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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.

  1. ADLER T. K. Comparative potencies of codeine and its demethylated metabolites after intraventricular injection in the mouse. J Pharmacol Exp Ther. 1963 May;140:155–161. [PubMed] [Google Scholar]
  2. COX B. M., WEINSTOCK M. QUANTITATIVE STUDIES OF THE ANTAGONISM BY NALORPHINE OF SOME OF THE ACTIONS OF MORPHINE-LIKE ANALGESIC DRUGS. Br J Pharmacol Chemother. 1964 Apr;22:289–300. doi: 10.1111/j.1476-5381.1964.tb02034.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Cox B. M., Weinstock M. The effect of analgesic drugs on the release of acetylcholine from electrically stimulated guinea-pig ileum. Br J Pharmacol Chemother. 1966 May;27(1):81–92. doi: 10.1111/j.1476-5381.1966.tb01643.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Goldstein A., Lowney L. I., Pal B. K. Stereospecific and nonspecific interactions of the morphine congener levorphanol in subcellular fractions of mouse brain. Proc Natl Acad Sci U S A. 1971 Aug;68(8):1742–1747. doi: 10.1073/pnas.68.8.1742. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Grumbach L., Chernov H. I. The analgesic effect of opiate-opiate antagonist combinations in the rat. J Pharmacol Exp Ther. 1965 Sep;149(3):385–396. [PubMed] [Google Scholar]
  6. Hug C. C., Jr, Oka T. Uptake of dihydromorphine-3H by synaptosomes. Life Sci I. 1971 Feb 15;10(4):201–213. doi: 10.1016/0024-3205(71)90249-9. [DOI] [PubMed] [Google Scholar]
  7. JOHANNESSON T., SCHOU J. MORPHINE AND NORMORPHINE IN THE BRAINS OF RATS GIVEN IDENTICALLY ANALGAESIC DOSES OF MORPHINE, CODEINE OR NORMORPHINE. Acta Pharmacol Toxicol (Copenh) 1963;20:165–173. doi: 10.1111/j.1600-0773.1963.tb01733.x. [DOI] [PubMed] [Google Scholar]
  8. LASAGNA L. THE CLINICAL EVALUATION OF MORPHINE AND ITS SUBSTITUTES AS ANALGESICS. Pharmacol Rev. 1964 Mar;16:47–83. [PubMed] [Google Scholar]
  9. LOWRY O. H., ROSEBROUGH N. J., FARR A. L., RANDALL R. J. Protein measurement with the Folin phenol reagent. J Biol Chem. 1951 Nov;193(1):265–275. [PubMed] [Google Scholar]
  10. Martin W. R. Opioid antagonists. Pharmacol Rev. 1967 Dec;19(4):463–521. [PubMed] [Google Scholar]
  11. Navon S., Lajtha A. Uptake of morphine in particulate fractions from rat brain. Brain Res. 1970 Dec 18;24(3):534–536. doi: 10.1016/0006-8993(70)90193-9. [DOI] [PubMed] [Google Scholar]
  12. Pert C. B., Snyder S. H. Opiate receptor: demonstration in nervous tissue. Science. 1973 Mar 9;179(4077):1011–1014. doi: 10.1126/science.179.4077.1011. [DOI] [PubMed] [Google Scholar]
  13. Portoghese P. S. Stereochemical factors and receptor interactions associated with narcotic analgesics. J Pharm Sci. 1966 Sep;55(9):865–887. doi: 10.1002/jps.2600550902. [DOI] [PubMed] [Google Scholar]
  14. WOODS L. A. The pharmacology of nalorphine (N-allylnormorphine). Pharmacol Rev. 1956 Jun;8(2):175–198. [PubMed] [Google Scholar]

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