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KNT-127

中文

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Opioid

KNT-127
Names

IUPAC name (1R,14S,15R)-25-Methyl-4,25-diazahexacyclo[13.7.3.0^1,14.0^3,12.0^5,10.0^17,22]pentacosa-3,5,7,9,11,17(22),18,20-octaene-14,20-diol
Identifiers
CAS Number	1256921-89-7
3D model (JSmol)	Interactive image
ChEMBL	ChEMBL1270282
ChemSpider	26362663
PubChem CID	52942137
InChI InChI=1S/C24H24N2O2/c1-26-9-8-23-14-21-17(10-16-4-2-3-5-20(16)25-21)13-24(23,28)22(26)11-15-6-7-18(27)12-19(15)23/h2-7,10,12,22,27-28H,8-9,11,13-14H2,1H3/t22-,23-,24-/m1/s1 Key: NFXFNBIPWUYEIM-WXFUMESZSA-N
SMILES CN1CC[C@]23CC4=NC5=CC=CC=C5C=C4C[C@]2([C@H]1CC6=C3C=C(C=C6)O)O
Properties
Chemical formula	C₂₄H₂₄N₂O₂
Molar mass	372.468 g·mol⁻¹
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa). Infobox references

Chemical compound

KNT-127 is an opioid drugselective for thedelta opioid receptors.^[1] It might be used as ananalgesic andanxiolytic.

Potential uses

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KNT-127 can be used as an analgesic. In mice, it was able to reverse inflammatoryhyperalgesia.^[2]

Multiple tests have shown KNT-127 to be able to reduce anxiety,^[3] in a similar way tomuscimol,^[4] aGABA_A agonist.

Tolerance

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Chronic administration of KNT-127 created cross-tolerance to the analgesic effects ofSNC-80, another opioid.

References

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^Yoshioka, Toshinori; Yamada, Daisuke; Segi-Nishida, Eri; Nagase, Hiroshi; Saitoh, Akiyoshi (2023-07-01). "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.232 109511.doi:10.1016/j.neuropharm.2023.109511.ISSN 1873-7064.PMID 37001727.S2CID 257807312.
^Nozaki, C.; Nagase, H.; Nemoto, T.; Matifas, A.; Kieffer, B. L.; Gaveriaux-Ruff, C. (December 2014)."In vivo properties of KNT-127, a novel δ opioid receptor agonist: receptor internalization, antihyperalgesia and antidepressant effects in mice".British Journal of Pharmacology.171 (23):5376–5386.doi:10.1111/bph.12852.ISSN 1476-5381.PMC 4294046.PMID 25048778.
^Saitoh, Akiyoshi; Soda, Akinobu; Kayashima, Shuhei; Yoshizawa, Kazumi; Oka, Jun-Ichiro; Nagase, Hiroshi; Yamada, Mitsuhiko (November 2018)."A delta opioid receptor agonist, KNT-127, in the prelimbic medial prefrontal cortex attenuates glial glutamate transporter blocker-induced anxiety-like behavior in mice".Journal of Pharmacological Sciences.138 (3):176–183.doi:10.1016/j.jphs.2018.09.009.ISSN 1347-8648.PMID 30322803.
^Sugiyama, Azusa; Yamada, Misa; Saitoh, Akiyoshi; Nagase, Hiroshi; Oka, Jun-Ichiro; Yamada, Mitsuhiko (October 2018). "Administration of a delta opioid receptor agonist KNT-127 to the basolateral amygdala has robust anxiolytic-like effects in rats".Psychopharmacology.235 (10):2947–2955.doi:10.1007/s00213-018-4984-7.ISSN 1432-2072.PMID 30066134.S2CID 51887526.