Chau T, Walter T, Zimmerman J, Hartman D, Ochalski S, Weichman B
Wyeth-Ayerst Research, Princeton, NJ 08543-8000.
Agents Actions. 1993;39 Spec No:C27-9. doi: 10.1007/BF01972710.
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.
培美洛酸的活性异构体PEM - 420抑制苯醌（PBQ）、乙酸和乙酰胆碱诱导的小鼠扭体反应，其口服半数有效剂量（ED50）分别为0.80、0.92和0.075mg/kg。在大鼠乙酸扭体试验中，PEM - 420口服半数有效剂量（ED50）值为8.4mg/kg。在兰德尔 - 塞利托试验中，PEM - 420提高了注射酵母爪的痛阈（口服半数有效剂量（ED50）= 0.55mg/kg）。与其他非甾体抗炎药一样，PEM - 420抑制PBQ诱导的小鼠腹腔中前列环素（PGI2）和前列腺素E2（PGE2）的产生，口服半数有效剂量（ED50）值分别为0.5和1.2mg/kg。它在大鼠中致溃疡作用较弱（禁食大鼠急性口服半数溃疡剂量（UD50）= 99mg/kg；喂食大鼠亚急性口服半数溃疡剂量（UD50）= 74mg/kg/天，持续4天）。数据表明PEM - 420是一种强效且安全的外周镇痛药。
