Sunobinop is a selective partial agonist of the human nociceptin/orphanin FQ receptor (NOP), exhibiting high affinity for human targets (Ki=3.3 nM; EC50=4.03 nM; Emax=47.8%) while not engaging μ or κ opioid receptors. This compound significantly reduces wakefulness and enhances non-rapid eye movement sleep in rodent models, demonstrating a favorable side effect profile with no notable impacts on learning, memory, respiration, or intestinal function. Sunobinop also acts as a competitive antagonist in certain signaling pathways, particularly β-arrestin 2 recruitment, making it a valuable tool for research into conditions such as insomnia, alcohol use disorder, and overactive bladder-induced urinary incontinence.
Sunobinop is a selective partial agonist of the human nociceptin/orphanin FQ receptor (NOP), exhibiting high affinity for human targets (Ki=3.3 nM; EC50=4.03 nM; Emax=47.8%) while not engaging μ or κ opioid receptors. This compound significantly reduces wakefulness and enhances non-rapid eye movement sleep in rodent models, demonstrating a favorable side effect profile with no notable impacts on learning, memory, respiration, or intestinal function. Sunobinop also acts as a competitive antagonist in certain signaling pathways, particularly β-arrestin 2 recruitment, making it a valuable tool for research into conditions such as insomnia, alcohol use disorder, and overactive bladder-induced urinary incontinence.
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