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3‐Hydroxymethylphenytoin Valproic Acid Ester, a New Prodrug Combining Two Anticonvulsant Drugs
Author(s) -
Scriba Gerhard K. E.
Publication year - 1996
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19963291208
Subject(s) - anticonvulsant , prodrug , valproic acid , phenytoin , pharmacology , chemistry , in vitro , epilepsy , medicine , biochemistry , psychiatry
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.