痛稳素和痛稳素(10～17)对孤啡肽对抗内吗啡肽-1及内吗啡肽-2镇痛作用的影响

目的研究痛稳素及其碳末端八肽在小鼠脑内对孤啡肽对抗内吗啡肽-1及内吗啡肽-2镇痛作用的影响。方法以固相多肽合成法合成了痛稳素及其碳末端八肽,侧脑室注射孤啡肽、痛稳素及其碳末端八肽,用辐射热甩尾法测定痛阈。结果孤啡肽可对抗内吗啡肽-1及内吗啡肽-2的镇痛作用;痛稳素及其碳末端八肽不影响小鼠的基础痛阈,但可逆转孤啡肽对抗内吗啡肽-1及内吗啡肽-2的镇痛作用。结论痛稳素及其碳末端八肽在脊髓以上水平可逆转孤啡肽对抗内吗啡肽-1及内吗啡肽-2的镇痛作用。

EFFECTS OF NOCISTATIN AND NOCISTATIN (10～17) ON NOCICEPTIN IN ANTAGONIZING ENDOMORPHIN-1 AND ENDOMORPHIN-2 ANALGESIA IN MICE

AIMTo investigate the effects of nocistatin and nocistatin (10～17) on nociceptin in antagonizing endomorphin-1 or endomorphin-2 analgesia in mice. METHODSNocistatin and nocistatin (10～17) were synthesized by solid-phase peptide synthesis method. The mouse tail-flick test was used to assess the pain threshold of the mice and observe the effects of nocistatin and nocistatin (10～17). RESULTSNociceptin was shown to antagonize endomorphin-1 and endomorphin-2 analgesia. Nocistatin or nocistatin (10～17) produced no significant effect on basic pain threshold; however,both of them were found to reverse the effects of nociceptin in antagonizing endomorphin-1 and endomorphin-2 analgesia. CONCLUSIONNocistatin and nocistatin (10～17) were shown to reverse the effects of nociceptin in antagonizing endomorphin-1 and endomorphin-2 analgesia at supraspinal level.