Purinergic inhibition of diazepam binding to rat brain (in vitro)

P. J. Marangos, S. M. Paul, A. M. Parma, F. K. Goodwin, P. Syapin, P. Skolnick

Research output: Contribution to journalArticlepeer-review

176 Scopus citations


Our recent report that the endogenous purines inosine and hypoxanthine competitively inhibit [3H] diazepam binding to rat brain synaptosomal membranes (1,2) has now been confirmed (3). We now report that a wide spectrum of purines are able to inhibit specific [3H] diazepam binding while pyrimidines are inactive. Preliminary structure activity relationships indicate that the 2′-deoxypurines are more potent in diazepam binding inhibition as are the l-methyl compounds, whereas the 7-methyl purines are inactive. Data are also presented which show that the xanthine stimulants caffeine, theophylline, and theobromine as well as the central nervous system convulsant pentylenetetrazol all competitively inhibit [3H] diazepam binding.

Original languageEnglish
Pages (from-to)851-857
Number of pages7
JournalLife Sciences
Issue number9
StatePublished - Feb 26 1979


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