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...
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Autor*in:	Justyna Piekielna-Ciesielska [verfasserIn] Adriano Mollica [verfasserIn] Stefano Pieretti [verfasserIn] Jakub Fichna [verfasserIn] Agata Szymaszkiewicz [verfasserIn] Marta Zielińska [verfasserIn] Radzisław Kordek [verfasserIn] Anna Janecka [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2018

Schlagwörter:	Blood–brain barrier permeability hot-plate test anti-nociceptive and anti-inflammatory activity colitis induction myeloperoxidase activity

Übergeordnetes Werk:	In: Journal of Enzyme Inhibition and Medicinal Chemistry - Taylor & Francis Group, 2017, 33(2018), 1, Seite 560-566
Übergeordnetes Werk:	volume:33 ; year:2018 ; number:1 ; pages:560-566

Links:	Link aufrufen Link aufrufen Link aufrufen Journal toc Journal toc

DOI / URN:	10.1080/14756366.2018.1441839

Katalog-ID:	DOAJ048104302

Internformat


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spelling	10.1080/14756366.2018.1441839 doi (DE-627)DOAJ048104302 (DE-599)DOAJ9d8be7976dd248ffb836d7e2a503beb2 DE-627 ger DE-627 rakwb eng RM1-950 Justyna Piekielna-Ciesielska verfasserin aut Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2 2018 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier 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. Blood–brain barrier permeability hot-plate test anti-nociceptive and anti-inflammatory activity colitis induction myeloperoxidase activity Therapeutics. Pharmacology Adriano Mollica verfasserin aut Stefano Pieretti verfasserin aut Jakub Fichna verfasserin aut Agata Szymaszkiewicz verfasserin aut Marta Zielińska verfasserin aut Radzisław Kordek verfasserin aut Anna Janecka verfasserin aut In Journal of Enzyme Inhibition and Medicinal Chemistry Taylor & Francis Group, 2017 33(2018), 1, Seite 560-566 (DE-627)330383906 (DE-600)2049579-1 14756374 nnns volume:33 year:2018 number:1 pages:560-566 https://doi.org/10.1080/14756366.2018.1441839 kostenfrei https://doaj.org/article/9d8be7976dd248ffb836d7e2a503beb2 kostenfrei http://dx.doi.org/10.1080/14756366.2018.1441839 kostenfrei https://doaj.org/toc/1475-6366 Journal toc kostenfrei https://doaj.org/toc/1475-6374 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_39 GBV_ILN_40 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2031 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2057 GBV_ILN_2061 GBV_ILN_2111 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 33 2018 1 560-566
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allfieldsGer	10.1080/14756366.2018.1441839 doi (DE-627)DOAJ048104302 (DE-599)DOAJ9d8be7976dd248ffb836d7e2a503beb2 DE-627 ger DE-627 rakwb eng RM1-950 Justyna Piekielna-Ciesielska verfasserin aut Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2 2018 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier 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. Blood–brain barrier permeability hot-plate test anti-nociceptive and anti-inflammatory activity colitis induction myeloperoxidase activity Therapeutics. Pharmacology Adriano Mollica verfasserin aut Stefano Pieretti verfasserin aut Jakub Fichna verfasserin aut Agata Szymaszkiewicz verfasserin aut Marta Zielińska verfasserin aut Radzisław Kordek verfasserin aut Anna Janecka verfasserin aut In Journal of Enzyme Inhibition and Medicinal Chemistry Taylor & Francis Group, 2017 33(2018), 1, Seite 560-566 (DE-627)330383906 (DE-600)2049579-1 14756374 nnns volume:33 year:2018 number:1 pages:560-566 https://doi.org/10.1080/14756366.2018.1441839 kostenfrei https://doaj.org/article/9d8be7976dd248ffb836d7e2a503beb2 kostenfrei http://dx.doi.org/10.1080/14756366.2018.1441839 kostenfrei https://doaj.org/toc/1475-6366 Journal toc kostenfrei https://doaj.org/toc/1475-6374 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_39 GBV_ILN_40 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2031 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2057 GBV_ILN_2061 GBV_ILN_2111 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 33 2018 1 560-566
allfieldsSound	10.1080/14756366.2018.1441839 doi (DE-627)DOAJ048104302 (DE-599)DOAJ9d8be7976dd248ffb836d7e2a503beb2 DE-627 ger DE-627 rakwb eng RM1-950 Justyna Piekielna-Ciesielska verfasserin aut Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2 2018 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier 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. Blood–brain barrier permeability hot-plate test anti-nociceptive and anti-inflammatory activity colitis induction myeloperoxidase activity Therapeutics. Pharmacology Adriano Mollica verfasserin aut Stefano Pieretti verfasserin aut Jakub Fichna verfasserin aut Agata Szymaszkiewicz verfasserin aut Marta Zielińska verfasserin aut Radzisław Kordek verfasserin aut Anna Janecka verfasserin aut In Journal of Enzyme Inhibition and Medicinal Chemistry Taylor & Francis Group, 2017 33(2018), 1, Seite 560-566 (DE-627)330383906 (DE-600)2049579-1 14756374 nnns volume:33 year:2018 number:1 pages:560-566 https://doi.org/10.1080/14756366.2018.1441839 kostenfrei https://doaj.org/article/9d8be7976dd248ffb836d7e2a503beb2 kostenfrei http://dx.doi.org/10.1080/14756366.2018.1441839 kostenfrei https://doaj.org/toc/1475-6366 Journal toc kostenfrei https://doaj.org/toc/1475-6374 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_39 GBV_ILN_40 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2031 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2057 GBV_ILN_2061 GBV_ILN_2111 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 33 2018 1 560-566
language	English
source	In Journal of Enzyme Inhibition and Medicinal Chemistry 33(2018), 1, Seite 560-566 volume:33 year:2018 number:1 pages:560-566
sourceStr	In Journal of Enzyme Inhibition and Medicinal Chemistry 33(2018), 1, Seite 560-566 volume:33 year:2018 number:1 pages:560-566
format_phy_str_mv	Article
institution	findex.gbv.de
topic_facet	Blood–brain barrier permeability hot-plate test anti-nociceptive and anti-inflammatory activity colitis induction myeloperoxidase activity Therapeutics. Pharmacology
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container_title	Journal of Enzyme Inhibition and Medicinal Chemistry
authorswithroles_txt_mv	Justyna Piekielna-Ciesielska @@aut@@ Adriano Mollica @@aut@@ Stefano Pieretti @@aut@@ Jakub Fichna @@aut@@ Agata Szymaszkiewicz @@aut@@ Marta Zielińska @@aut@@ Radzisław Kordek @@aut@@ Anna Janecka @@aut@@
publishDateDaySort_date	2018-01-01T00:00:00Z
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callnumber-first	R - Medicine
author	Justyna Piekielna-Ciesielska
spellingShingle	Justyna Piekielna-Ciesielska misc RM1-950 misc Blood–brain barrier permeability misc hot-plate test misc anti-nociceptive and anti-inflammatory activity misc colitis induction misc myeloperoxidase activity misc Therapeutics. Pharmacology Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2
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topic_title	RM1-950 Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2 Blood–brain barrier permeability hot-plate test anti-nociceptive and anti-inflammatory activity colitis induction myeloperoxidase activity
topic	misc RM1-950 misc Blood–brain barrier permeability misc hot-plate test misc anti-nociceptive and anti-inflammatory activity misc colitis induction misc myeloperoxidase activity misc Therapeutics. Pharmacology
topic_unstemmed	misc RM1-950 misc Blood–brain barrier permeability misc hot-plate test misc anti-nociceptive and anti-inflammatory activity misc colitis induction misc myeloperoxidase activity misc Therapeutics. Pharmacology
topic_browse	misc RM1-950 misc Blood–brain barrier permeability misc hot-plate test misc anti-nociceptive and anti-inflammatory activity misc colitis induction misc myeloperoxidase activity misc Therapeutics. Pharmacology
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title	Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2
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title_full	Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2
author_sort	Justyna Piekielna-Ciesielska
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author_browse	Justyna Piekielna-Ciesielska Adriano Mollica Stefano Pieretti Jakub Fichna Agata Szymaszkiewicz Marta Zielińska Radzisław Kordek Anna Janecka
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author-letter	Justyna Piekielna-Ciesielska
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title_sort	antinociceptive potency of a fluorinated cyclopeptide dmt-c[d-lys-phe-p-cf3-phe-asp]nh2
callnumber	RM1-950
title_auth	Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2
abstract	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.
abstractGer	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.
abstract_unstemmed	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.
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title_short	Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2
url	https://doi.org/10.1080/14756366.2018.1441839 https://doaj.org/article/9d8be7976dd248ffb836d7e2a503beb2 http://dx.doi.org/10.1080/14756366.2018.1441839 https://doaj.org/toc/1475-6366 https://doaj.org/toc/1475-6374
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author2	Adriano Mollica Stefano Pieretti Jakub Fichna Agata Szymaszkiewicz Marta Zielińska Radzisław Kordek Anna Janecka
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up_date	2024-07-03T15:57:17.587Z
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Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2

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