Ganz A J, Waser P G, Pfirrmann R W
Arzneimittelforschung. 1978;28(8):1331-4.
9 derivatives of sulfanilamide were tested for anticonvulsant properties against electroconvulsive shock in mice and rats and against pentylenetetrazole shock in mice. Reference standard in these tests was sulfanilamide. Their toxic, analgesic and sedative activities were also examined. The anticonvulsive activity of sulfanilamide could be enhanced by substitution of the phenyl ring with a halogen atom. Substitution of the sulfonamide group diminishes the anticonvulsant and increases the sedative activity of sulfanilamide. Detoxication of the basic substance by substitution of the aromatic amino group only little influences the anticonvulsant activity and may even enhance it. Of the tested substances, 1742 (3-chloro-4-phenacetamido-benzene-sulfonamide) exhibited the best anticonvulsant activity; slightly weaker was PB 311 (3-chloro-4-amino-benzene-sulfonamide). The ED50 for the activity against electroconvulsive shock of both substances was about 30 mg/kg p.o. in mice. The relationship between anticonvulsant activity and inhibition of the renal and cerebral carbonic anhydrase is discussed.
对9种磺胺衍生物进行了测试，以考察其对小鼠和大鼠电惊厥休克以及对小鼠戊四氮休克的抗惊厥特性。这些测试中的参考标准物是磺胺。还检测了它们的毒性、镇痛和镇静活性。用卤原子取代苯环可增强磺胺的抗惊厥活性。取代磺酰胺基团会降低磺胺的抗惊厥活性并增加其镇静活性。通过取代芳香氨基对碱性物质进行解毒对其抗惊厥活性影响很小，甚至可能增强该活性。在所测试的物质中，1742（3-氯-4-苯乙酰氨基苯磺酰胺）表现出最佳的抗惊厥活性；PB 311（3-氯-4-氨基苯磺酰胺）的活性稍弱。两种物质对电惊厥休克活性的半数有效剂量在小鼠口服时约为30毫克/千克。讨论了抗惊厥活性与肾和脑碳酸酐酶抑制之间的关系。
