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Potent, selective 5-HT2C/2B receptor antagonist. pKi values are 6.4, 7.9 and 8.6 for 5-HT2A, 2B and 2C receptors respectively. Centrally active upon systemic administration in vivo.
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|Storage||Store at +4°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 353.36. 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||2.83 mL||14.15 mL||28.3 mL|
|5 mM||0.57 mL||2.83 mL||5.66 mL|
|10 mM||0.28 mL||1.41 mL||2.83 mL|
|50 mM||0.06 mL||0.28 mL||0.57 mL|
References are publications that support the biological activity of the product.
Bristow et al (2000) Evidence for accelerated desensitisation of 5-HT2C receptors following combined treatment with fluox. and the 5-HT1A receptor antagonist, WAY 100,635, in the rat. Neuropharmacology 39 1222 PMID: 10760364
Bromidge et al (1998) Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines. J.Med.Chem. 41 1598 PMID: 9572885
Hutson et al (2000) Activation of mesolimbic DA function by phencyclidine is enhanced by 5-HT2C/2B receptor antagonists: neurochemical and behavioural studies. Neuropharmacology 39 2318 PMID: 10974315
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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.