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咪唑啉6,7-苯并二唑烷的抗惊厥活性。

Anticonvulsant activity of the imidazoline 6,7-benzoidazoxan.

作者信息

Jackson H C, Ripley T L, Dickinson S L, Nutt D J

机构信息

Reckitt & Colman Psychopharmacology Unit, Department of Pharmacology, School of Medical Sciences, Bristol, U.K.

出版信息

Epilepsy Res. 1991 Jul;9(2):121-6. doi: 10.1016/0920-1211(91)90022-8.

Abstract

The effects of the imidazoline 6,7-benzoidazoxan on seizure threshold were assessed using standard tests of anticonvulsant activity. Benzoidazoxan (10-30 mg/kg i.p.; 100 mg/kg p.o.) prevented tonic, but not clonic, convulsions induced by electroshock in mice. The increase in seizure threshold was of rapid onset, and, although of short duration, was comparable with that obtained using phenytoin and sodium valproate. Moreover, unlike sodium valproate, benzoidazoxan was an efficacious anticonvulsant at doses (20, 30 mg/kg i.p.) which did not impair rotarod performance. The anticonvulsant effects of benzoidazoxan were confirmed using the maximal electroshock test in mice (median effective dose, 13.2 mg/kg i.p.) and rats (anticonvulsant at 30 mg/kg i.p.). In addition, benzoidazoxan (10, 30 mg/kg i.p.) prevented tonic, but not clonic, seizures induced by bicuculline in mice. Thus, the imidazoline benzoidazoxan was found to be a novel anticonvulsant agent against electrically and chemically induced seizures in mice and rats with a profile of action similar to that of phenytoin.

摘要

使用抗惊厥活性的标准测试评估了咪唑啉6,7-苯并异恶唑对癫痫阈值的影响。苯并异恶唑(腹腔注射10 - 30毫克/千克;口服100毫克/千克)可预防小鼠电休克诱发的强直性惊厥,但不能预防阵挛性惊厥。癫痫阈值的升高起效迅速,虽然持续时间短,但与使用苯妥英钠和丙戊酸钠所获得的效果相当。此外,与丙戊酸钠不同,苯并异恶唑在不损害转棒试验表现的剂量(腹腔注射20、30毫克/千克)下是一种有效的抗惊厥药。使用小鼠(腹腔注射的半数有效剂量为13.2毫克/千克)和大鼠(腹腔注射30毫克/千克时有抗惊厥作用)的最大电休克试验证实了苯并异恶唑的抗惊厥作用。此外,苯并异恶唑(腹腔注射10、30毫克/千克)可预防小鼠荷包牡丹碱诱发的强直性惊厥,但不能预防阵挛性惊厥。因此,发现咪唑啉苯并异恶唑是一种新型抗惊厥药,对小鼠和大鼠电诱发和化学诱发的癫痫发作均有作用,其作用谱与苯妥英钠相似。

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