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Submit ReviewBRL 44408 maleate
Description: Selective α2A antagonist
Chemical Name: 2-[(4,5-Dihydro-1H-imidazol-2-yl)methyl]-2,3-dihydro-1-methyl-1H-isoindole maleate
Purity: ≥98% (HPLC)
Biological Activity for BRL 44408 maleate
BRL 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.
Licensing Information
Sold with the permission of GlaxoSmithKline
Technical Data for BRL 44408 maleate
| M. Wt | 331.37 |
| Formula | C13H17N3.C4H4O4 |
| Storage | Desiccate at -20°C |
| Purity | ≥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 |
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.
Solubility Data for BRL 44408 maleate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 33.14 | 100 |
Preparing Stock Solutions for BRL 44408 maleate
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for BRL 44408 maleate
References for BRL 44408 maleate
References are publications that support the biological activity of the product.
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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2 Citations for BRL 44408 maleate
Citations are publications that use Tocris products. Selected citations for BRL 44408 maleate include:
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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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!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Depression Poster
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 Poster
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.