BRL 44408 maleate
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. Also available as part of the α2-Adrenoceptor Tocriset™.
Sold with the permission of GlaxoSmithKline
|Storage||Desiccate at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 331.37. Batch specific molecular weights may vary from batch to batch due to solvent 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|
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 norepinephrine 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
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2 Citations for BRL 44408 maleate
Citations are publications that use Tocris products. Selected citations for BRL 44408 maleate include:
Rennekamp et al (2016) σ1 receptor ligands control a switch between passive and active threat responses. Nat Chem Biol 12 552 PMID: 27239788
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
Do you know of a great paper that uses BRL 44408 maleate from Tocris? Please let us know.
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Literature in this Area
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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.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
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.