Czuczwar S J
Pol J Pharmacol Pharm. 1981 Jan-Feb;33(1):25-35.
Aminooxyacetic acid (AOAA; 20 and 40 mg/kg), baclofen (15 and 20 mg/kg), gamma-hydroxybutyric acid (GHBA; 250 mg/kg) and gamma-aminobutyric acid (GABA: 3000 mg/kg), administered intraperitoneally, increased the convulsive threshold in mice but to a relatively small degree. Bicuculline and picrotoxin were shown to reverse these anticonvulsant effects except for baclofen. Apomorphine (10 mg/kg), amantadine (100 mg/kg) and L-DOPA (62 . 5 and 125 mg/kg) potentiated the action of AOAA (20 mg/kg). Also apomorphine (5 and 10 mg/kg) and amantadine (25 and 100 mg/kg) potentiated the anticonvulsant activity of baclofen (15 mg/kg). Combined treatment with baclofen (15 mg/kg) and amantadine (100 mg/kg) resulted in about 4-fold increase in the convulsive threshold. However, the action of GABA and GHBA was poorly affected by dopaminergic agonists, amantadine even decreased the threshold in animals pretreated with these substances. The results obtained in this study suggest dopaminergic stimulation to be of importance in potentiating the anticonvulsant action of some GABA-ergic drugs.
腹腔注射氨基氧乙酸(AOAA;20和40毫克/千克)、巴氯芬(15和20毫克/千克)、γ-羟基丁酸(GHBA;250毫克/千克)和γ-氨基丁酸(GABA:3000毫克/千克)可提高小鼠的惊厥阈值,但提高幅度相对较小。除巴氯芬外,荷包牡丹碱和印防己毒素可逆转这些抗惊厥作用。阿扑吗啡(10毫克/千克)、金刚烷胺(100毫克/千克)和左旋多巴(62.5和125毫克/千克)可增强AOAA(20毫克/千克)的作用。同样,阿扑吗啡(5和10毫克/千克)和金刚烷胺(25和100毫克/千克)可增强巴氯芬(15毫克/千克)的抗惊厥活性。巴氯芬(15毫克/千克)和金刚烷胺(100毫克/千克)联合治疗可使惊厥阈值提高约4倍。然而,多巴胺能激动剂对GABA和GHBA的作用影响较小,金刚烷胺甚至会降低预先用这些物质处理过的动物的阈值。本研究获得的结果表明,多巴胺能刺激在增强某些GABA能药物的抗惊厥作用中具有重要意义。