Sunobinop TFA

Sunobinop (S 117957) TFA is an orally active and blood-brain barrier-penetrating selective partial agonist of the human nociceptin/orphanin FQ peptide receptor (NOP), with high affinity for human targets (Ki=3.3 nM; EC50=4.03 nM; Emax=47.8%), without activating μ and κ opioid receptors. In rats, Sunobinop TFA significantly reduces wakefulness and increases non-rapid eye movement (NREM) sleep through NOP receptor activation, without significant side effects on learning, memory, reward, respiration, or intestinal function at effective doses. It also displays competitive antagonist properties in certain signaling pathways [such as β-Arrestin 2 recruitment]. Sunobinop TFA can be employed in research involving insomnia, moderate to severe alcohol use disorder, and incontinence due to bladder overactivity.