Czuczwar S J, Szczepanik B, Wamil A, Janusz W, Kleinrok Z
Department of Pharmacology, Lublin Medical School, Poland.
J Neural Transm Gen Sect. 1990;81(2):153-66. doi: 10.1007/BF01245835.
L-phenylisopropyladenosine (L-PIA; a preferential A1 adenosine agonist-0.05 mg/kg) offered no protection against electroconvulsions in mice but potentiated the anticonvulsant action of diazepam and valproate against maximal electroshock-induced seizures, decreasing the respective ED50 values from 9.5 to 4.0 mg/kg and from 250 to 185 mg/kg. However, it remained without effect on the protective activity of phenobarbital, carbamazepine and diphenylhydantoin. 5'-N-ethylcarboxamidoadenosine (NECA; a preferential A2 adenosine agonist-0.5 mg/kg) potentiated the efficacy of valproate. On the other hand, NECA (1 mg/kg) diminished the anticonvulsant action of phenobarbital (ED50 was elevated from 16.5 to 20.5 mg/kg), possessing no effect upon the protective action of carbamazepine. In addition, papaverine (20 mg/kg) significantly enhanced the protective efficacy of valproate and up to 40 mg/kg remained without influence upon the protective action of carbamazepine. However, papaverine (20 and 40 mg/kg) inhibited the anticonvulsive potential of phenobarbital. In the light of the results obtained A1 and A2 adenosine receptor-mediated events seem to possess different influences upon the protective effects of antiepileptic drugs.
L-苯异丙基腺苷(L-PIA;一种选择性A1腺苷激动剂,剂量为0.05毫克/千克)对小鼠电惊厥无保护作用,但能增强地西泮和丙戊酸对最大电休克诱发惊厥的抗惊厥作用,使各自的半数有效剂量(ED50)值分别从9.5毫克/千克降至4.0毫克/千克,从250毫克/千克降至185毫克/千克。然而,它对苯巴比妥、卡马西平和苯妥英钠的保护活性没有影响。5'-N-乙基羧酰胺腺苷(NECA;一种选择性A2腺苷激动剂,剂量为0.5毫克/千克)增强了丙戊酸的疗效。另一方面,NECA(1毫克/千克)减弱了苯巴比妥的抗惊厥作用(ED50从16.5毫克/千克升至20.5毫克/千克),对卡马西平的保护作用没有影响。此外,罂粟碱(20毫克/千克)显著增强了丙戊酸的保护效果,高达40毫克/千克时对卡马西平的保护作用仍无影响。然而,罂粟碱(20毫克/千克和40毫克/千克)抑制了苯巴比妥的抗惊厥潜力。根据所得结果,A1和A2腺苷受体介导的事件似乎对抗癫痫药物的保护作用有不同影响。