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R 1485 dihydrochloride
Selective and high affinity 5-HT6 antagonist (pKi = 8.9); displays low hERG inhibition. Exhibits >100 fold selectivity against a panel of 50 targets including other 5-HT receptor subtypes. Brain penetrant.
|Storage||Store at -20°C|
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 450.35. 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||2.22 mL||11.1 mL||22.2 mL|
|5 mM||0.44 mL||2.22 mL||4.44 mL|
|10 mM||0.22 mL||1.11 mL||2.22 mL|
|50 mM||0.04 mL||0.22 mL||0.44 mL|
References are publications that support the biological activity of the product.
Zhao et al (2007) 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives as 5-HT6 receptor antagonists. Bioorg.Med.Chem.Lett. 17 3504 PMID: 17485206
Liu et al (2009) 5-HT6 antagonists as potential treatment for cognitive dysfunction. Drug Des.Rev. 70 145
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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.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.