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Molecular Pharmacology, Vol 16, 91-104, Copyright © 1979 by the American Society for Pharmacology and Experimental Therapeutics
1 The Wellcome Research Laboratories, Research Triangle Park, N. C. 27709
In rat brain membrane preparations, the parenterally and orally active peptide, [D-Ala2, MePhe4, Met(O)5-ol]-enkephalin, binds to morphine receptor sites ([3H]naloxone or [3H]dihydromorphine binding sites) with an affinity higher than that for enkephalin receptor sites ([125I] [D-Ala2, D-Leu5]-enkephalin binding sites). [125I] [D-Ala2, MePhe4, Met(O)5-ol]-enkephalin binds to morphine receptor sites stereospecifically, in a saturable manner and with characteristics similar to that of [3H]dihydromorphine; this ligand can be used as an 125I-labeled probe to measure specific binding to morphine receptor sites. Na+ decreases and Mn2+ increases the binding capacity with a concomitant reduction of affinity for [125I] [D-Ala2, MePhe4, Met(O)5-ol]-enkephalin. This peptide does not bind to neuroblastoma cells with high affinity. The brain regional distribution of binding of [125I] [D-Ala2, MePhe4, Met(O)5-ol]-enkephalin or [3H]naloxone and [125I] [D-Ala2, D-Leu5]-enkephalin are different. The differential potency of binding of opiate agonists, antagonists, mixed agonist-antagonists, enkephalins and enkephalin analogues is studied by competition of binding of [3H]naloxone or [125I] [D-Ala2, MePhe4, Met(O)5-ol]-enkephalin (morphine receptor) and of [125I] [D-Ala2, D-Leu5]-enkephalin sites (enkephalin receptor). All of these results support the contention that there are multiple opiate receptors with differing characteristics.
Note:
ACKNOWLEDGMENT
We are grateful to Mark Collins for excellent technical assistance.
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