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Identification and Characterisation of Novel Positive AUosteric Modulators of the Peptide GPCR Galanin Receptor 2

机译:肽GPCR甘硫蛋白受体2的新型阳性阳性阳离子剂调节剂的鉴定与表征

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摘要

Galanin is a 30 amino acid neuropeptide widely expressed in the brain, spinal cord and gut. The physiological effects of galanin are mediated by activation of three G-protein coupled receptors GalR1, GalR2 and GalR3. The physiological effects of galanin are predominantly attributed to inhibition of adenylyl cyclase (GalRl) and intracellular calcium mobilisation (GalR2). Truncation of the native peptide is known to confer receptor subtype selectivity.
机译:环肽是在脑,脊髓和肠道中广泛表达的30个氨基酸神经肽。 通过激活三种G蛋白偶联受体Galr1,Galr2和Galr3来介导的Galanin的生理效果。 环肽的生理效果主要归因于腺苷酸环酶(GALRL)和细胞内钙动员(GALR2)的抑制作用。 已知原生肽的截短赋予受体亚型选择性。

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