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

Raymond S L Chang, Solomon H Snyder

Research output: Contribution to journalArticle

Abstract

[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
Volume48
Issue number2
DOIs
StatePublished - Mar 15 1978

Fingerprint

Flunitrazepam
GABA-A Receptors
Binding Sites
Strychnine
Picrotoxin
Bicuculline
Brain
Pentobarbital
Benzodiazepines
Occupations
Pharmacology
Injections
Membranes
Pharmaceutical Preparations
In Vitro Techniques

Keywords

  • Benzodiazepine
  • Diazepam
  • Flunitrazepam
  • Pentobarbital
  • Receptor

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Benzodiazepine receptors : labeling in intact animals with [3H] flunitrazepam. / Chang, Raymond S L; Snyder, Solomon H.

In: European Journal of Pharmacology, Vol. 48, No. 2, 15.03.1978, p. 213-218.

Research output: Contribution to journalArticle

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