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Category: 7TM Receptorsarrow5-HT Receptorsarrow5-HT4 ReceptorsarrowAntagonists
Cat.No. Product Name
1658

GR 125487 sulfamate

Price and Availability

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GR 125487

Other Information:

Sold for research purposes under agreement from GlaxoSmithKline
Chemical Name: 5-Fluoro-2-methoxy-[1-[2-[(methylsulfonyl)amino]ethyl]- 4-piperidinyl]-1H-indole-3-methylcarboxylate sulfamate

Biological Activity:

Potent and selective 5-HT4 receptor antagonist (Ki = 0.19 nM for porcine 5-HT4). Centrally active following systemic administration in vivo.

Technical Data:

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M.Wt: 524.58
Formula: C19H26FN3O5S.H2NSO3H
Storage: Desiccate at RT
Solubility: Soluble to 10 mM in Water
Purity: >99%
CAS No: [144625-67-2]

Resources:

  • Certificate of Analysis / MSDS:

    Certificate of Analysis: View current batch
    Product/Material Safety Data Sheet: View current batch

    References:

    Schiavi et al (1994) Identification of serotonin 5-HT4 recognition sites in the porcine caudate nucleus by radioligand binding. Neuropharmacology 33 543. Galeotti et al (1998) Role of 5-HT4 receptors in the mouse passive avoidance test. J.Pharmacol.Exp.Ther. 286 1115. 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.
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    Keywords: GR 125487, 5-HT Receptors, Potent, Selective 5-HT4 Antagonist. Active In Vivo, GR125487, Tocris Bioscience

    Literature in this Area
    Scientific Reviews
    5-HT Receptors & their Ligands
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