Ligands of the neuropeptide Y Y2 receptor

被引:25
|
作者
Mittapalli, Gopi Kumar [1 ]
Roberts, Edward [1 ]
机构
[1] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
关键词
Neuropeptide Y; Y2; receptor; Antagonists; Agonists; Structure-activity relationships; Brain-penetration; Non-peptidic; SMALL-MOLECULE ANTAGONIST; YY2; RECEPTOR; Y-2; FOOD-INTAKE; KNOCKOUT MICE; ANTIOBESITY DRUGS; PEPTIDE AGONISTS; BODY-WEIGHT; NPY; BIIE0246;
D O I
10.1016/j.bmcl.2013.11.061
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Neuropeptide Y (NPY) is one of the most abundant neuropeptides in the mammalian brain and exerts a variety of physiological processes in humans via four different receptor subtypes Y1, Y2, Y4 and Y5. Y2 receptor is the most abundant Y subtype receptor in the central nervous system and implicated with food intake, bone formation, affective disorders, alcohol and drugs of abuse, epilepsy, pain, and cancer. The lack of small molecule non-peptidic Y2 receptor modulators suitable as in vivo pharmacological tools hampered the progress to uncover the precise pharmacological role of Y2. Only in recent years, several potent, selective and non-peptidic Y2 antagonists have been discovered providing the tools to validate Y2 receptor as a therapeutic target. This Letter reviews Y2 receptor modulators mainly non-peptidic antagonists and their structure-activity relationships. (C) 2013 The Authors. Published by Elsevier Ltd. All rights reserved.
引用
收藏
页码:430 / 441
页数:12
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