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Reassessment of the anticonvulsant activity of diphenylacetylurea
Author(s) -
Amato Robert J.,
Jones Gary L.
Publication year - 1982
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430020107
Subject(s) - potency , anticonvulsant , bioavailability , phenytoin , phenobarbital , pharmacology , chemistry , significant difference , solubility , medicine , psychology , biochemistry , epilepsy , in vitro , neuroscience , organic chemistry
On the basis of current information about the structure‐activity relationships of anticonvulsant compounds, it is predicted that diphenylacetylurea should possess some degree of antielectroshock activity. However, past attempts to demonstrate this have failed. In the present investigation the authors have determined that this compound does in fact possess such efficacy, although its potency is relatively low in comparison with phenytoin and phenobarbital. The difference in potency among these drugs is greatest when expressed in terms of the i.p. dosage, and much smaller when expressed in terms of blood or brain concentrations. The difference on the basis of i.p. dosage might be due to differences in bioavailability, but the lower potency of diphenylacetylurea expressed in terms of brain concentration is possibly due to its very high lipid solubility, as discussed in the text.