1256921-89-7
Chemical Structure
KNT-127
- CAS No.: 1256921-89-7
- Formula:C24H24N2O2
- Molecular Weight:372.46
IUPAC Name: (6R,6aS,14aR)-17-methyl-5,6,7,14-tetrahydro-6aH-6,14a-(epiminoethano)naphtho[2,1-b]acridine-2,6a-diol
InChIKey: NFXFNBIPWUYEIM-WXFUMESZSA-N
SMILES: O[C@@]12[C@]3(CC4=NC5=CC=CC=C5C=C4C2)C6=CC(O)=CC=C6C[C@H]1N(CC3)C
Biological Activity: KNT-127 is a selective and BBB-penetrant δ-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].
| Cat. No. | Nom du produit | Pureté | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
KNT-127 | 99.11% | KNT-127 is a selective and BBB-penetrant δ-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. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. 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. [Content Brief]
- [2]. 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. [Content Brief]
- [3]. 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. [Content Brief]
- [4]. 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. [Content Brief]
- [5]. 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. [Content Brief]
