Nguyen T T, Matsumoto K, Yamasaki K, Nguyen M D, Nguyen T N, Watanabe H
Division of Pharmacology, Research Institute for Wakan-Yaku (Oriental Medicines), Toyama Medical and Pharmaceutical University, Japan.
Jpn J Pharmacol. 1996 Aug;71(4):345-9. doi: 10.1254/jjp.71.345.
The effect of majonoside-R2 on morphine- and U-50,488H-induced antinociception was examined by the tail-pinch test in mice and compared with that of diazepam. Majonoside-R2 and diazepam inhibited the morphine- and U-50,488H-induced antinociception, and the actions were antagonized by the benzodiazepine receptor antagonist flumazenil and the GABA-gated CI- channel blocker picrotoxin. Diazepam but not majonoside-R2 exhibited a protective activity against convulsion caused by the GABAA antagonists bicuculline and picrotoxin. These results indicate that GABAA systems are involved in the effect of majonoside-R2 on the opioid-induced antinociception and suggest that the mechanisms of action of majonoside-R2 may differ from those of diazepam.
通过小鼠夹尾试验研究了马钱子苷 -R2 对吗啡和 U-50,488H 诱导的镇痛作用的影响，并与地西泮进行了比较。马钱子苷 -R2 和地西泮均抑制吗啡和 U-50,488H 诱导的镇痛作用，且这些作用被苯二氮䓬受体拮抗剂氟马西尼和 GABA 门控氯离子通道阻滞剂印防己毒素所拮抗。地西泮而非马钱子苷 -R2 对由 GABAA 拮抗剂荷包牡丹碱和印防己毒素引起的惊厥具有保护活性。这些结果表明，GABAA 系统参与了马钱子苷 -R2 对阿片类药物诱导的镇痛作用，提示马钱子苷 -R2 的作用机制可能与地西泮不同。
