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. 1973 Jul;70(7):1947–1949. doi: 10.1073/pnas.70.7.1947

Stereospecific Binding of the Potent Narcotic Analgesic [3H]Etorphine to Rat-Brain Homogenate

Eric J Simon 1, Jacob M Hiller 1, Irit Edelman 1
PMCID: PMC433639  PMID: 4516196

Abstract

Etorphine, the most potent narcotic analgesic known, was labeled with tritium by catalytic exchange. This drug exhibits stereospecific, saturable binding to rat-brain homogenate. At saturation, the stereospecific binding is 0.1-0.15 pmol/mg of protein. Specific binding is inhibited high salt concentrations, sulfhydryl reagents, and proteolytic enzymes, but is unaffected by phospholipases A and C, sodium azide, sodium fluoride, and prostaglandins E1 and E2. Competition for binding of [3H]etorphine correlates with agonist and antagonist potencies. The stable, stereospecific binding of an active narcotic analgesic supports the existence of opiate receptors.

Keywords: opiate receptor, morphine, antagonist

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1949

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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