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EN
Opioid receptors play the pain control function in the body. Most of the research is carried out to find the most effective analgesic. The earliest analgesic i s morphine, however, unfortunately it has many side effects [Mizoguchi H et al. 2003 J. Pharmacol Sci. 93 423]. At a later time dermorphin was discovered as another potent analgesic [Mont ecucchi P C et al. 1981 Int. J. Pept. Protein Res. 17 275]. Unfortunately, this peptide is not resistant to enzymatic metabolism [Kisara K et al. 1986 Br. J. Pharmacol. 87 183; Sasaki Y et al. 1985 Neuropeptides 5 391]. The objective of this study is to search for new opioid analgesics by in vestigation of interactions between dermorphin analogs and the μ -opioid receptor using molecular modeling methods. MOPR ( μ -Opioid Peptide Receptor) complexes with several ligands (with kno wn biological activity) were modeled to explain how the structure of the complex was related to the biological activity. The investigated dermorphin analogs containing [ DMT 1 , D -Arg 2 ] (especially tetrapeptides) may become a good alternative for the currently used an algesics.
EN
Opioid peptides recently attracted much attention as low molecular weight compounds, which can target malignant cells expressing opioid receptors on their cell surface. Therefore opioid peptides have a potential to be introduced as radiopharmaceuticals. In this paper, we describe the method of conjugation of two bifunctional chelating agents (BFCAs), hydrazinopyridine-3-carboxylic acid (HYNIC) and 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid (DOTA), to the N-terminal amino group of morphiceptin, endomorphin-2, and two of their analogs modified in position 3. GABA was used as a spacer molecule. mi-Opioid binding affinities of the peptides were compared with the binding affinities of BFCA-GABA-peptide conjugates. It was shown that the introduction of HYNIC to mi-opioid ligands causes only a slight decrease of -opioid receptor affinity, while DOTA-conjugates loose their affinity for mi-receptors completely.
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