5-HT2C受体
药物发现
药理学
神经科学
受体
G蛋白偶联受体
兴奋剂
反激动剂
背景(考古学)
变构调节
抗抑郁药
5-羟色胺受体
变构调节剂
医学
生物
血清素
生物信息学
内科学
古生物学
海马体
作者
Eric A. Wold,Christopher Wild,Kathryn A. Cunningham,Jia Zhou
标识
DOI:10.2174/1568026619666190709101449
摘要
Serotonin (5-HT) 5-HT2C receptor (5-HT2CR) is recognized as a critical mediator of diseaserelated pathways and behaviors based upon actions in the central nervous system (CNS). Since 5-HT2CR is a class A G protein-coupled receptor (GPCR), drug discovery efforts have traditionally pursued the activation of the receptor through synthetic ligands with agonists proposed for the treatment of obesity, substance use disorders and impulse control disorders while antagonists may add value for the treatment of anxiety, depression and schizophrenia. The most significant agonist discovery to date is the FDAapproved anti-obesity medication lorcaserin. In recent years, efforts towards developing other mechanisms to enhance receptor function have resulted in the discovery of Positive Allosteric Modulators (PAMs) for the 5-HT2CR, with several molecule series now reported. The biological significance and context for signaling and function of the 5-HT2CR, and the current status of 5-HT2CR agonists and PAMs are discussed in this review.
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