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Glemanserin

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Glemanserin
Clinical data
Other namesMDL-11,939; MDL-11939; MDL11939
Routes of
administration
Oral[1]
Drug classSerotonin 5-HT2A receptor antagonist
ATC code
  • None
Identifiers
  • α-phenyl-1-(2-phenylethyl)-4-piperidine methanol
CAS Number
PubChemCID
ChemSpider
UNII
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC20H25NO
Molar mass295.426 g·mol−1
3D model (JSmol)
  • OC(c1ccccc1)C3CCN(CCc2ccccc2)CC3
  • InChI=1S/C20H25NO/c22-20(18-9-5-2-6-10-18)19-12-15-21(16-13-19)14-11-17-7-3-1-4-8-17/h1-10,19-20,22H,11-16H2
  • Key:AXNGJCOYCMDPQG-UHFFFAOYSA-N

Glemanserin (INNTooltip International Nonproprietary Name; developmental codeMDL-11,939) is adrug which acts as apotent andselective5-HT2A receptorantagonist .[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selective 5-HT2A receptor antagonistvolinanserin (MDL-100,907), which is afluorinatedanalogue.[3] Though it was largely superseded inscientific research by volinanserin, glemanserin was investigatedclinically for the treatment ofgeneralized anxiety disorder and reachedphase 3 trials for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 ofcardiac arrhythmias, but was not marketed for this use either.[1]

See also

[edit]

References

[edit]
  1. ^abcde"Glemanserin".AdisInsight. 4 April 1995. Retrieved16 January 2026.
  2. ^Dudley MW, Wiech NL, Miller FP, Carr AA, Cheng HC, Roebel LE, et al. (1988). "Pharmacological effects of MDL 11,939: A selective, centrally acting antagonist of 5-HT2 receptors".Drug Development Research.13 (1):29–43.doi:10.1002/ddr.430130104.S2CID 85075328.
  3. ^van Wijngaarden I, Soudijn W (10 July 1997)."5-HT2A, 5-HT2B, and 5-HT2C Receptor Ligands". In Olivier B (ed.).Serotonin Receptors and Their Ligands. Elsevier. p. 167.ISBN 978-0-444-82041-9. Retrieved6 May 2012.
  4. ^abSramek JJ, Robinson RE, Suri A, Cutler NR (February 1995). "Efficacy trial of the 5-HT2 antagonist MDL 11,939 in patients with generalized anxiety disorder".Journal of Clinical Psychopharmacology.15 (1):20–22.doi:10.1097/00004714-199502000-00004.PMID 7714223.
  5. ^Sramek JJ, Zarotsky V, Cutler NR (2002). "Generalised anxiety disorder: treatment options".Drugs.62 (11):1635–1648.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]
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT37
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
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