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Synthesis and biological activity of N-methylated analogs of endomorphin-2 |
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| Authors: | Kruszynski Rafal Fichna Jakub do-Rego Jean-Claude Janecki Tomasz Kosson Piotr Pakulska Wanda Costentin Jean Janecka Anna |
| Affiliation: | aInstitute of General and Ecological Chemistry, Technical University of Lodz, Lodz, Poland bDepartment of Medicinal Chemistry, Medical University, Lodz, Poland cLaboratoire de Neuropsychopharmacologie Expérimentale, CNRS-FRE 2735, Université de Rouen, Rouen, France dInstitute of Organic Chemistry, Technical University of Lodz, Lodz, Poland eMedical Research Centre, Polish Academy of Sciences, Warsaw, Poland fDepartment of Pharmacodynamics, Medical University, Lodz, Poland |
| Abstract: | In this paper, we describe the synthesis of a series of endomorphin-2 analogs containing N-methylated amino acids, consecutively in each position. The μ-opioid receptor binding affinities of the new analogs were determined in the displacement experiments. Their in vivo antinociceptive activity was assessed in the hot-plate test in mice after central (icv) and peripheral (ip) administration. [Sar2]endomorphin-2, which had the highest μ-receptor affinity, also showed the strongest analgesic effect when administered centrally and was the only analog that retained activity after peripheral injection. |
| Keywords: | Antinociceptive activity Binding studies μ-Opioid receptor agonists |
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