Institute of Technology, University of Tartu, Tartu, Estonia.
Neurochem Int. 2011 May;58(6):714-20. doi: 10.1016/j.neuint.2011.02.012. Epub 2011 Feb 17.
Galanin a 29/30-residue neuropeptide has been implicated in several functions in the central nervous system, including the regulation of food consumption. Galanin and its analogues administered intraventricularly or into the hypothalamic region of brain have been shown to reliably and robustly stimulate the consumption of food in sated rodents. Three galanin receptor subtypes have been isolated, all present in the hypothalamus, but little is known about their specific role in mediating this acute feeding response. Presently, we introduce several novel GalR2 selective agonists and then compare the most selective of these novel GalR2 subtype selective agonists to known GalR1 selective agonist M617 for their ability to stimulate acute consumption of several foods shown to be stimulated by central administration of galanin. GalR1 selective agonist M617 markedly stimulated acute consumption of high-fat milk, but neither GalR2 selective agonist affected either high-fat milk or cookie mash intake. The present results are consistent with the involvement of GalR1 in mediating the acute feeding consumption by galanin and suggest an approach applicable to exploring galanin receptor specificity in normal and abnormal behavior and physiology.
甘丙肽是一种 29/30 个氨基酸残基的神经肽，已被证实参与了中枢神经系统的多种功能，包括食物消耗的调节。已经证明，甘丙肽及其类似物经脑室或脑下丘脑区域给药，可可靠且有效地刺激饱食啮齿动物的食物消耗。已经分离出三种甘丙肽受体亚型，它们都存在于下丘脑，但对于它们在介导这种急性摄食反应中的特定作用知之甚少。目前，我们引入了几种新型 GalR2 选择性激动剂，然后比较这些新型 GalR2 亚型选择性激动剂中最具选择性的激动剂与已知的 GalR1 选择性激动剂 M617，以研究它们刺激几种已被证明可被甘丙肽中枢给药刺激的食物急性消耗的能力。GalR1 选择性激动剂 M617 显著刺激高脂肪牛奶的急性消耗，但 GalR2 选择性激动剂均未影响高脂肪牛奶或曲奇糊的摄入。目前的结果与 GalR1 参与甘丙肽介导的急性摄食消耗一致，并为探索正常和异常行为和生理学中甘丙肽受体特异性提供了一种方法。
