Sunobinop (S 117957) TFA is an orally active and blood-brain barrier-permeable selective partial agonist of the human nociceptin/orphanin FQ receptor (NOP), which exhibits high affinity for human targets (Ki=3.3 nM, EC50=4.03 nM, Emax=47.8%) without activating µ and kappa opioid receptors. Sunobinop TFA significantly reduces wakefulness time and increases non-rapid eye movement sleep in rats by activating NOP receptors, and produces no significant side effects on learning, memory, reward, respiration or intestinal function at effective doses. Sunobinop TFA displays competitive antagonist properties in specific signaling pathways, such as beta-arrestin 2 recruitment. With these unique pharmacological properties, Sunobinop TFA can be used to investigate insomnia, moderate-to-severe alcohol use disorder, and urinary incontinence caused by overactive bladder[1][2].
Molekulargewicht:
549.58
Reinheit:
98.26
Formel:
C28H34F3N3O5
Target-Kategorie:
Opioid Receptor
Anwendungsbeschreibung:
MCE Product type: Reference compound
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