Product Description: KNT-127 is a selective and BBB-penetrantδ-opioid receptor (DOR) agonist (Ki = 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[1][2][3][4][5].
Applications: Neuroscience-Neuromodulation
Formula: C24H24N2O2
References: [1]Nagase H, et al. Design and synthesis of KNT-127, a δ-opioid receptor agonist effective by systemic administration. Bioorg Med Chem Lett. 2010;20(21):6302-6305. /[2]Tanahashi S, et al. Novel δ1-receptor agonist KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens and median pre-frontal cortex. Neuropharmacology. 2012;62(5-6):2057-2067. /[3]Yoshioka T, et al. KNT-127, a selective delta opioid receptor agonist, shows beneficial effects in the hippocampal dentate gyrus of a chronic vicarious social defeat stress mouse model. Neuropharmacology. 2023 Jul 1;232:109511./[4]Bertels Z, et al. A non-convulsant delta-opioid receptor agonist, KNT-127, reduces cortical spreading depression and nitroglycerin-induced allodynia. Headache. 2021 Jan;61(1):170-178./[5]Yoshioka T, et al. Delta opioid receptor agonists activate PI3K-mTORC1 signaling in parvalbumin-positive interneurons in mouse infralimbic prefrontal cortex to exert acute antidepressant-lie effects. Mol Psychiatry. 2024 Dec 6.
CAS Number: 1256921-89-7
Molecular Weight: 372.46
Compound Purity: 99.60
Research Area: Neurological Disease
Solubility: DMSO : 25 mg/mL (ultrasonic)
Target: Opioid Receptor
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