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. 1973 Aug;70(8):2243–2247. doi: 10.1073/pnas.70.8.2243

Properties of Opiate-Receptor Binding in Rat Brain

Candace B Pert 1,2,3,4, Solomon H Snyder 1,2,3,4,*
PMCID: PMC433710  PMID: 4525427

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.

Keywords: naloxone, opiate antagonist

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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