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Biological Activity for GR 231118
GR 231118 is a potent neuropeptide Y (NPY) Y1 receptor antagonist (pA2 = 10 and 10.5 at rY1 and hY1, receptors respectively). Also a potent and selective NPY Y4 receptor agonist (pEC50 values are 6.0, 8.6 and 6.1 for rY2, hY4 and rY5 receptors respectively). Suppresses food intake in rats in vivo. Also has affinity for neuropeptide FF (NPFF) receptors in vitro (Ki = 43-73 nM).
Technical Data for GR 231118
(Modifications: X = Dpr, Amide Bridge = 2 - 4*, 4 - 2*, Tyr-9 = C-terminal amide)
|Storage||Desiccate at -20°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.
References for GR 231118
References are publications that support the biological activity of the product.
Ishihara et al (1998) A potent neuropeptide Y antagonist, 1229U91, suppressed spontaneous food intake in Zucker fatty rats. Am.J.Physiol. 274 R1500 PMID: 9612420
Mollereau et al (2001) Agonist and antagonist activities on human NPFF2 receptors of the NPY ligands GR231118 and BIBP3226. Br.J.Pharmacol. 133 1 PMID: 11325787
Parker et al (1998) GR231118 (1229U91) and other analogues of the C-terminus of neuropeptide Y are potent neuropeptide Y Y1 receptor antagonists and neuropeptide Y Y4 receptor agonists. Eur.J.Pharmacol. 349 97 PMID: 9669502
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Keywords: GR 231118, GR 231118 supplier, NPFF, receptor, ligands, NPY, Y1, antagonists, Y4, agonists, Neuropeptide, FF, GR231118, npffr1, npffr2, npff1, npff2, GW1229, 1229, U91, neuropeptides, 1229U91, GW, Receptors, FF/AF, 1486, Tocris Bioscience
Citations for GR 231118
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Currently there are no citations for GR 231118.
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.