Lee R J, Bajorek J G, Lomax P
Neuropharmacology. 1984 May;23(5):517-24. doi: 10.1016/0028-3908(84)90024-8.
Opioid agonists were used to investigate the modulation of seizures mediated by mu, kappa and delta opiate receptors in the seizure-sensitive Mongolian gerbil. Morphine (1.0-25 mg/kg, s.c.) were used as prototypic agonists for mu, kappa and delta opiate receptors. Each opioid decreased the incidence and severity of the seizure as compared to control values. The anticonvulsant effects of morphine (10 mg/kg, s.c.) and ketocyclazocine (0.5 mg/kg, s.c.) were reversed by naloxone (1.0 mg/kg, s.c.), while the anticonvulsant effects of N-allylnormetazocine (2 mg/kg, s.c.) were not significantly changed by naloxone. Additionally, abnormal behavior was observed following administration of the opioids. Morphine (10 mg/kg, s.c.) produced excitation and hyperresponsiveness with intermittent cataleptic-like states. Ketocyclazocine (10 mg/kg, s.c.) predominantly produced a stuporous, immobile state, accompanied by some loss of posture. N-allylnormetazocine (10 mg/kg, s.c.) produced ataxia and stereotypic side-to-side head nodding . Naloxone was able to reverse the behavioral effects produced by morphine and ketocyclazocine but not those produced by N-allylnormetazocine. The data presented are consistent with earlier studies which demonstrated the anticonvulsant effects of beta-endorphin in the gerbil. This study further suggests that opioids have a protective role against seizure activity in the gerbil and the opioid anticonvulsant effect is not specific to one type of opioid agonist.
阿片类激动剂被用于研究在对癫痫敏感的蒙古沙鼠中,由μ、κ和δ阿片受体介导的癫痫调节作用。吗啡(1.0 - 25毫克/千克,皮下注射)被用作μ、κ和δ阿片受体的典型激动剂。与对照值相比,每种阿片类药物都降低了癫痫的发生率和严重程度。纳洛酮(1.0毫克/千克,皮下注射)可逆转吗啡(10毫克/千克,皮下注射)和酮环唑辛(0.5毫克/千克,皮下注射)的抗惊厥作用,而纳洛酮对N - 烯丙基去甲左啡诺(2毫克/千克,皮下注射)的抗惊厥作用无显著影响。此外,在给予阿片类药物后观察到了异常行为。吗啡(10毫克/千克,皮下注射)产生兴奋和高反应性,并伴有间歇性的类僵住状态。酮环唑辛(10毫克/千克,皮下注射)主要产生一种昏睡、不动的状态,并伴有一些姿势丧失。N - 烯丙基去甲左啡诺(10毫克/千克,皮下注射)产生共济失调和刻板的左右点头动作。纳洛酮能够逆转吗啡和酮环唑辛产生的行为效应,但不能逆转N - 烯丙基去甲左啡诺产生的行为效应。所呈现的数据与早期证明β - 内啡肽对沙鼠有抗惊厥作用的研究一致。这项研究进一步表明,阿片类药物在沙鼠中对癫痫活动具有保护作用,并且阿片类抗惊厥作用并非特定于某一种阿片类激动剂。