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醋甲酰胺的抗惊厥活性。

Anticonvulsant activity of milacemide.

作者信息

van Dorsser W, Barris D, Cordi A, Roba J

出版信息

Arch Int Pharmacodyn Ther. 1983 Dec;266(2):239-49.

PMID:6667068
Abstract

The anticonvulsant activity of a new drug, milacemide (2-(pentylamino)-acetamide), has been studied in animal models of convulsions like those induced by bicuculline, pentylenetetrazol, picrotoxin, strychnine, inhibitors of GABA synthesis as 3-mercaptopropionic acid, allylglycine, isoniazid and thiosemicarbazide and electroshock. Milacemide is particularly effective in inhibiting the convulsions induced by bicuculline. The ED50 is 5.7 mg/kg by oral route and the activity lasts for more than 48 hr. It is less active against pentylenetetrazol and only marginally active against electroshock. It has not be found active against the other types of convulsions. Milacemide has a low toxicity (LD50: 2585 mg/kg in the mouse) and alters the behaviour of mouse, rat and monkey, only at high doses (greater than or equal to 1000 mg/kg). Milacemide seems to be specially free of sedative potential.

摘要

一种新药米拉醋胺(2 -(戊基氨基)乙酰胺)的抗惊厥活性已在多种惊厥动物模型中进行了研究,这些模型包括由荷包牡丹碱、戊四氮、印防己毒素、士的宁、γ-氨基丁酸(GABA)合成抑制剂如3 - 巯基丙酸、烯丙基甘氨酸、异烟肼和氨基硫脲诱导的惊厥模型以及电休克模型。米拉醋胺在抑制荷包牡丹碱诱导的惊厥方面特别有效。口服给药的半数有效量(ED50)为5.7毫克/千克,且活性持续超过48小时。它对戊四氮的活性较低,对电休克仅有微弱活性。尚未发现它对其他类型的惊厥有活性。米拉醋胺毒性较低(小鼠的半数致死量:2585毫克/千克),并且仅在高剂量(大于或等于1000毫克/千克)时才会改变小鼠、大鼠和猴子的行为。米拉醋胺似乎特别没有镇静作用。

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