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.
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Chau, T., Walter, T., Zimmerman, J. et al. Analgesic activities of PEM-420, the active eutomer of pemedolac. Agents and Actions 39 (Suppl 1), C27–C29 (1993). https://doi.org/10.1007/BF01972710
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DOI: https://doi.org/10.1007/BF01972710