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Potent and selective α2D-adrenoceptor agonist (Ki values are 8.6 pM and 110 nM for rat α2D and α1 receptors respectively and 25, 26 and 100 nM for human α2A, α2C and α2B receptors respectively. Exhibits analgesic activity in a mouse model of abdominal irritation. Orally active.
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 346.4. 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||2.89 mL||14.43 mL||28.87 mL|
|5 mM||0.58 mL||2.89 mL||5.77 mL|
|10 mM||0.29 mL||1.44 mL||2.89 mL|
|50 mM||0.06 mL||0.29 mL||0.58 mL|
References are publications that support the biological activity of the product.
Ross et al (2000) α2 adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene as a high-affinity ligand for the α2D adrenergic receptor. J.Med.Chem. 43 1423 PMID: 10715142
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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.