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• W1996215570 abstract "To elucidate which portions of the opioid receptor molecules are involved in the ligand selectivity, we have expressed chimeric receptors between the rat δ- and μ-opioid receptors from cDNAs and analyzed their ligand binding properties. We demonstrate that the major binding determinant for the δ-selective enkephalin-related peptide, [D-Pen2,D-Pen5]enkephalin, resides within the region comprising the transmembrane segments V-VII and the intervening loop regions. On the other hand, the region spanning from the intracellular loop I to the amino-terminal half of the transmembrane segment III is shown to be involved in determining high-affinity binding of the μ-selective enkephalin-related peptides, [D-Ala2,MePhe4,Gly-ol5]enkephalin and [D-Ala2,MePhe4,Met-ol5]enkephalin, whereas the major determinant for binding of the μ-selective alkaloids, morphine and codeine, is demonstrated to exist in the region spanning the transmembrane segments V-VII. These results indicate that distinct regions of the opioid receptor determine the selectivity for the δ- and the μ-selective enkephalin-related peptides and that the binding determinant for the μ-selective alkaloids is distinct from that for the μ-selective enkephalin-related peptides. To elucidate which portions of the opioid receptor molecules are involved in the ligand selectivity, we have expressed chimeric receptors between the rat δ- and μ-opioid receptors from cDNAs and analyzed their ligand binding properties. We demonstrate that the major binding determinant for the δ-selective enkephalin-related peptide, [D-Pen2,D-Pen5]enkephalin, resides within the region comprising the transmembrane segments V-VII and the intervening loop regions. On the other hand, the region spanning from the intracellular loop I to the amino-terminal half of the transmembrane segment III is shown to be involved in determining high-affinity binding of the μ-selective enkephalin-related peptides, [D-Ala2,MePhe4,Gly-ol5]enkephalin and [D-Ala2,MePhe4,Met-ol5]enkephalin, whereas the major determinant for binding of the μ-selective alkaloids, morphine and codeine, is demonstrated to exist in the region spanning the transmembrane segments V-VII. These results indicate that distinct regions of the opioid receptor determine the selectivity for the δ- and the μ-selective enkephalin-related peptides and that the binding determinant for the μ-selective alkaloids is distinct from that for the μ-selective enkephalin-related peptides." @default.
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• W1996215570 date "1995-03-01" @default.
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• W1996215570 title "Location of Regions of the Opioid Receptor Involved in Selective Agonist Binding" @default.
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• W1996215570 doi "https://doi.org/10.1074/jbc.270.12.6702" @default.
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