Abstract
[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) |
---|---|
Pages (from-to) | 2243-2247 |
Number of pages | 5 |
Journal | Proceedings of the National Academy of Sciences of the United States of America |
Volume | 70 |
Issue number | 8 |
DOIs | |
State | Published - 1973 |
ASJC Scopus subject areas
- General