Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2
Opioid peptides and opiate drugs such as morphine, mediate their analgesic effects, but also undesired side effects, mostly through activation of the mu opioid receptor. However, delta- and kappa-opioid receptors can also contribute to the analgesic effects of opioids. Recent findings showed that si...
| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2018-01-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/14756366.2018.1441839 |
| _version_ | 1818338345201172480 |
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| author | Justyna Piekielna-Ciesielska Adriano Mollica Stefano Pieretti Jakub Fichna Agata Szymaszkiewicz Marta Zielińska Radzisław Kordek Anna Janecka |
| author_facet | Justyna Piekielna-Ciesielska Adriano Mollica Stefano Pieretti Jakub Fichna Agata Szymaszkiewicz Marta Zielińska Radzisław Kordek Anna Janecka |
| author_sort | Justyna Piekielna-Ciesielska |
| collection | DOAJ |
| description | Opioid peptides and opiate drugs such as morphine, mediate their analgesic effects, but also undesired side effects, mostly through activation of the mu opioid receptor. However, delta- and kappa-opioid receptors can also contribute to the analgesic effects of opioids. Recent findings showed that simultaneous activation of multiple opioid receptors may result in additional analgesia with fewer side effects. Here, we evaluated the pharmacological profile of our formerly developed mixed mu/kappa-opioid receptor ligands, Dmt-c[D-Lys-Phe-Phe-Asp]NH2 (C-36) and Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2 (F-81). The ability of these peptides to cross the blood–brain barrier was tested in the parallel artificial membrane permeability (PAMPA) assay. On the basis of the hot-plate test in mice after central and peripheral administration, analog F-81 was selected for the anti-nociceptive and anti-inflammatory activity assessment after peripheral administration. |
| first_indexed | 2024-12-13T15:09:38Z |
| format | Article |
| id | doaj.art-9d8be7976dd248ffb836d7e2a503beb2 |
| institution | Directory Open Access Journal |
| issn | 1475-6366 1475-6374 |
| language | English |
| last_indexed | 2024-12-13T15:09:38Z |
| publishDate | 2018-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Journal of Enzyme Inhibition and Medicinal Chemistry |
| spelling | doaj.art-9d8be7976dd248ffb836d7e2a503beb22022-12-21T23:40:55ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742018-01-0133156056610.1080/14756366.2018.14418391441839Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2Justyna Piekielna-Ciesielska0Adriano Mollica1Stefano Pieretti2Jakub Fichna3Agata Szymaszkiewicz4Marta Zielińska5Radzisław Kordek6Anna Janecka7Medical University of LodzUniversity “‘G. d’Annunzio”’ of Chieti-PescaraNational Center for Drug Research and EvaluationMedical University of LodzMedical University of LodzMedical University of LodzMedical University of LodzMedical University of LodzOpioid peptides and opiate drugs such as morphine, mediate their analgesic effects, but also undesired side effects, mostly through activation of the mu opioid receptor. However, delta- and kappa-opioid receptors can also contribute to the analgesic effects of opioids. Recent findings showed that simultaneous activation of multiple opioid receptors may result in additional analgesia with fewer side effects. Here, we evaluated the pharmacological profile of our formerly developed mixed mu/kappa-opioid receptor ligands, Dmt-c[D-Lys-Phe-Phe-Asp]NH2 (C-36) and Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2 (F-81). The ability of these peptides to cross the blood–brain barrier was tested in the parallel artificial membrane permeability (PAMPA) assay. On the basis of the hot-plate test in mice after central and peripheral administration, analog F-81 was selected for the anti-nociceptive and anti-inflammatory activity assessment after peripheral administration.http://dx.doi.org/10.1080/14756366.2018.1441839Blood–brain barrier permeabilityhot-plate testanti-nociceptive and anti-inflammatory activitycolitis inductionmyeloperoxidase activity |
| spellingShingle | Justyna Piekielna-Ciesielska Adriano Mollica Stefano Pieretti Jakub Fichna Agata Szymaszkiewicz Marta Zielińska Radzisław Kordek Anna Janecka Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2 Journal of Enzyme Inhibition and Medicinal Chemistry Blood–brain barrier permeability hot-plate test anti-nociceptive and anti-inflammatory activity colitis induction myeloperoxidase activity |
| title | Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2 |
| title_full | Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2 |
| title_fullStr | Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2 |
| title_full_unstemmed | Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2 |
| title_short | Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2 |
| title_sort | antinociceptive potency of a fluorinated cyclopeptide dmt c d lys phe p cf3 phe asp nh2 |
| topic | Blood–brain barrier permeability hot-plate test anti-nociceptive and anti-inflammatory activity colitis induction myeloperoxidase activity |
| url | http://dx.doi.org/10.1080/14756366.2018.1441839 |
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