Thorat S N, Kulkarni S K
Department of Pharmaceutical Sciences, Panjab University, Chandigarh, India.
Methods Find Exp Clin Pharmacol. 1991 Jul-Aug;13(6):413-7.
Ethanol (1 and 2 g/kg, i.p.) and MK-801 (1 mg/kg, i.p.), N-methyl-D-aspartate (NMDA) receptor antagonist, offered protection against caffeine-induced convulsions in mice. Subeffective doses of ethanol (0.5-g/kg, i.p.) and MK-801 (0.5 mg/kg, i.p.) when administered concurrently, did not provide a facilitatory anticonvulsant action against caffeine-induced convulsions. Ethanol (0.5 g/kg, i.p.) when administered concurrently with adenosine (100 mg/kg, i.p.) or dipyridamole (5 mg/kg, i.p.) elicited a facilitatory anticonvulsant action. However, concurrent administration of subeffective doses of MK-801 (0.5 mg/kg i.p.) with adenosine (100 mg/kg, i.p.) did not offer a facilitatory anticonvulsant action against caffeine-induced convulsions. The protective effect of ethanol (1 g/kg, i.p.) against caffeine-induced convulsions was reversed by an imidazobenzodiazepine, Ro 15-4513 (4 mg/kg, i.p.). Ro 15-4513 did not produce any proconvulsant effect with caffeine. It is suggested that ethanol and MK-801 elicit their anticonvulsant actions against caffeine-induced convulsions through different receptor mechanisms and that the anticonvulsant action of ethanol may be partly attributed to its ability to act via central adenosinergic mechanisms.
乙醇（腹腔注射，1和2克/千克）和MK-801（腹腔注射，1毫克/千克），一种N-甲基-D-天冬氨酸（NMDA）受体拮抗剂，对咖啡因诱发的小鼠惊厥具有保护作用。当同时给予亚有效剂量的乙醇（腹腔注射，0.5克/千克）和MK-801（腹腔注射，0.5毫克/千克）时，对咖啡因诱发的惊厥没有促进抗惊厥作用。当乙醇（腹腔注射，0.5克/千克）与腺苷（腹腔注射，100毫克/千克）或双嘧达莫（腹腔注射，5毫克/千克）同时给药时，会产生促进抗惊厥作用。然而，亚有效剂量的MK-801（腹腔注射，0.5毫克/千克）与腺苷（腹腔注射，100毫克/千克）同时给药，对咖啡因诱发的惊厥没有促进抗惊厥作用。乙醇（腹腔注射，1克/千克）对咖啡因诱发惊厥的保护作用被一种咪唑并苯二氮䓬Ro 15-4513（腹腔注射，4毫克/千克）逆转。Ro 15-4513与咖啡因一起不会产生任何促惊厥作用。提示乙醇和MK-801通过不同的受体机制对咖啡因诱发的惊厥产生抗惊厥作用，并且乙醇的抗惊厥作用可能部分归因于其通过中枢腺苷能机制发挥作用的能力。
