Catalog Number: 1658
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
  • M.Wt:
    524.58
  • Formula:
    C19H26FN3O5S.H2NSO3H
  • Solubility:
    Soluble to 10 mM in water with gentle warming
  • Purity:
    >97%
  • Storage:
    Desiccate at RT
  • CAS No:
    859502-43-5
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.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline
Background References
  1. Possible involvement of 5-HT4 receptors, in addition to 5-HT3 receptors, in the emesis induced by high-dose cisplatin in Suncus murinus.
    Horikoshi et al.
    Jpn.J.Pharmacol., 2001;85:70
  2. Role of 5-HT4 receptors in the mouse passive avoidance test.
    Galeotti et al.
    J.Pharmacol.Exp.Ther., 1998;286:1115
  3. Identification of serotonin 5-HT4 recognition sites in the porcine caudate nucleus by radioligand binding.
    Schiavi et al.
    Neuropharmacology, 1994;33:543
Citations:

The citations listed below are publications that use Tocris products. Selected citations for GR 125487 sulfamate include:

2 Citations: Showing 1 - 2
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  1. Astrocytic adenosine receptor A2A and Gs-coupled signaling regulate memory.
    Authors: Orr Et al.
    J Neurosci 2015;18:423
  2. Role of p11 in cellular and behavioral effects of 5-HT4 receptor stimulation.
    Authors: Warner-Schmidt Et al.
    Dis Model Mech 2009;29:1937

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