Yamamoto H, Kuki M, Ozaki M
Nihon Yakurigaku Zasshi. 1977 Oct;73(7):703-15. doi: 10.1254/fpj.73.703.
Effects of beta-(p-chlorophenyl)-GABA (baclofen), a muscle relaxant, on the response of mice and rats to various noxious stimuli were studied. In mice, 5 approximately 10 mg/kg i.p. of baclofen delayed the response time to tail-pinch and hot-plate stimuli but the relaxation was also apparent with this dose range. Mephenesin also delayed the response time to tail-pinch stimuli with the dose producing muscle relaxation. Baclofen, 3 mg/kg i.p., while producing no muscle relaxation, suppressed the acetic acid-induced writhing. The same effect, suppression of writhing and no muscle relaxation, was achieved with 50 mg/kg i.p. of mephenesin. In rats, baclofen (5 approximately 10 mg/kg i.p.) increased the response threshold in Randall-Selitto method and suppressed the bradykinin-induced symptoms, however, muscle relaxation was also produced with these same doses. Increase in response threshold in Randall-Selitto method was achieved with the dose of mephenesin producing muscle relaxation. The time courses of the depression of response to noxious stimuli and the muscle relaxation induced by baclofen and mephenesin were consistent in mice and rats. A small dose (3 mg/kg i.p. in mice, 2 mg/kg/h s.c. in rats) of baclofen reduced the antinociceptive effect of morphine but a larger dose (5 mg/kg i.p. in mice, 7 mg/kg/h s.c. in rats) of baclofen increased or did not alter the effect of morphine. It seems likely that the antinociceptive effect of baclofen may be nonspecific to analgesia.
研究了肌肉松弛剂β-(对氯苯基)-γ-氨基丁酸(巴氯芬)对小鼠和大鼠对各种有害刺激反应的影响。在小鼠中,腹腔注射5~10mg/kg的巴氯芬可延迟对夹尾和热板刺激的反应时间,但在此剂量范围内也出现了松弛现象。甲芬那酸在产生肌肉松弛的剂量下也延迟了对夹尾刺激的反应时间。腹腔注射3mg/kg的巴氯芬虽未产生肌肉松弛,但抑制了醋酸诱导的扭体反应。腹腔注射50mg/kg的甲芬那酸也产生了同样的效果,即抑制扭体反应且无肌肉松弛。在大鼠中,腹腔注射巴氯芬(5~10mg/kg)可提高兰德尔-塞利托法中的反应阈值并抑制缓激肽诱导的症状,然而,这些相同剂量也会产生肌肉松弛。在产生肌肉松弛的甲芬那酸剂量下,可提高兰德尔-塞利托法中的反应阈值。巴氯芬和甲芬那酸对有害刺激反应的抑制和肌肉松弛的时间进程在小鼠和大鼠中是一致的。小剂量的巴氯芬(小鼠腹腔注射3mg/kg,大鼠皮下注射2mg/kg/h)可降低吗啡的镇痛作用,但大剂量的巴氯芬(小鼠腹腔注射5mg/kg,大鼠皮下注射7mg/kg/h)可增强或不改变吗啡的作用。巴氯芬的镇痛作用似乎可能对镇痛是非特异性的。