Wacker Dean A, Miller Keith J
Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543, USA.
Curr Opin Drug Discov Devel. 2008 Jul;11(4):438-45.
The serotonin 5-HT2C receptor is a G-protein-coupled receptor and is one of the 14 subtypes that constitutes the serotonin receptor family. Agonists of 5-HT2C have been implicated as potential treatments for diseases of significant unmet medical need, including obesity and schizophrenia. Despite approximately 10 years of discovery efforts, 5-HT2C agonists have only recently advanced into the clinic, likely because many of the early drug discovery efforts experienced significant difficulties with attaining receptor selectivity. Several of these issues related to receptor selectivity have now been overcome, resulting in the entry of compounds into advanced clinical trials. This review summarizes the progress in 5-HT2C agonist discovery and clinical development over the last 3 years. [sw1]what are the several issues - several issues relating to receptor selectivity?
血清素5-HT2C受体是一种G蛋白偶联受体，是构成血清素受体家族的14种亚型之一。5-HT2C激动剂已被认为是治疗包括肥胖症和精神分裂症在内的重大未满足医疗需求疾病的潜在药物。尽管经过了大约10年的研发努力，但5-HT2C激动剂直到最近才进入临床，这可能是因为许多早期药物研发工作在实现受体选择性方面遇到了重大困难。现在，其中一些与受体选择性相关的问题已经得到克服，使得化合物进入了晚期临床试验。本综述总结了过去3年中5-HT2C激动剂研发和临床开发的进展。[sw1]几个问题是什么——与受体选择性相关的几个问题？
