5-HT2C receptor agonist

5-HT2C receptor agonists are a class of drugs that activate 5-HT2C receptors. They have been investigated for the treatment of a number of conditions including obesity, psychiatric disorders, sexual dysfunction and urinary incontinence.[1][2][3][4][5]

The 5-HT2C receptors are one of three subtypes that belong to the serotonin 5-HT2 receptor subfamily along with 5-HT2A and 5-HT2B receptors. The development of 5-HT2C agonists has been a major obstacle, because of severe side effects due to a lack of selectivity over 5-HT2A and 5-HT2B receptors. Activation of 5-HT2A receptors can induce hallucinations, and the activation of 5-HT2B receptors has been implicated in cardiac valvular insufficiency and possibly in pulmonary hypertension.[6][7]

  1. ^ Wacker, DA; Miller, KJ (2008). "Agonists of the serotonin 5-HT2C receptor: Preclinical and clinical progression in multiple diseases". Current Opinion in Drug Discovery & Development. 11 (4): 438–45. PMID 18600561.
  2. ^ Cryan, John F.; Lucki, Irwin (2000). "Antidepressant-Like Behavioral Effects Mediated by 5-Hydroxytryptamine2C Receptors". The Journal of Pharmacology and Experimental Therapeutics. 295 (3): 1120–6. PMID 11082448.
  3. ^ Tsui, Marco M.; York, John D. (2010). "Roles of inositol phosphates and inositol pyrophosphates in development, cell signaling and nuclear processes". Advances in Enzyme Regulation. 50 (1): 324–37. doi:10.1016/j.advenzreg.2009.12.002. PMC 3269838. PMID 20006638.
  4. ^ Leopoldo, Marcello; Lacivita, Enza; De Giorgio, Paola; Berardi, Francesco; Perrone, Roberto (2011). "The Medicinal Chemistry of 5-HT2C Receptor Ligands". 5-HT2C Receptors in the Pathophysiology of CNS Disease. Totowa, NJ: Humana Press. pp. 29–50. doi:10.1007/978-1-60761-941-3_3. ISBN 978-1-60761-940-6.
  5. ^ Yang, Yang; An, Shu; Liu, Ying; Guo, Xiao-Xi; Gao, Linghuan; Wei, Ji-Fu; Xu, Tian-Rui (2016). "Novel serotonin receptor 2 (5-HT2R) agonists and antagonists: a patent review (2004-2014)". Expert Opinion on Therapeutic Patents. 26 (1): 89–106. doi:10.1517/13543776.2016.1113257. ISSN 1744-7674. PMID 26609882. S2CID 10831801.
  6. ^ Wang, Yu; Bai, Y (2010). "The use of lorcaserin in the management of obesity: A critical appraisal". Drug Design, Development and Therapy. 5: 1–7. doi:10.2147/Dddt.S11945. PMC 3023275. PMID 21267355.
  7. ^ Thomsen, W. J.; Grottick, A. J.; Menzaghi, F.; Reyes-Saldana, H.; Espitia, S.; Yuskin, D.; Whelan, K.; Martin, M.; Morgan, M.; Chen, W.; Al-Shamma, H.; Smith, B.; Chalmers, D.; Behan, D. (2008). "Lorcaserin, a Novel Selective Human 5-Hydroxytryptamine2C Agonist: in Vitro and in Vivo Pharmacological Characterization". Journal of Pharmacology and Experimental Therapeutics. 325 (2): 577–587. doi:10.1124/jpet.107.133348. PMID 18252809. S2CID 20924745.