KNT-127

KNT-127
Names
	IUPAC name (1R,14S,15R)-25-Methyl-4,25-diazahexacyclo[13.7.3.01,14.03,12.05,10.017,22]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;
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 CN1CCC23CC4=NC5=CC=CC=C5C=C4CC2(C1CC6=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 their standard state (at 25 °C [77 °F], 100 kPa). Infobox references

KNT-127 is an opioid drug selective for the delta opioid receptors.^[1] It might be used as an analgesic and anxiolytic.

Potential uses

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

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

Tolerance

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

References

^ 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.

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[1] 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.

[2] 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.

[3] 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.

[4] 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.

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