Berman E F, Adler M W
Neuropharmacology. 1984 Mar;23(3):367-71. doi: 10.1016/0028-3908(84)90200-4.
Opioids and opioid peptides influence the threshold to a seizure which is a model of petit mal epilepsy (Cowan, Geller and Adler, 1979). The present authors investigated representative opioid compounds in a model of a grand mal seizure, maximal electroshock (MES). Although all of the opioids and opioid peptides tested blocked tonic hindlimb extension, they divided into two groups, based on their ability to decrease the total length of the tonic component of the maximal electroshock seizure and their sensitivity to blockade by naloxone. The first group contained morphine, meperidine, methadone, ethylketocyclazocine (EK), D-ala2-met-enkephalinamide, D-ala2-leu5-enkephalin and beta-endorphin. The compounds in this group caused a decrease in the length of the tonic component that was dose-related, with the maximum decrease amounting to approx. 40%. The effect was blocked by the prior administration of 1 mg/kg of naloxone. The second group contained the partial agonists, pentazocine and cyclazocine. These opioids also caused a dose-related decrease in the length of the tonic component and, in the largest doses, the tonic component of the convulsion was completely blocked. Naloxone, in doses as large as 10 mg/kg, did not appreciably reverse the action of either drug.
阿片类药物和阿片肽会影响癫痫发作阈值，癫痫小发作模型就是一种失神性癫痫（考恩、盖勒和阿德勒，1979年）。本文作者在大发作模型——最大电休克（MES）中研究了具有代表性的阿片类化合物。尽管所测试的所有阿片类药物和阿片肽都能阻断强直性后肢伸展，但根据它们降低最大电休克发作强直性成分总时长的能力以及对纳洛酮阻断作用的敏感性，可将它们分为两组。第一组包括吗啡、哌替啶、美沙酮、乙基酮环唑辛（EK）、D - 丙氨酸2 - 甲硫氨酸脑啡肽酰胺、D - 丙氨酸2 - 亮氨酸5 - 脑啡肽和β - 内啡肽。该组化合物会使强直性成分的时长出现剂量相关的减少，最大减少幅度约为40%。预先给予1mg/kg的纳洛酮可阻断这种作用。第二组包括部分激动剂喷他佐辛和环唑辛。这些阿片类药物也会使强直性成分的时长出现剂量相关的减少，且在最大剂量时，惊厥的强直性成分会被完全阻断。高达10mg/kg剂量的纳洛酮并未明显逆转这两种药物的作用。
