title: Novel serotonin receptor 2 (5-HT2R) agonists and antagonists: a patent review (2004-2014).
abstract: BACKGROUND
  Serotonin or 5-hydroxytryptamine (5-HT) is a substance found in plasma, which increases smooth muscle contraction and mediates platelet aggregation. In addition, it is a monoamine neurotransmitter and is implicated in diverse behaviors. The serotonin receptor 2 (5-HT2) subfamily is best known for biased signaling and is strongly expressed mainly in the brain regions postulated to be involved in the modulation of higher cognitive and affective functions. Modulators of the 5-HT2 receptor are currently used to treat a variety of diseases including chronic pain and psychonosema. These properties suggest that 5-HT2 receptors may become an important therapeutic target for the treatment of various pathological conditions.
  
  
  METHODS
  This review highlights the significant progress that has been made in the discovery and development of 5-HT2 receptor agonists and antagonists based on an analysis of the patent literature between January 2004 and December 2014.
  
  
  CONCLUSIONS
  Cumulative evidence over the past decade supports the notion that the modulation of 5-HT2 receptors has a positive effect on human cognition and emotion. Therefore, we suggest that new agonists and antagonists may play an important role in the treatment of disorders such as schizophrenia, addiction and obesity.
authors.affiliation: a Faculty of Life Science and Technology , Kunming University of Science and Technology , Kunming , Yunnan 650500 , China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Yang
authors.affiliation: a Faculty of Life Science and Technology , Kunming University of Science and Technology , Kunming , Yunnan 650500 , China.
authors.forename: Shu
authors.initials: S
authors.lastname: An
authors.affiliation: a Faculty of Life Science and Technology , Kunming University of Science and Technology , Kunming , Yunnan 650500 , China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Liu
authors.affiliation: a Faculty of Life Science and Technology , Kunming University of Science and Technology , Kunming , Yunnan 650500 , China.
authors.forename: Xiao-Xi
authors.initials: XX
authors.lastname: Guo
authors.affiliation: a Faculty of Life Science and Technology , Kunming University of Science and Technology , Kunming , Yunnan 650500 , China.
authors.forename: Linghuan
authors.initials: L
authors.lastname: Gao
authors.affiliation: b Research Division of Clinical Pharmacology , The First Affiliated Hospital with Nanjing Medical University , 300 Guangzhou Road, Nanjing 210029 , China.
authors.forename: Ji-Fu
authors.initials: JF
authors.lastname: Wei
authors.affiliation: a Faculty of Life Science and Technology , Kunming University of Science and Technology , Kunming , Yunnan 650500 , China.
authors.forename: Tian-Rui
authors.initials: TR
authors.lastname: Xu
mesh_terms: D000818:Animals; D015195:Drug Design; D006801:Humans; D009765:Obesity / Q000188:drug therapy / Q000503:physiopathology; D010330:Patents as Topic; D044348:Receptors, Serotonin, 5-HT2 / Q000187:drug effects* / Q000378:metabolism; D012559:Schizophrenia / Q000188:drug therapy / Q000503:physiopathology; D012701:Serotonin / Q000378:metabolism; D058826:Serotonin 5-HT2 Receptor Agonists / Q000494:pharmacology / Q000627:therapeutic use*; D058830:Serotonin 5-HT2 Receptor Antagonists / Q000494:pharmacology / Q000627:therapeutic use*; D019966:Substance-Related Disorders / Q000188:drug therapy / Q000503:physiopathology
chemical_list: D044348:Receptors, Serotonin, 5-HT2; D058826:Serotonin 5-HT2 Receptor Agonists; D058830:Serotonin 5-HT2 Receptor Antagonists; D012701:Serotonin
keywords: agonists; antagonists; biased signaling; mental disorders; serotonin receptor 2