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Exploring the first Rimonabant analog-opioid peptide hybrid compound, as bivalent ligand for CB1 and opioid receptors

Cannabinoid (CB) and opioid systems are both involved in analgesia, food intake, mood and behavior. Due to the co-localization of µ-opioid (MOR) and CB1 receptors in various regions of the central nervous system (CNS) and their ability to form heterodimers, bivalent ligands targeting to both these s...

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Autores principales: Mollica, Adriano, Pelliccia, Sveva, Famiglini, Valeria, Stefanucci, Azzurra, Macedonio, Giorgia, Chiavaroli, Annalisa, Orlando, Giustino, Brunetti, Luigi, Ferrante, Claudio, Pieretti, Stefano, Novellino, Ettore, Benyhe, Sandor, Zador, Ferenc, Erdei, Anna, Szucs, Edina, Samavati, Reza, Dvorácskó, Szabolcs, Tomboly, Csaba, Ragno, Rino, Patsilinakos, Alexandros, Silvestri, Romano
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6009935/
https://www.ncbi.nlm.nih.gov/pubmed/28097916
http://dx.doi.org/10.1080/14756366.2016.1260565
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author Mollica, Adriano
Pelliccia, Sveva
Famiglini, Valeria
Stefanucci, Azzurra
Macedonio, Giorgia
Chiavaroli, Annalisa
Orlando, Giustino
Brunetti, Luigi
Ferrante, Claudio
Pieretti, Stefano
Novellino, Ettore
Benyhe, Sandor
Zador, Ferenc
Erdei, Anna
Szucs, Edina
Samavati, Reza
Dvorácskó, Szabolcs
Tomboly, Csaba
Ragno, Rino
Patsilinakos, Alexandros
Silvestri, Romano
author_facet Mollica, Adriano
Pelliccia, Sveva
Famiglini, Valeria
Stefanucci, Azzurra
Macedonio, Giorgia
Chiavaroli, Annalisa
Orlando, Giustino
Brunetti, Luigi
Ferrante, Claudio
Pieretti, Stefano
Novellino, Ettore
Benyhe, Sandor
Zador, Ferenc
Erdei, Anna
Szucs, Edina
Samavati, Reza
Dvorácskó, Szabolcs
Tomboly, Csaba
Ragno, Rino
Patsilinakos, Alexandros
Silvestri, Romano
author_sort Mollica, Adriano
collection PubMed
description Cannabinoid (CB) and opioid systems are both involved in analgesia, food intake, mood and behavior. Due to the co-localization of µ-opioid (MOR) and CB1 receptors in various regions of the central nervous system (CNS) and their ability to form heterodimers, bivalent ligands targeting to both these systems may be good candidates to investigate the existence of possible cross-talking or synergistic effects, also at sub-effective doses. In this work, we selected from a small series of new Rimonabant analogs one CB1R reverse agonist to be conjugated to the opioid fragment Tyr-D-Ala-Gly-Phe-NH(2). The bivalent compound (9) has been used for in vitro binding assays, for in vivo antinociception models and in vitro hypothalamic perfusion test, to evaluate the neurotransmitters release.
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spelling pubmed-60099352018-07-11 Exploring the first Rimonabant analog-opioid peptide hybrid compound, as bivalent ligand for CB1 and opioid receptors Mollica, Adriano Pelliccia, Sveva Famiglini, Valeria Stefanucci, Azzurra Macedonio, Giorgia Chiavaroli, Annalisa Orlando, Giustino Brunetti, Luigi Ferrante, Claudio Pieretti, Stefano Novellino, Ettore Benyhe, Sandor Zador, Ferenc Erdei, Anna Szucs, Edina Samavati, Reza Dvorácskó, Szabolcs Tomboly, Csaba Ragno, Rino Patsilinakos, Alexandros Silvestri, Romano J Enzyme Inhib Med Chem Short Communication Cannabinoid (CB) and opioid systems are both involved in analgesia, food intake, mood and behavior. Due to the co-localization of µ-opioid (MOR) and CB1 receptors in various regions of the central nervous system (CNS) and their ability to form heterodimers, bivalent ligands targeting to both these systems may be good candidates to investigate the existence of possible cross-talking or synergistic effects, also at sub-effective doses. In this work, we selected from a small series of new Rimonabant analogs one CB1R reverse agonist to be conjugated to the opioid fragment Tyr-D-Ala-Gly-Phe-NH(2). The bivalent compound (9) has been used for in vitro binding assays, for in vivo antinociception models and in vitro hypothalamic perfusion test, to evaluate the neurotransmitters release. Taylor & Francis 2017-01-18 /pmc/articles/PMC6009935/ /pubmed/28097916 http://dx.doi.org/10.1080/14756366.2016.1260565 Text en © 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. http://creativecommons.org/licenses/by/4.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Short Communication
Mollica, Adriano
Pelliccia, Sveva
Famiglini, Valeria
Stefanucci, Azzurra
Macedonio, Giorgia
Chiavaroli, Annalisa
Orlando, Giustino
Brunetti, Luigi
Ferrante, Claudio
Pieretti, Stefano
Novellino, Ettore
Benyhe, Sandor
Zador, Ferenc
Erdei, Anna
Szucs, Edina
Samavati, Reza
Dvorácskó, Szabolcs
Tomboly, Csaba
Ragno, Rino
Patsilinakos, Alexandros
Silvestri, Romano
Exploring the first Rimonabant analog-opioid peptide hybrid compound, as bivalent ligand for CB1 and opioid receptors
title Exploring the first Rimonabant analog-opioid peptide hybrid compound, as bivalent ligand for CB1 and opioid receptors
title_full Exploring the first Rimonabant analog-opioid peptide hybrid compound, as bivalent ligand for CB1 and opioid receptors
title_fullStr Exploring the first Rimonabant analog-opioid peptide hybrid compound, as bivalent ligand for CB1 and opioid receptors
title_full_unstemmed Exploring the first Rimonabant analog-opioid peptide hybrid compound, as bivalent ligand for CB1 and opioid receptors
title_short Exploring the first Rimonabant analog-opioid peptide hybrid compound, as bivalent ligand for CB1 and opioid receptors
title_sort exploring the first rimonabant analog-opioid peptide hybrid compound, as bivalent ligand for cb1 and opioid receptors
topic Short Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6009935/
https://www.ncbi.nlm.nih.gov/pubmed/28097916
http://dx.doi.org/10.1080/14756366.2016.1260565
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