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Submit ReviewGR 231118
说明： Potent NPY Y1 antagonist/NPY Y4 agonist. Binds to NPFF receptors
别名： 1229U91,GW 1229
生物活性 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).
技术数据 for GR 231118
| 分子量 | 2352.77 |
| 公式 | C110H170N34O24 |
| 序列 |
IEPXYRLRY IEPXYRLRY* (Modifications: X = Dpr, Amide Bridge = 2 - 4*, 4 - 2*, Tyr-9 = C-terminal amide) |
| 储存 | Desiccate at -20°C |
| CAS Number | 158859-98-4 |
| PubChem ID | 24868178 |
| InChI Key | RJRBRCCJETZJLT-GSICZYLSSA-N |
| Smiles | [H]N[C@@H]([C@@H](C)CC)C(=O)N[C@H]1CCC(=O)NCC(NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCC(=O)NCC(NC(=O)[C@@H]2CCCN2C1=O)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(N)=O)NC(=O)[C@@H](N[H])[C@@H](C)CC)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(N)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for GR 231118
参考文献 for GR 231118
参考文献是支持产品生物活性的出版物。
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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关键词: 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
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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.