Opiate agonists and antagonists discriminated by receptor binding in brain

Candace B. Pert, Gavril Pasternak, Solomon H Snyder

Research output: Contribution to journalArticle

Abstract

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
JournalScience
Volume182
Issue number4119
StatePublished - 1973

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Opiate Alkaloids
Opioid Receptors
Dihydromorphine
Brain
Naloxone
Sodium
Body Weight
Pharmacology
In Vitro Techniques

ASJC Scopus subject areas

  • General

Cite this

Opiate agonists and antagonists discriminated by receptor binding in brain. / Pert, Candace B.; Pasternak, Gavril; Snyder, Solomon H.

In: Science, Vol. 182, No. 4119, 1973, p. 1359-1361.

Research output: Contribution to journalArticle

Pert, CB, Pasternak, G & Snyder, SH 1973, 'Opiate agonists and antagonists discriminated by receptor binding in brain', Science, vol. 182, no. 4119, pp. 1359-1361.
Pert, Candace B. ; Pasternak, Gavril ; Snyder, Solomon H. / Opiate agonists and antagonists discriminated by receptor binding in brain. In: Science. 1973 ; Vol. 182, No. 4119. pp. 1359-1361.
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