蛋白激酶C的抑制而非蛋白激酶A的抑制，会阻断小鼠对鞘内注射μ-阿片受体激动剂产生急性抗伤害感受耐受性的过程。
Inhibition of protein kinase C, but not of protein kinase A, blocks the development of acute antinociceptive tolerance to an intrathecally administered mu-opioid receptor agonist in the mouse.
作者信息
Narita M, Narita M, Mizoguchi H, Tseng L F
机构信息
Department of Anesthesiology, Medical College of Wisconsin, Milwaukee 53226, USA.
出版信息
Eur J Pharmacol. 1995 Jul 4;280(2):R1-3. doi: 10.1016/0014-2999(95)00322-c.
A specific protein kinase C inhibitor, calphostin C, which injected alone had no effect on the antinociception induced by intrathecal (i.t.) administration of a selective mu-opioid receptor agonist, [D-Ala2,NMePhe4,Gly(ol)5]enkephalin (DAMGO), dose-dependently attenuated the development of acute tolerance to the i.t. DAMGO-induced antinociception in male ICR mice. On the other hand, a selective protein kinase A inhibitor, KT5720, did not have any effect on the development of acute tolerance to DAMGO antinociception. These findings suggest that protein kinase C, but not protein kinase A, plays an important role in the development of acute tolerance to the mu-opioid receptor agonist-induced antinociception.
一种特异性蛋白激酶C抑制剂——钙泊三醇（calphostin C），单独注射时对鞘内注射选择性μ-阿片受体激动剂[D-丙氨酸2，N-甲基苯丙氨酸4，甘氨酸（醇）5]脑啡肽（DAMGO）诱导的抗伤害感受没有影响，但能剂量依赖性地减弱雄性ICR小鼠对鞘内注射DAMGO诱导的抗伤害感受的急性耐受性的形成。另一方面，选择性蛋白激酶A抑制剂KT5720对DAMGO抗伤害感受的急性耐受性形成没有任何影响。这些发现表明，在对μ-阿片受体激动剂诱导的抗伤害感受的急性耐受性形成过程中，起重要作用的是蛋白激酶C，而非蛋白激酶A。
Zotero 插件