[3H]Naloxone, a potent opiate antagonist, binds stereospecifically to opiate receptor sites in rat brain tissue. The binding is time, temperature, and pH dependent and saturable with respect to [3H]naloxone and tissue concentration. The [3H]naloxone receptor complex formation is bimolecular with a dissociation constant of 20 nM. 15 opiate agonists and antagonists compete for the same receptors, whose density is 30 pmol/g. Potencies of opiates and their antagonists in displacing [3H]naloxone binding parallel their pharmacological potencies.
|Original language||English (US)|
|Number of pages||5|
|Journal||Proceedings of the National Academy of Sciences of the United States of America|
|State||Published - 1973|
ASJC Scopus subject areas