In vitro pharmacological evaluation of the novel NOP receptor partial agonist sunobinop
Year: 2025
Type: article
Abstract: Sleep-related disorders affect a significant portion of the global population. The nociceptin/orphanin FQ (N/OFQ) peptide (NOP) receptor has become a promising candidate for the development of innovative drugs to treat sleep disorders. In this study, we conducted an in-depth pharmacological characterization of sunobinop, a selective NOP receptor partial agonist already under clinical evaluation for treating multiple conditions including insomnia, using a wide range of in vitro and ex vivo methodologies. Sunobinop exhibited partial agonist activity in calcium mobilization, NOP - G protein interaction, label-free bioimpedance, and cAMP inhibition assays. Notably, it demonstrated competitive antagonism in the NOP - β-Arrestin 2 recruitment and ex vivo electrically stimulated mouse Vas Deferens, assays characterized by low amplification. The findings reported here confirm and extend the characterization of sunobinop as a tool for studying NOP receptor pharmacology providing new insights into its mode of action, relevant to its clinical evaluation.
Source: Biochemical Pharmacology
Authors: Riccardo Camilotto, Davide Malfacini, Pietro Pola, Erika Morrone, Alessia Frezza, Rahul Ramalingam, Chiara Sturaro, Salvatore Pacifico, Chiara Ruzza, Remo Guerrini, Garth Whiteside, Girolamo Calo’
Institutions: University of Padua, University of Ferrara
Language: English
Subfield: Cellular and Molecular Neuroscience
Field: Neuroscience
Domain: Life Sciences
Open Access status: hybrid
Estimated APC paid: $3,590
Funders: Kaiser Permanente Division of Research, Ministero dell’Istruzione, dell’Università e della Ricerca, Università degli Studi di Padova, Università degli Studi di Ferrara, Dipartimento di Scienze Chimiche e Farmaceutiche, Università degli Studi di Ferrara, Ministero dell'Istruzione e del Merito
Award: G1224549619
OpenAlex ID: W4410237166