Gaudriault G, Zsürger N, Vincent J P
Institut de Pharmacologie Moléculaire et Cellulaire, CNRS UPR 411-Université de Nice Sophia Antipolis, Valbonne, France.
J Neurochem. 1997 Feb;68(2):813-9. doi: 10.1046/j.1471-4159.1997.68020813.x.
The synthesis, purification, chemical characterization, and binding properties of two 125I-labeled analogues of dermorphin and deltorphin-I are described. Native deltorphin-I and [Lys7] dermorphin sequences were elongated by an aminopentyl chain on their C-terminal amide function and alkylated with the 125I-labeled monoiodinated derivative of Bolton-Hunter reagent (BH*). The resulting radiolabeled peptides, epsilon-BH* [Lys7] dermorphin 5-aminopentylamide and omega-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 mu- (dermorphin analogue) or delta- (deltorphin-I analogue) opioid receptors from rat brain or from cells transfected with cDNAs encoding the mu and delta receptors. The autoradiographic distribution of specific binding sites for the 125I-labeled dermorphin and deltorphin-I analogues in rat brain is in complete agreement with previously reported localizations of mu- and delta-opioid receptors. The two radiolabeled peptides are the best ligands of mu- and delta-opioid receptors currently available in terms of sensitivity, specificity, and selectivity.
本文描述了两种125I标记的皮啡肽和强啡肽-I类似物的合成、纯化、化学表征及结合特性。天然强啡肽-I和[Lys7]皮啡肽序列在其C末端酰胺功能上通过一个氨基戊基链进行延长，并与Bolton-Hunter试剂（BH*）的125I标记的单碘化衍生物进行烷基化反应。所得的放射性标记肽，即ε-BH*[Lys7]皮啡肽5-氨基戊酰胺和ω-BH*强啡肽-I 5-氨基戊酰胺，保留了母体肽的大部分原始特性。它们以高选择性和特异性与大鼠脑或转染了编码μ和δ受体cDNA的细胞中的μ-（皮啡肽类似物）或δ-（强啡肽-I类似物）阿片受体结合。125I标记的皮啡肽和强啡肽-I类似物在大鼠脑中特异性结合位点的放射自显影分布与先前报道的μ-和δ-阿片受体定位完全一致。就敏感性、特异性和选择性而言，这两种放射性标记肽是目前可用的μ-和δ-阿片受体的最佳配体。
