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登齐莫尔,一种新型抗惊厥药物。I. 一般抗惊厥概况。

Denzimol, a new anticonvulsant drug. I. General anticonvulsant profile.

作者信息

Graziani G, Tirone F, Barbadoro E, Testa R

出版信息

Arzneimittelforschung. 1983;33(8):1155-60.

PMID:6685493
Abstract

The anticonvulsant profile of N-[beta-[4-(beta-phenylethyl)phenyl]-beta-hydroxyethyl]imidazole hydrochloride (denzimol, Rec 15-1533) has been evaluated in mice, rats and rabbits in comparison with some standard antiepileptic drugs. Denzimol suppressed electrically and chemically induced tonic seizures but did not prevent the clonic ones. In mice and rabbits the anticonvulsant activity of denzimol against maximal electroshock seizures was almost equal to that of phenytoin and phenobarbital with more rapid onset of action, whereas in rats the compound resulted in being the most potent and the less toxic one showing a longer duration of anticonvulsant activity than phenytoin. In the maximal pentetrazol seizures test in rats denzimol showed a profile similar to that of phenytoin and carbamazepine, but different from that of barbiturates and benzodiazepines so that it is suggested that its clinical application would be that of "grand mal" and psychomotor type seizures therapy.

摘要

已将盐酸N - [β - [4 - (β - 苯乙基)苯基]-β - 羟乙基]咪唑(登齐莫尔,Rec 15 - 1533)与一些标准抗癫痫药物相比较,在小鼠、大鼠和兔子身上评估了其抗惊厥特性。登齐莫尔可抑制电诱导和化学诱导的强直性惊厥,但不能预防阵挛性惊厥。在小鼠和兔子中,登齐莫尔对最大电休克惊厥的抗惊厥活性几乎与苯妥英和苯巴比妥相当,且起效更快,而在大鼠中,该化合物是最有效的且毒性最小的,其抗惊厥活性持续时间比苯妥英更长。在大鼠最大戊四氮惊厥试验中,登齐莫尔表现出与苯妥英和卡马西平相似的特性,但与巴比妥类药物和苯二氮䓬类药物不同,因此有人提出其临床应用将用于“大发作”和精神运动型癫痫的治疗。

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