| |
| 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 | |
3D model (
JSmol)
|
|
PubChem
CID
|
|
| |
| |
| Properties | |
| 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).
| |
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 GABAA 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.
 | This article about an organic compound is a stub. You can help Wikipedia by expanding it. |
|
| |
| 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 | |
3D model (
JSmol)
|
|
PubChem
CID
|
|
| |
| |
| Properties | |
| 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).
| |
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 GABAA 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.
|
| This article about an organic compound is a stub. You can help Wikipedia by expanding it. |