Opiate agonists and antagonists discriminated by receptor binding in brain

Candace B. Pert, Gavril Pasternak, Solomon H. Snyder

Research output: Contribution to journalArticlepeer-review


Receptor binding of opiate agonists and antagonists can be differentiated in vivo and in vitro. Administration of either rapidly elevates stereospecific [3H]dihydromorphine binding to mouse brain extracts by 40 to 100 percent, but antagonists are 10 to 1000 times more potent than agonists; as little as 0.02 milligram of naloxone per kilogram of body weight significantly enhances opiate receptor binding. Sodium enhances antagonist binding in vitro but decreases agonist binding, a qualitative difference that may be relevant to the divergent pharmacological properties of opiate agonists and antagonists.

Original languageEnglish (US)
Pages (from-to)1359-1361
Number of pages3
Issue number4119
StatePublished - 1973

ASJC Scopus subject areas

  • General


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