doi: 10.1073/pnas.70.8.2243.
Properties of opiate-receptor binding in rat brain
- PMID: 4525427
- PMCID: PMC433710
- DOI: 10.1073/pnas.70.8.2243
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Properties of opiate-receptor binding in rat brain
Proc Natl Acad Sci U S A.
1973 Aug.
Abstract
[(3)H]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 [(3)H]naloxone and tissue concentration. The [(3)H]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 [(3)H]naloxone binding parallel their pharmacological potencies.
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