Benzodiazepine receptors: labeling in intact animals with [3H] flunitrazepam

Raymond S.L. Chang, Solomon H. Snyder

Research output: Contribution to journalArticlepeer-review

130 Scopus citations


[3H]Flumitrazepam appears to label specific benzodiazepine receptors in vitro after i.v. injection in mice. Benzodiazepine potencies in reducing [3H]flunitrazepam binding in vivo correspond to pharmacological potencies and parallel relative affinities for [3H]flunitrazepam binding sites in isolated brain membranes. However, 50% occupation of [3H]-flunitrazepam sites by benzodiazzepines in vivo requires brain concentrations of the drugs about 1000 times higher than their Ki values for the binding sites in vitro. In pharmacologically active doses sodium pentobarbital, strychnine, picrotoxin and bicuculline fail to influence [3H]flunitrazepam binding in vivo.

Original languageEnglish (US)
Pages (from-to)213-218
Number of pages6
JournalEuropean Journal of Pharmacology
Issue number2
StatePublished - Mar 15 1978


  • Benzodiazepine
  • Diazepam
  • Flunitrazepam
  • Pentobarbital
  • Receptor

ASJC Scopus subject areas

  • Pharmacology


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