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Metrenperone

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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
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.072.413 Edit 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 name R-50970) is a serotonin 5-HT2 receptor antagonist which was never marketed.[1][2] The drug also shows lower affinity for the α1-adrenergic and histamine H1 receptor and much lower affinity for the dopamine D2 receptor, but no affinity for the serotonin 5-HT1 and muscarinic acetylcholine receptors.[2] It is a weak antagonist of the α1-adrenergic receptor in addition to its potent serotonin 5-HT2A receptor antagonism.[3] Metrenperone has been investigated for use in veterinary medicine to treat acute respiratory distress in cattle and has also been studied for topical treatment of wounds as well as injuries.[1][4][5] It was first described in the scientific literature by 1982.[2]

See also

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References

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  1. 1 2 Morton 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. Retrieved 17 January 2026.
  2. 1 2 3 Janssen 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. Retrieved 17 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. Retrieved 17 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.
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