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. 1973 Jul;70(7):1947-9.
doi: 10.1073/pnas.70.7.1947.

Stereospecific binding of the potent narcotic analgesic (3H) Etorphine to rat-brain homogenate

E J Simon, J M Hiller, I Edelman

Stereospecific binding of the potent narcotic analgesic (3H) Etorphine to rat-brain homogenate

E J Simon et al. Proc Natl Acad Sci U S A. 1973 Jul.

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 E(1) and E(2). Competition for binding of [(3)H]etorphine correlates with agonist and antagonist potencies. The stable, stereospecific binding of an active narcotic analgesic supports the existence of opiate receptors.

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