Properties of opiate receptor binding in rat brain

C. B. Pert; S. H. Snyder

doi:10.1073/pnas.70.8.2243

Properties of opiate receptor binding in rat brain

C. B. Pert, S. H. Snyder

School of Medicine

Research output: Contribution to journal › Article › peer-review

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	https://doi.org/10.1073/pnas.70.8.2243
State	Published - 1973

ASJC Scopus subject areas

General

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AB - [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.

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