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. 1973 Aug;70(8):2243-7.
doi: 10.1073/pnas.70.8.2243.

Properties of opiate-receptor binding in rat brain

C B Pert, S H Snyder

Properties of opiate-receptor binding in rat brain

C B Pert et al. 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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References

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