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Submit ReviewBRL 44408 maleate is a selective α2A-adrenoceptor antagonist (Ki = 1.7 nM and 144.5 nM at α2A and α2B-adrenergic receptors respectively). Increases hippocampal noradrenalin release following systemic administration.
Sold with the permission of GlaxoSmithKline
分子量 | 331.37 |
公式 | C13H17N3.C4H4O4 |
储存 | Desiccate at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 681806-46-2 |
PubChem ID | 10382026 |
InChI Key | DDIQGSUEJOOQQQ-BTJKTKAUSA-N |
Smiles | OC(=O)\C=C/C(O)=O.CC1N(CC2=NCCN2)CC2=C1C=CC=C2 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 33.14 | 100 |
以下数据基于产品分子量 331.37。 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 |
---|---|---|---|
1 mM | 3.02 mL | 15.09 mL | 30.18 mL |
5 mM | 0.6 mL | 3.02 mL | 6.04 mL |
10 mM | 0.3 mL | 1.51 mL | 3.02 mL |
50 mM | 0.06 mL | 0.3 mL | 0.6 mL |
参考文献是支持产品生物活性的出版物。
Callado et al (1999) α2A-But not α2B/C-adrenoceptors modulate noradrenaline release in rat locus coeruleus: voltammetric data. Eur.J.Pharmacol. 366 35 PMID: 10064149
Gavin et al (1997) α2C-adrenoceptors mediate contractile responses to noradrenaline in the human saphenous vein. Naunyn Schmiedebergs Arch.Pharmacol. 355 406 PMID: 9089673
Kiss et al (1995) Subtype-specificity of the presynaptic α2-adrenoceptors modulating hippocampal NE release in rat. Brain Res. 674 238 PMID: 7796102
Young et al (1989) Novel α2-adrenoceptor antagonists show selectivity for α2A- and α2B-adrenoceptor subtypes. Eur.J.Pharmacol. 168 381 PMID: 2573535
If you know of a relevant reference for BRL 44408 maleate, please let us know.
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引用文献是使用了 Tocris 产品的出版物。 BRL 44408 maleate 的部分引用包括:
Backman et al (2013) Alpha-2 adrenergic stimulation triggers Achilles tenocyte hypercellularity: Comparison between two model systems. Scand J Med Sci Sports 23 687 PMID: 22292987
Rennekamp et al (2016) σ1 receptor ligands control a switch between passive and active threat responses. Nat Chem Biol 12 552 PMID: 27239788
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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!
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
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.