Anticonvulsant doses of inosine result in brain levels sufficient to inhibit [3H] diazepam binding

P. J. Marangos, E. Trams, R. L. Clark-Rosenberg, S. M. Paul, P. Skolnick

Research output: Contribution to journalArticlepeer-review

20 Scopus citations


Several purines have been shown to be competitive inhibitors of [3H] diazepam binding. Inosine has also been shown to have benzodiazepine-like neurophysiologic, pharmacologic and behavioral effects, and to partially inhibit caffeine-induced seizures in mice. Using presumptive therapeutic doses of inosine, levels were determined in mouse brain at various times following injection. Inosine and hypoxanthine concentrations in brain increased several fold following inosine administration, indicating that inosine permeated the blood-brain barrier. The levels of inosine and hypoxanthine attained in brain were sufficient to inhibit by more than 50% the GABA-stimulated [3H] diazepam binding. These data suggest that that the anticonvulsant properties of inosine are related to its interaction with the benzodiazepine receptor.

Original languageEnglish
Pages (from-to)175-178
Number of pages4
Issue number2
StatePublished - Nov 1981


  • Benzodiazepine receptor
  • Convulsions
  • Hypoxanthine
  • Inosine


Dive into the research topics of 'Anticonvulsant doses of inosine result in brain levels sufficient to inhibit [3H] diazepam binding'. Together they form a unique fingerprint.

Cite this