Related Experiment Video
Updated: May 13, 2025

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
In vitro pharmacological evaluation of the novel NOP receptor partial agonist sunobinop
Riccardo Camilotto1, Davide Malfacini1, Pietro Pola2
1Department of Pharmaceutical and Pharmacological Sciences, Section of Pharmacology, University of Padova, Padova, Italy.
None:
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.
More Related Videos
Related Concept Videos
Drug-Receptor Interaction: Agonist
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous...
Opioid Receptors: Overview
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists
Drug-Receptor Interaction: Antagonist
Antagonists can be classified as competitive or noncompetitive based on their...
Drug-Receptor Interactions
Several parameters, such as the drug's affinity for its receptor and its efficacy, which is its ability to activate the receptor, determine the drug's effect on the tissue....

