KNT-127 is a selective δ-opioid receptor (DOR) agonist that effectively crosses the blood-brain barrier (Ki = 0.16 nM). It demonstrates high selectivity for the δ receptor, with Ki values of 0.16 nM, 21.3 nM, and 153 nM for δ, μ, and κ receptors, respectively. As a biased ligand, KNT-127 primarily activates cyclic adenosine monophosphate (cAMP) signaling while exhibiting lower beta-arrestin signaling. This compound enhances the release of dopamine and L-glutamate in key brain regions, including the striatum, nucleus accumbens, and prefrontal cortex, and is relevant for studies on neurological diseases due to its antidepressant and anxiolytic-like effects.
KNT-127 is a selective δ-opioid receptor (DOR) agonist that effectively crosses the blood-brain barrier (Ki = 0.16 nM). It demonstrates high selectivity for the δ receptor, with Ki values of 0.16 nM, 21.3 nM, and 153 nM for δ, μ, and κ receptors, respectively. As a biased ligand, KNT-127 primarily activates cyclic adenosine monophosphate (cAMP) signaling while exhibiting lower beta-arrestin signaling. This compound enhances the release of dopamine and L-glutamate in key brain regions, including the striatum, nucleus accumbens, and prefrontal cortex, and is relevant for studies on neurological diseases due to its antidepressant and anxiolytic-like effects.
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