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Submit ReviewGR 125487 sulfamate
Description: Potent and selective 5-HT4 antagonist; active in vivo
Chemical Name: 5-Fluoro-2-methoxy-[1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]-1H-indole-3-methylcarboxylate sulfamate
Purity: ≥97% (HPLC)
Biological Activity for GR 125487 sulfamate
GR 125487 sulfamate is a potent and selective 5-HT4 receptor antagonist (Ki = 0.19 nM for porcine 5-HT4). Centrally active following systemic administration in vivo.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Technical Data for GR 125487 sulfamate
| M. Wt | 524.58 |
| Formula | C19H26FN3O5S.H2NSO3H |
| Storage | Desiccate at RT |
| Purity | ≥97% (HPLC) |
| CAS Number | 859502-43-5 |
| PubChem ID | 6604955 |
| InChI Key | VQJFDBXITIOGJM-UHFFFAOYSA-N |
| Smiles | NS(O)(=O)=O.COC1=C(C(=O)OCC2CCN(CCNS(C)(=O)=O)CC2)C2=CC(F)=CC=C2N1 |
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.
Solubility Data for GR 125487 sulfamate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 4.27 | 10 with gentle warming |
Preparing Stock Solutions for GR 125487 sulfamate
The following data is based on the product molecular weight 524.58. 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 |
|---|---|---|---|
| 0.1 mM | 19.06 mL | 95.31 mL | 190.63 mL |
| 0.5 mM | 3.81 mL | 19.06 mL | 38.13 mL |
| 1 mM | 1.91 mL | 9.53 mL | 19.06 mL |
| 5 mM | 0.38 mL | 1.91 mL | 3.81 mL |
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Product Datasheets for GR 125487 sulfamate
References for GR 125487 sulfamate
References are publications that support the biological activity of the product.
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 cisp. 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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Keywords: GR 125487 sulfamate, GR 125487 sulfamate supplier, Potent, selective, 5-HT4, antagonists, Serotonin, Receptors, 5-Hydroxytryptamine, GR125487, sulfamate, GlaxoSmithKline, GSK, 1658, Tocris Bioscience
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? Please let us know.
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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.
Depression Poster
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.