Opiate agonists and antagonists discriminated by receptor binding in brain.

Receptor binding of opiate agonists and antagonists can be differentiated in vivo and in vitro. Administration of either rapidly elevates stereospecific [(3)H]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.