Sunobinop (S 117957, IMB 115) 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 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 displays competitive antagonist properties in specific signaling pathways, such as beta-arrestin 2 recruitment. With these unique pharmacological properties, Sunobinop can be used to investigate insomnia, moderate-to-severe alcohol use disorder, and urinary incontinence caused by overactive bladder[1][2].
Molecular Weight:
435.56
CAS Number:
[1126793-40-5]
Formula:
C26H33N3O3
Target:
Opioid Receptor
Application Notes:
MCE Product type: Reference compound
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