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Metrenperone

From Wikipedia, the free encyclopedia

Pharmaceutical compound
Metrenperone
Clinical data
Other namesR-50970; R50970; R-50,970
Drug classSerotonin 5-HT2A receptor antagonist
ATC code
  • None
Identifiers
  • 3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-2,7-dimethylpyrido[1,2-a]pyrimidin-4-one
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard100.072.413Edit this at Wikidata
Chemical and physical data
FormulaC24H26FN3O2
Molar mass407.489 g·mol−1
3D model (JSmol)
  • CC1=CN2C(=NC(=C(C2=O)CCN3CCC(CC3)C(=O)C4=CC=C(C=C4)F)C)C=C1
  • InChI=1S/C24H26FN3O2/c1-16-3-8-22-26-17(2)21(24(30)28(22)15-16)11-14-27-12-9-19(10-13-27)23(29)18-4-6-20(25)7-5-18/h3-8,15,19H,9-14H2,1-2H3
  • Key:AXQRPYKSPHUOGZ-UHFFFAOYSA-N

Metrenperone (INNTooltip International Nonproprietary Name,USANTooltip United States Adopted Name,BANTooltip British Approved Name; developmental code nameR-50970) is aserotonin5-HT2 receptorantagonist which was never marketed.[1][2] The drug also shows loweraffinity for theα1-adrenergic andhistamineH1 receptor and much lower affinity for thedopamineD2 receptor, but no affinity for the serotonin5-HT1 andmuscarinic acetylcholine receptors.[2] It is a weak antagonist of the α1-adrenergic receptor in addition to itspotent serotonin 5-HT2A receptor antagonism.[3] Metrenperone has been investigated for use inveterinary medicine to treat acuterespiratory distress in cattle and has also been studied fortopical treatment ofwounds as well asinjuries.[1][4][5] It was first described in thescientific literature by 1982.[2]

See also

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References

[edit]
  1. ^abMorton DI, Morton IK, Hall JM, Hall DJ (31 October 1999).Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media.ISBN 978-0-7514-0499-9. Retrieved17 January 2026.
  2. ^abcJanssen P (1982). "The Pharmacology of Specific, Pure and Potent Serotonin 5-HT2 or S2-Antagonists".Biochemical Immunological Pharmacology. Elsevier. pp. 21–33.doi:10.1016/b978-0-08-028024-0.50006-2.ISBN 978-0-08-028024-0. Retrieved17 January 2026.
  3. ^Ooms LA, Degryse AA, Fransen JL, van Mol KA (1986)."Treatment of chronic myopathies in horses with the serotonin S 2 -antagonist R 50970: A preclinical study".Drug Development Research.8 (1–4):219–224.doi:10.1002/ddr.430080126.ISSN 0272-4391. Retrieved17 January 2026.
  4. ^Linden A, Desmecht D, Amory H, Lekeux P (January 1999). "Cardiovascular response to intravenous administration of 5-hydroxytryptamine after type-2 receptor blockade, by metrenperone, in healthy calves".Veterinary Journal.157 (1):31–37.doi:10.1053/tvjl.1998.0250.PMID 10030126.
  5. ^Oryan A, Silver IA, Goodship AE (2009). "Effects of a serotonin S2-receptor blocker on healing of acute and chronic tendon injuries".Journal of Investigative Surgery.22 (4):246–255.doi:10.1080/08941930903040114.PMID 19842899.
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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