We Need 2C but Not 2B: Developing Serotonin 2C (5-HT2C) Receptor Agonists for the Treatment of CNS Disorders.
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.
Drug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA.
Jianjun
J
Cheng
Drug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA. kozikowa@uic.edu.
Alan P
AP
Kozikowski
D000588:Amines / Q000737:chemistry* / Q000627:therapeutic use; D002493:Central Nervous System Diseases / Q000188:drug therapy / Q000473:pathology; D006801:Humans; D044405:Receptor, Serotonin, 5-HT2C / Q000737:chemistry* / Q000378:metabolism; D058826:Serotonin 5-HT2 Receptor Agonists / Q000737:chemistry* / Q000627:therapeutic use; D054852:Small Molecule Libraries / Q000737:chemistry; D013329:Structure-Activity Relationship
D000588:Amines; D044405:Receptor, Serotonin, 5-HT2C; D058826:Serotonin 5-HT2 Receptor Agonists; D054852:Small Molecule Libraries
drug discovery; medicinal chemistry; receptors; schizophrenia; serotonin