Nabeshima T, Matsuno K, Kameyama T
Eur J Pharmacol. 1985 Aug 15;114(2):197-207. doi: 10.1016/0014-2999(85)90628-4.
We have investigated the correlation of electric shock-induced behavioral changes and functional alterations of endogenous opioid receptor subtypes. The degree of electric shock-induced behavioral changes, such as analgesia and motor suppression, was dependent on the duration of and time after electric shock application. The electric shock-induced behavioral changes were completely antagonized by naloxone. The apparent development of tolerance to both behavioral effects as a result of successive daily electric shock was different: Tolerance to electric shock-induced analgesia developed after 2 days' successive electric shock application, while tolerance to motor suppression was not observed even after 7 days' successive electric shock application. There was a decrease of [3H][D-Ala2, Met5]enkephalinamide ([3H]DAMEA, delta agonist) binding and an increase of [3H]naloxone (mu antagonist) binding when potent electric shock-induced analgesia developed. On the other hand, the binding of [3H]DAMEA and [3H]ethylketocyclazocine (kappa agonist) was significantly changed when locomotion was suppressed. These results suggest strongly that different opioid systems may participate in electric shock-induced analgesia and motor suppression: electric shock-induced analgesia and motor suppression may be mediated by mu/delta and kappa/delta receptors, respectively.
我们研究了电击诱导的行为变化与内源性阿片受体亚型功能改变之间的相关性。电击诱导的行为变化程度,如镇痛和运动抑制,取决于电击施加的持续时间和电击后的时间。电击诱导的行为变化可被纳洛酮完全拮抗。连续每日电击导致对两种行为效应的耐受性明显发展情况不同:连续电击2天后出现对电击诱导镇痛的耐受性,而即使连续电击7天也未观察到对运动抑制的耐受性。当强烈的电击诱导镇痛出现时,[3H][D-Ala2,Met5]脑啡肽酰胺([3H]DAMEA,δ激动剂)结合减少,[3H]纳洛酮(μ拮抗剂)结合增加。另一方面,当运动受到抑制时,[3H]DAMEA和[3H]乙基酮环唑新(κ激动剂)的结合发生显著变化。这些结果强烈表明,不同的阿片系统可能参与电击诱导的镇痛和运动抑制:电击诱导的镇痛和运动抑制可能分别由μ/δ和κ/δ受体介导。