Agents and Actions

, Volume 39, Supplement 1, pp C27–C29

Analgesic activities of PEM-420, the active eutomer of pemedolac

  • T. Chau
  • T. Walter
  • J. Zimmerman
  • D. Hartman
  • S. Ochalski
  • B. Weichman
Drugs and Lipid Mediators

DOI: 10.1007/BF01972710

Cite this article as:
Chau, T., Walter, T., Zimmerman, J. et al. Agents and Actions (1993) 39(Suppl 1): C27. doi:10.1007/BF01972710

Abstract

PEM-420, the active isomer of pemedolac, inhibited the writhing responses induced by phenylbenzoquinone (PBQ), acetic acid, and acetylcholine in mice with ED50's of 0.80, 0.92, and 0.075 mg/kg p.o., respectively. In the rat acetic acid writhing assay, PEM-420 exhibited an ED50 value of 8.4 mg/kg p.o. In the Randall-Selitto test, PEM-420 raised the pain threshold of the yeast-injected paw (ED50-0.55 mg/kg p.o.). Like other NSAIDs, PEM-420 inhibited the PBQ-induced production of PGI2 and PGE2 in the mouse peritoneal cavity, with ED50 values of 0.5 and 1.2 mg/kg p.o., respectively. It had weak ulcerogenic liability in rats (acute UD50=99 mg/kg p.o. in fasted rats; subacute UD50=74 mg/kg/day for 4 days in fed rats). The data indicate that PEM-420 is a potent and safe peripheral analgesic.

Copyright information

© Birkhäuser Verlag 1993

Authors and Affiliations

  • T. Chau
    • 1
  • T. Walter
    • 1
  • J. Zimmerman
    • 1
  • D. Hartman
    • 1
  • S. Ochalski
    • 1
  • B. Weichman
    • 1
  1. 1.Wyeth-Ayerst Research, CN 8000PrincetonUSA