motor stereotypies and co-localizes with gp130 in regions linked to cortico-striato-thalamo-cortical circuits. PLoS One 7 e41623 PMID: 22911828
Koprich et al (2010) Expression of human A53T alpha-synuclein in the rat substantia nigra using a novel AAV1/2 vector produces a rapidly evolving pathology with protein aggregation, dystrophic neurite architecture and nigrostriatal degeneration with potential to model the pat Mol Neurodegener 5 43 PMID: 21029459
Beerepoot et al (2016) Pharmacological Chaperones of the DA Transporter Rescue DA Transporter Deficiency Syndrome Mutations in Heterologous Cells. J Biol Chem 291 22053 PMID: 27555326
Kim et al (2015) Spinal DArgic projections control the transition to pathological pain plasticity via a D1/D5-mediated mechanism. J Neurosci 35 6307 PMID: 25904784
Hutchinson et al (2012) Differential regulation of MeCP2 phosphorylation in the CNS by DA and serotonin. J Neurosci 37 321 PMID: 21956448
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GBR used as a selective DAT blocker for increasing dopamine release.
By
Anonymous on 05/15/2018
分析类型： Ex Vivo
种属： Mouse
GBR-12909 (300 nM) was used as a DAT blocker in slice voltametry experiments. It's difficult to get into solution. Just use some warming.
该领域的文献
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。
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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