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1346133-11-6

1346133-11-6 structure
1346133-11-6 structure
  • Name: LY2444296
  • Chemical Name: LY2444296
  • CAS Number: 1346133-11-6
  • Molecular Formula: C24H22F2N2O2
  • Molecular Weight: 408.44
  • Catalog: Signaling Pathways GPCR/G Protein Opioid Receptor
  • Create Date: 2020-01-23 16:39:51
  • Modify Date: 2024-01-10 18:00:45
  • LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects[1][2].

Name LY2444296
Synonyms MFCD32067413
Description LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects[1][2].
Related Catalog
Target

Ki: ~1 nM (KOPR)[1]

In Vivo LY2444296 displays anti-anxiety like effects in the EPM test[1]. LY2444296 (3 mg/kg; i.p.; 30 min before U69,593 administration) prevents behavioral and neuroendocrine effects caused by the reference kappa agonist U69,593 in cocaine-naïve rats[2]. LY2444296 reduces anxiety-like and depressive-like behaviors, as well as CORT release, in rats tested after chronic extended access cocaine self-administration, but not in cocaine-naïve rats[2]. Animal Model: Adult male Sprague Dawley rats (240–250 g)[2] Dosage: 3 mg/kg Administration: Injected intraperitoneally; 30 min before U69,593 administration Result: Prevented behavioral and neuroendocrine effects caused by U69,593 in cocaine-naïve rats.
References

[1]. Huang P, et al. Two short-acting kappa opioid receptor antagonists (zyklophin and LY2444296) exhibited different behavioral effects from the long-acting antagonist norbinaltorphimine in mouse anxiety tests. Neurosci Lett. 2016 Feb 26;615:15-20.

[2]. Valenza M, et al. "Effects of the novel relatively short-acting kappa opioid receptor antagonist LY2444296 in behaviors observed after chronic extended-access cocaine self-administration in rats". Psychopharmacology (Berl). 2017 Aug;234(15):2219-2231.

Molecular Formula C24H22F2N2O2
Molecular Weight 408.44
Hazard Codes Xi