前列腺素拮抗剂在大鼠体内的抗伤害感受作用。

The antinociceptive effects of prostaglandin antagonists in the rat.

作者信息

Drower E J, Stapelfeld A, Mueller R A, Hammond D L

出版信息

Eur J Pharmacol. 1987 Jan 20;133(3):249-56. doi: 10.1016/0014-2999(87)90020-3.

Abstract

This study examined the antinociceptive effects of two prostaglandin antagonists, SC-25469 and SC-19220 in the rat. SC-25469 and SC-19220 inhibited acetic acid-induced writhing with ED50 s of 6.9 and 6.8 mg/kg p.o., respectively. When compared to other analgesics, the rank order of potency in the writhing test was morphine greater than pentazocine = U-50,488 greater than SC-25469 = SC-19220 greater than ibuprofen greater than aspirin greater than acetaminophen. SC-25469 (150 and 300 mg/kg p.o.) and SC-19220 (50-300 mg/kg p.o.) also suppressed the behavioral response to s.c. injection of formalin, as did aspirin (50-150 mg/kg p.o.), ibuprofen (25-100 mg/kg p.o.) and acetaminophen (300 mg/kg p.o.). However, the suppression was not of the magnitude observed after administration of morphine (ED50: 0.9 mg/kg s.c.), pentazocine (ED50: 2.4 mg/kg s.c.) or U-50,488 (ED50: 0.8 mg/kg s.c.). This study demonstrates the antinociceptive properties of prostaglandin antagonists in two distinct tests of nociception.

摘要

本研究考察了两种前列腺素拮抗剂SC - 25469和SC - 19220对大鼠的抗伤害感受作用。SC - 25469和SC - 19220抑制乙酸诱导的扭体反应，口服给药的半数有效剂量（ED50）分别为6.9和6.8 mg/kg。与其他镇痛药相比，在扭体试验中效力的排序为：吗啡＞喷他佐辛 = U - 50,488＞SC - 25469 = SC - 19220＞布洛芬＞阿司匹林＞对乙酰氨基酚。SC - 25469（口服150和300 mg/kg）和SC - 19220（口服50 - 300 mg/kg）也抑制了皮下注射福尔马林引起的行为反应，阿司匹林（口服50 - 150 mg/kg）、布洛芬（口服25 - 100 mg/kg）和对乙酰氨基酚（口服300 mg/kg）也有同样作用。然而，这种抑制作用的程度不如给予吗啡（皮下注射ED50：0.9 mg/kg）、喷他佐辛（皮下注射ED50：2.4 mg/kg）或U - 50,488（皮下注射ED50：0.8 mg/kg）后所观察到的程度。本研究在两种不同的伤害感受试验中证明了前列腺素拮抗剂的抗伤害感受特性。