GR231118(Synonyms: 1229U91 GW1229)

发表于由

GR231118;(Synonyms: 1229U91; GW1229)

GR231118 是神经肽Y 的 C 末端的类似物，对人神经肽 Y Y 受体具有较强的竞争性和相对选择性拮抗剂，其拮抗剂的 pKi 为10.4。GR231118 是人类神经肽 Y4 受体 (pEC50=8.6; pKi=9.6) 和对人及大鼠神经肽 YY2 和 Y5 受体的弱激动剂。GR231118 对小鼠神经肽 YY6 受体也有较高亲和力 (pKi= 8.8)。

GR231118amp;;(Synonyms: 1229U91; GW1229)

GR231118 Chemical Structure

CAS No. : 158859-98-4

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生物活性

GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8)[1].

分子量

2352.74

Formula

C110H170N34O24
CAS 号

158859-98-4
Sequence Shortening

Sequence 1:IEP-{Dpr}-YRLRY-NH2;Sequence 1′:IEP-{Dpr}-YRLRY-NH2 (Amide bridge:Glu2-Dpr4′;Dpr4-Glu2′)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. E M Parker, et al. 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

    [2]. Y Dumont, et al. [(125)I]-GR231118: a high affinity radioligand to investigate neuropeptide Y Y(1) and Y(4) receptors. Br J Pharmacol. 2000 Jan;129(1):37-46.