3-羟甲基苯妥英丙戊酸酯，一种结合两种抗惊厥药物的新型前药。

3-Hydroxymethylphenytoin valproic acid ester, a new prodrug combining two anticonvulsant drugs.

作者信息

Scriba G K

机构信息

Department of Pharmaceutical Chemistry, University of Münster, Germany.

出版信息

Arch Pharm (Weinheim). 1996 Dec;329(12):554-5. doi: 10.1002/ardp.19963291208.

DOI:10.1002/ardp.19963291208

PMID:9038424

Abstract

3-Hydroxymethylphenytoin valproic acid ester (VAL-PHT) was designed as a new prodrug combining valproic acid and phenytoin, two anticonvulsant drugs with different pharmacological profiles. The compound was hydrolyzed by rat plasma esterases in vitro but exhibited only activity in the maximal electroshock seizure test (MES test) after intraperitoneal administration to mice. The compound did not protect against pentylenetetrazole-induced seizures. It is concluded that VAL-PHT acts as a prodrug displaying the anticonvulsant profile of phenytoin.

摘要

3-羟甲基苯妥英丙戊酸酯（VAL-PHT）被设计为一种新的前药，它结合了丙戊酸和苯妥英这两种具有不同药理学特性的抗惊厥药物。该化合物在体外被大鼠血浆酯酶水解，但在对小鼠腹腔注射后仅在最大电休克惊厥试验（MES试验）中表现出活性。该化合物不能预防戊四氮诱导的惊厥。结论是VAL-PHT作为一种前药，表现出苯妥英的抗惊厥特性。