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Submit ReviewBD 1047 dihydrobromide
说明： σ1 selective antagonist
化学名： N-[2-(3,4-Dichlorophenyl)ethyl]-N-methyl-2-(dimethylamino)ethylamine dihydrobromide
纯度： ≥99% (HPLC)
生物活性 for BD 1047 dihydrobromide
BD 1047 dihydrobromide is a σ1 receptor antagonist, exhibiting a similar binding profile to that of BD 1063 (Cat. No. 0883) but with higher affinity (approximately 10-fold) at both σ1 and σ2 sites.
技术数据 for BD 1047 dihydrobromide
| 分子量 | 437.04 |
| 公式 | C13H20Cl2N2.2HBr |
| 储存 | Desiccate at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 138356-21-5 |
| PubChem ID | 45073418 |
| InChI Key | WOALTFHGLDVJHK-UHFFFAOYSA-N |
| Smiles | Br.Br.CN(C)CCN(C)CCC1=CC=C(Cl)C(Cl)=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 BD 1047 dihydrobromide
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 21.85 | 50 | |
| DMSO | 21.85 | 50 |
制备储备液 for BD 1047 dihydrobromide
以下数据基于产品分子量 437.04。 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 | 4.58 mL | 22.88 mL | 45.76 mL |
| 2.5 mM | 0.92 mL | 4.58 mL | 9.15 mL |
| 5 mM | 0.46 mL | 2.29 mL | 4.58 mL |
| 25 mM | 0.09 mL | 0.46 mL | 0.92 mL |
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产品说明书 for BD 1047 dihydrobromide
参考文献 for BD 1047 dihydrobromide
参考文献是支持产品生物活性的出版物。
Garrone et al (2000) Effects of traz. on neurotransmitter release from rat mossy fibre cerebellar synaptosomes. Eur.J.Pharmacol. 400 35 PMID: 10913582
Matsumoto et al (1995) Characterisation of two novel σ receptor ligands: antidystonic effects in rats suggest σ receptor antagonism. Eur.J.Pharmacol. 280 301 PMID: 8566098
Romieu et al (2000) Involvement of the sigma1 receptor in the cocaine-induced conditioned place preference. Neuroreport 11 2885 PMID: 11006959
If you know of a relevant reference for BD 1047 dihydrobromide, please let us know.
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关键词: BD 1047 dihydrobromide, BD 1047 dihydrobromide supplier, σ1, sigma1, selective, antagonist, receptors, BD1047, dihydrobromide, Sigma1, Receptors, 0956, Tocris Bioscience
23 篇 BD 1047 dihydrobromide 的引用文献
引用文献是使用了 Tocris 产品的出版物。 BD 1047 dihydrobromide 的部分引用包括：
Rodríguez-Muñoz et al (2015) The ON:OFF switch, σ1R-HINT1 protein, controls GPCR-NMDA receptor cross-regulation: implications in neurological disorders. Int J Neuropsychopharmacol 6 35458 PMID: 26461475
Son and Kwon (2010) σ-1 Receptor Antagonist BD1047 Reduces Allodynia and Spinal ERK Phosphorylation Following Chronic Compression of Dorsal Root Ganglion in Rats. J Neurophysiol 14 359 PMID: 21311675
Behensky et al (2013) Afobazole activation of σ-1 receptors modulates neuronal responses to amyloid-β25-35. J Pharmacol Exp Ther 347 468 PMID: 24006338
Amer et al (2013) Inhibition of endothelial cell Ca2+ entry and transient receptor potential channels by Sigma-1 receptor ligands. Br J Pharmacol 168 1445 PMID: 23121507
Pabba et al (2014) NMDA receptors are upregulated and trafficked to the plasma membrane after sigma-1 receptor activation in the rat hippocampus. J Neurosci 34 11325 PMID: 25143613
Moon et al (2014) σ1 receptors activate astrocytes via p38 MAPK phosphorylation leading to the development of mechanical allodynia in a mouse model of neuropathic pain. Br J Pharmacol 171 5881 PMID: 25158784
Lesch et al (2014) Activation and inhibition of transient receptor potential TRPM3-induced gene transcription. Br J Pharmacol 171 2645 PMID: 24895737
Sánchez-Blázquez et al (2018) The Sigma-1 Receptor Antagonist, S1RA, Reduces Stroke Damage, Ameliorates Post-Stroke Neurological Deficits and Suppresses the Overexpression of MMP-9. Mol Neurobiol 55 4940 PMID: 28779350
Sánchez-Blázquez et al (2018) Sigma 1 Receptor Antagonists Inhibit Manic-Like Behaviors in Two Congenital Strains of Mice. Int J Neuropsychopharmacol 21 938 PMID: 29860313
Gear et al (2014) NOP receptor mediates anti-analgesia induced by agonist-antagonist opioids. Neuroscience 257 139 PMID: 24188792
Hiranita et al (2011) Decreases in cocaine self-administration with dual inhibition of the DA transporter and σ receptors. J Pharmacol Exp Ther 339 662 PMID: 21859929
Nguyen et al (2014) Involvement of sigma-1 receptors in the antidepressant-like effects of dextromethorphan. PLoS One 9 e89985 PMID: 24587167
Kwon et al (2009) The Antinociceptive Effect of σ-1 Receptor Antagonist, BD1047, in a Capsaicin Induced Headache Model in Rats. Br J Ophthalmol 13 425 PMID: 20054487
Brailoiu et al (2019) Choline Is an Intracellular Messenger Linking Extracellular Stimuli to IP3-Evoked Ca2+ Signals through Sigma-1 Receptors. Cell Rep 26 330 PMID: 30625315
Sánchez-Blázquez et al (2014) The calcium-sensitive σ-1 receptor prevents cannabinoids from provoking glutamate NMDA receptor hypofunction: implications in antinociception and psychotic diseases. Korean J Physiol Pharmacol 17 1943 PMID: 24485144
Pan et al (2014) σ-1 receptor antagonism restores injury-induced decrease of voltage-gated Ca2+ current in sensory neurons. Exp Ther Med 350 290 PMID: 24891452
Su et al (2014) Effects of BD1047, aσ1 receptor antagonist, on the expression of mTOR, Camk2γ and GSK-3β in fluvoxamine-treated N2a cells. Oncotarget 7 435 PMID: 24396420
Kourrich et al (2013) Dynamic interaction between sigma-1 receptor and Kv1.2 shapes neuronal and behavioral responses to cocaine. Cell 152 236 PMID: 23332758
Roh et al (2011) Spinal neuronal NOS activation mediates sigma-1 receptor-induced mechanical and thermal hypersensitivity in mice: involvement of PKC-dependent GluN1 phosphorylation. Br J Pharmacol 163 1707 PMID: 21391983
Yoon et al (2009) Intrathecal injection of the neurosteroid, DHEAS, produces mechanical allodynia in mice: involvement of spinal sigma-1 and GABA receptors. Br J Pharmacol 157 666 PMID: 19422393
Shin et al (2005) The dextromethorphan analog dimemorfan attenuates kainate-induced seizures via sigma1 receptor activation: comparison with the effects of dextromethorphan. Br J Pharmacol 144 908 PMID: 15723099
Brown et al (2004) Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br J Pharmacol 141 233 PMID: 14691051
Cantarella et al (2007) Protective effects of the σ agonist Pre-084 in the rat retina. Korean J Physiol Pharmacol 91 1382 PMID: 17522150
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Effect of BD 1047 on viability of 661W cells.
By
Timur Mavlyutov on 02/04/2018
分析类型： In Vitro
种属： Mouse
细胞系/组织： 661W
MTT (cell viability assay) of 661W cultured cells. Cells were pretreated with sigma-1 receptor antagonist BD 1047. Results show that 100uM concentration of BD1047 significantly inhibited viability of this cell line.
