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Preparation and Binding Properties of Radioiodinated Analogues of Dermorphin and Deltorphin with High Specificity for the μ‐ and δ‐Opioid Receptors
Author(s) -
Gaudriault Georges,
Zsürger Nicole,
Vincent JeanPierre
Publication year - 1997
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1046/j.1471-4159.1997.68020813.x
Subject(s) - dermorphin , chemistry , receptor , opioid peptide , stereochemistry , opioid , peptide , biochemistry
The synthesis, purification, chemical characterization, and binding properties of two 125 I‐labeled analogues of dermorphin and deltorphin‐I are described. Native deltorphin‐I and [Lys 7 ]dermorphin sequences were elongated by an aminopentyl chain on their C‐terminal amide function and alkylated with the 125 I‐labeled monoiodinated derivative of Bolton‐Hunter reagent (BH * ). The resulting radiolabeled peptides, ε‐BH * [Lys 7 ]dermorphin 5‐aminopentylamide and ω‐BH * deltorphin‐I 5‐aminopentylamide, have kept most of the original properties of the parent peptides. They bind with high selectivity and specificity to the μ‐ (dermorphin analogue) or δ‐ (deltorphin‐I analogue) opioid receptors from rat brain or from cells transfected with cDNAs encoding the μ and δ receptors. The autoradiographic distribution of specific binding sites for the 125 I‐labeled dermorphin and deltorphin‐I analogues in rat brain is in complete agreement with previously reported localizations of μ‐ and δ‐opioid receptors. The two radiolabeled peptides are the best ligands of μ‐ and δ‐opioid receptors currently available in terms of sensitivity, specificity, and selectivity.