We Need 2C but Not 2B: Developing Serotonin 2C (5-HT2C) Receptor Agonists for the Treatment of CNS Disorders.
We Need 2C but Not 2B: Developing Serotonin 2C (5-HT2C) Receptor Agonists for the Treatment of CNS Disorders.
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DOI：
10.1002/cmdc.201500437
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发表时间：
2015-12
期刊：
影响因子：
3.4
通讯作者：
Kozikowski AP
中科院分区：
文献类型：
--
作者：
Cheng J;Kozikowski AP
5-羟色胺2C(5-HT2C)受体已被确定为治疗多种中枢神经系统(CNS)疾病的潜在药物靶点，如肥胖、药物滥用和精神分裂症。在这篇观点文章中，总结了在开发用于治疗这些疾病的选择性5-HT2C激动剂方面的最新进展，包括我们小组的工作。描述了这一领域面临的挑战和未来可能的发展方向。本文还讨论了用同源模型预测5-HT2C配体与受体结合方式的方法。与已知的配体相比，基于2-苯基环丙基甲胺的5-HT2C激动剂的药理特征使其成为进一步研究的首选对象。
The serotonin 2C (5-HT2C) receptor has been identified as a potential drug target for the treatment of a variety of central nervous system (CNS) disorders, such as obesity, substance abuse, and schizophrenia. In this Viewpoint article, recent progress in developing selective 5-HT2C agonists for use in treating these disorders is summarized, including the work of our group. Challenges in this field and the possible future directions are described. Homology modeling as a method to predict the binding modes of 5-HT2C ligands to the receptor is also discussed. Compared to known ligands, the improved pharmacological profiles of the 2-phenylcyclopropylmethylamine-based 5-HT2C agonists make them preferred candidates for further studies.