KNT-127 is a selective and BBB-penetrant δ-opioid receptor (DOR) agonist ( K i = 0.16 nM). KNT-127 is highly selective to the δ receptor, with Ki values of 0.16, 21.3 and 153 nM for δ, μ and κ receptors, respectively. KNT-127 acts as a biased ligand that mainly activates cyclic adenosine monophosphate (cAMP) signaling with lower beta-arrestin signaling activation. KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens, and prefrontal cortex. KNT-127 exhibits antidepressant- and anxiolytic-like effects. KNT-127 can be studied in research on neurological diseases.
Products | Products > Disease Areas > Neurological, Eye or Ear Disease | Products > Signaling Pathways > GPCR/G Protein | Products > Signaling Pathways > Neuronal Signaling | Products > Research Areas > Neurological Disease | Products > Signaling Pathways > Opioid Receptor
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