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Potent and selective 5-HT2C agonist (EC50 = 10 nM). Exhibits > 100-fold selectivity over a panel of 90 receptors, enzymes and ion channels, except for 5-HT2A (IC50 = 360 nM antagonist), 5-HT2B (EC50 = 67 nM antagonist), 5-HT1A and 5-HT6 (functional activity not tested).
Sold for research purposes under agreement from Pfizer Inc.
|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 282.39. 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||3.54 mL||17.71 mL||35.41 mL|
|5 mM||0.71 mL||3.54 mL||7.08 mL|
|10 mM||0.35 mL||1.77 mL||3.54 mL|
|50 mM||0.07 mL||0.35 mL||0.71 mL|
References are publications that support the biological activity of the product.
Storer et al (2014) Multiparameter optimization in CNS drug discovery: Design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT2C) receptor agonists with exquisite functional selectivity over 5-HT2A and 5-HT2B receptors. J.Med.Chem. 57 5258 PMID: 24878222
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Keywords: PF 04479745, PF 04479745 supplier, PF04479745, potent, selective, 5-hydroxytryptamine, 2C, 5-HT2C, agonists, agonism, Receptors, 5755, Tocris Bioscience
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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.
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.