Li L Y, Chang K J
Department of Anesthesiology, Duke University Medical Center, Durham, North Carolina 27710, USA.
Mol Pharmacol. 1996 Sep;50(3):599-602.
The mitogen-activated protein (MAP) kinase of Chinese hamster ovary cells (CHO mu66 cell line) transfected to express mu-opioid receptors was markedly activated by mu agonists. The rank order of effectiveness of agonists was approximately the same as the rank order of their binding affinities to the mu receptor. The delta and kappa receptor-specific agonists cyclic[D-Pen2, D-Pen5]enkephalin and U69,593 showed a very weak stimulatory effect. The mu agonist-stimulated MAP kinase activity peaked at approximately 4-8 min and lasted almost 1 hr. The stimulatory effect of mu agonists was antagonized by the opioid receptor antagonist naltrexone and inhibited by pretreatment of cells with pertussis toxin. This opioid-induced activation of MAP kinase activity may have a role in the long term effects of opioids.
转染以表达μ阿片受体的中国仓鼠卵巢细胞（CHO mu66细胞系）的丝裂原活化蛋白（MAP）激酶被μ激动剂显著激活。激动剂的效力顺序与其对μ受体的结合亲和力顺序大致相同。δ和κ受体特异性激动剂环[D-青霉胺2，D-青霉胺5]脑啡肽和U69,593显示出非常微弱的刺激作用。μ激动剂刺激的MAP激酶活性在约4-8分钟达到峰值，并持续近1小时。μ激动剂的刺激作用被阿片受体拮抗剂纳曲酮拮抗，并被用百日咳毒素预处理细胞所抑制。这种阿片类药物诱导的MAP激酶活性激活可能在阿片类药物的长期作用中起作用。
