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Novel galanin receptor subtype specific ligands in feeding regulation.

机译:新的甘丙肽受体亚型的特定配体在进食调节中。

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摘要

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.
机译:甘丙肽29/30残基神经肽已参与中枢神经系统的多种功能,包括对食物消耗的调节。脑室内或脑下丘脑区域施用的甘丙肽及其类似物已显示出可靠而有力地刺激了啮齿类动物的食物消耗。已经分离出三种甘丙肽受体亚型,它们都存在于下丘脑中,但是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,我们介绍了几种新颖的GalR2选择性激动剂,然后将这些新颖的GalR2亚型选择性激动剂中最具有选择性的与已知的GalR1选择性激动剂M617进行了比较,因为它们具有刺激几种食品的急性消耗的能力,这些食物显示出可通过甘丙肽的中央给药来刺激。 GalR1选择性激动剂M617显着刺激了高脂牛奶的急性消耗,但GalR2选择性激动剂均未影响高脂牛奶或饼干糊的摄入。目前的结果与GalR1参与通过甘丙肽介导的急性进食消耗相一致,并提出了一种可用于探索甘丙肽受体在正常和异常行为以及生理学上的特异性的方法。

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