Chemistry:Glemanserin

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Glemanserin (INN; developmental code MDL-11,939) is a drug which acts as a potent and selective 5-HT2A receptor antagonist .[1][2] The first truly selective 5-HT2A ligand to be discovered, glemanserin resulted in the development of the widely used and even more potent and selective 5-HT2A receptor antagonist volinanserin (MDL-100,907), which is a fluorinated analogue.[3] Though it was largely superseded in scientific research by volinanserin, glemanserin was investigated clinically for the treatment of generalized anxiety disorder and reached phase 3 trials for this use.[1][4] However, it was ultimately found to be ineffective and was not marketed.[1][4][5] The drug was also investigated for treatment of cardiac arrhythmias, but was not marketed for this use either.[1]

See also

References

  1. 1.0 1.1 1.2 1.3 "Glemanserin". 4 April 1995. https://adisinsight.springer.com/drugs/800000314. 
  2. "Pharmacological effects of MDL 11,939: A selective, centrally acting antagonist of 5-HT2 receptors". Drug Development Research 13 (1): 29–43. 1988. doi:10.1002/ddr.430130104. 
  3. "5-HT2A, 5-HT2B, and 5-HT2C Receptor Ligands". Serotonin Receptors and Their Ligands. Elsevier. 10 July 1997. p. 167. ISBN 978-0-444-82041-9. https://books.google.com/books?id=lfo0hGqIex0C&pg=PA167. Retrieved 6 May 2012. 
  4. 4.0 4.1 "Efficacy trial of the 5-HT2 antagonist MDL 11,939 in patients with generalized anxiety disorder". Journal of Clinical Psychopharmacology 15 (1): 20–22. February 1995. doi:10.1097/00004714-199502000-00004. PMID 7714223. 
  5. "Generalised anxiety disorder: treatment options". Drugs 62 (11): 1635–1648. 2002. doi:10.2165/00003495-200262110-00005. PMID 12109925. "Another 5-HT2–receptor antagonist glemanserin (MDL-11939) was evaluated against placebo in 72 male patients with GAD (DSM III-R criteria). Although all measures showed trends favouring glemanserin, no significant changes from baseline compared with placebo were observed.[94]".