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

• Main Authors: Adriano Mollica (Author), Sveva Pelliccia (Author), Valeria Famiglini (Author), Azzurra Stefanucci (Author), Giorgia Macedonio (Author), Annalisa Chiavaroli (Author), Giustino Orlando (Author), Luigi Brunetti (Author), Claudio Ferrante (Author), Stefano Pieretti (Author), Ettore Novellino (Author), Sandor Benyhe (Author), Ferenc Zador (Author), Anna Erdei (Author), Edina Szucs (Author), Reza Samavati (Author), Szabolcs Dvorácskó (Author), Csaba Tomboly (Author), Rino Ragno (Author), Alexandros Patsilinakos (Author), Romano Silvestri (Author)
• Format: Book
• Published: Taylor & Francis Group, 2017-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Summary

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-NH2. 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.

Item Description

1475-6366
1475-6374
10.1080/14756366.2016.1260565