Properties of opiate receptor binding in rat brain

C. B. Pert, S. H. Snyder

Research output: Contribution to journalArticlepeer-review

Abstract

[3H]Naloxone, a potent opiate antagonist, binds stereospecifically to opiate receptor sites in rat brain tissue. The binding is time, temperature, and pH dependent and saturable with respect to [3H]naloxone and tissue concentration. The [3H]naloxone receptor complex formation is bimolecular with a dissociation constant of 20 nM. 15 opiate agonists and antagonists compete for the same receptors, whose density is 30 pmol/g. Potencies of opiates and their antagonists in displacing [3H]naloxone binding parallel their pharmacological potencies.

Original languageEnglish (US)
Pages (from-to)2243-2247
Number of pages5
JournalProceedings of the National Academy of Sciences of the United States of America
Volume70
Issue number8
DOIs
StatePublished - 1973

ASJC Scopus subject areas

  • General

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