2. Academic Validation
  3. In vitro pharmacological evaluation of the novel NOP receptor partial agonist sunobinop

In vitro pharmacological evaluation of the novel NOP receptor partial agonist sunobinop

  • Biochem Pharmacol. 2025 Aug:238:116972. doi: 10.1016/j.bcp.2025.116972.
Riccardo Camilotto 1,  Davide Malfacini 2,  Pietro Pola 3,  Erika Morrone 1,  Alessia Frezza 3,  Rahul Ramalingam 1,  Chiara Sturaro 3,  Salvatore Pacifico 4,  Chiara Ruzza 5,  Remo Guerrini 6,  Garth Whiteside 7,  Girolamo Calo' 1
Affiliations

Affiliations

  • 1 Department of Pharmaceutical and Pharmacological Sciences, Section of Pharmacology, University of Padova, Padova, Italy.
  • 2 Department of Pharmaceutical and Pharmacological Sciences, Section of Pharmacology, University of Padova, Padova, Italy. Electronic address: davide.malfacini@unipd.it.
  • 3 Department of Neuroscience and Rehabilitation, University of Ferrara, Ferrara, Italy.
  • 4 Department of Chemical, Pharmaceutical and Agricultural Sciences, University of Ferrara, Ferrara, Italy.
  • 5 Department of Neuroscience and Rehabilitation, University of Ferrara, Ferrara, Italy; LTTA Laboratory for Advanced Therapies, Technopole of Ferrara 44121 Ferrara, Italy.
  • 6 Department of Chemical, Pharmaceutical and Agricultural Sciences, University of Ferrara, Ferrara, Italy; LTTA Laboratory for Advanced Therapies, Technopole of Ferrara 44121 Ferrara, Italy.
  • 7 Imbrium Therapeutics L.P., Stamford, CT, United States.
PMID: 40350096 DOI: 10.1016/j.bcp.2025.116972
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.

Keywords

GPCRs; In vitro pharmacology; NOP receptor; Sleep modulation; Sunobinop.

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