GR 125487 sulfamate
Potent and selective 5-HT4 receptor antagonist (Ki = 0.19 nM for porcine 5-HT4). Centrally active following systemic administration in vivo.
Sold for research purposes under agreement from GlaxoSmithKline
|Storage||Desiccate at RT|
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|
|water||4.27||10mM with gentle warming|
|phosphate buffered saline||2.14||5mM with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 524.58. 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||1.91 mL||9.53 mL||19.06 mL|
|5 mM||0.38 mL||1.91 mL||3.81 mL|
|10 mM||0.19 mL||0.95 mL||1.91 mL|
|50 mM||0.04 mL||0.19 mL||0.38 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
Galeotti et al (1998) Role of 5-HT4 receptors in the mouse passive avoidance test. J.Pharmacol.Exp.Ther. 286 1115 PMID: 9732367
Horikoshi et al (2001) Possible involvement of 5-HT4 receptors, in addition to 5-HT3 receptors, in the emesis induced by high-dose cisplatin in Suncus murinus. Jpn.J.Pharmacol. 85 70 PMID: 11243577
Schiavi et al (1994) Identification of serotonin 5-HT4 recognition sites in the porcine caudate nucleus by radioligand binding. Neuropharmacology 33 543 PMID: 7984293
If you know of a relevant reference for GR 125487 sulfamate, please let us know.
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2 Citations for GR 125487 sulfamate
Citations are publications that use Tocris products. Selected citations for GR 125487 sulfamate include:
Warner-Schmidt et al (2009) Role of p11 in cellular and behavioral effects of 5-HT4 receptor stimulation. Dis Model Mech 29 1937 PMID: 19211900
Orr et al (2015) Astrocytic adenosine receptor A2A and Gs-coupled signaling regulate memory. J Neurosci 18 423 PMID: 25622143
Do you know of a great paper that uses GR 125487 sulfamate from Tocris? If so please let us know.
Literature in this Area
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.