Effect of Chlorination on the Anticonvulsant Activity of Phenobarbital

The lethal doses, neurotoxic doses, anticonvulsant potencies, and protective indices for two chlorinated barbiturates, 5-(4-chlorophenyl)-5-ethylbarbituric acid (mono-chloro) and 5-(3,4-dichlorophenyl)-5-ethylbarbituric acid (dichloro), were determined in mice and the results compared with similar v...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1963-05, Vol.52 (5), p.463-465
Main Authors: Swinyard, Ewart A., Goodman, Louis S., Miyahara, James T.
Format: Article
Language:English
Subjects:
Anticonvulsants
Chlorine
Halogenation
Humans
Ions
Phenobarbital
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Summary:The lethal doses, neurotoxic doses, anticonvulsant potencies, and protective indices for two chlorinated barbiturates, 5-(4-chlorophenyl)-5-ethylbarbituric acid (mono-chloro) and 5-(3,4-dichlorophenyl)-5-ethylbarbituric acid (dichloro), were determined in mice and the results compared with similar values concomitantly determined for phenobarbital. Chlorination was found to delay markedly the time for peak anticonvulsant effect and to prolong duration of action. The lethal dose for monochloro was somewhat larger and that for dichloro significantly smaller than that for phenobarbital. The minimal neurotoxic dose for monochloro was significantly larger than that for either dichloro or phenobarbital. All three compounds exhibited anticonvulsant activity in nontoxic doses. Although chlorination of phenobarbital had no significant effect on protective indices, the protective indices for dichloro tended to be somewhat higher than those for the other two compounds.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600520513