Chemistry:ICI-199,441

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Short description: Chemical compound
ICI-199,441
ICI-199,441 Structure.svg
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC21H24Cl2N2O
Molar mass391.34 g·mol−1
3D model (JSmol)
 ☒N☑Y (what is this?)  (verify)

ICI-199,441 is a drug which acts as a potent and selective κ-opioid agonist, and has analgesic effects.[1][2] It is a biased agonist of the KOR, and is one of relatively few KOR ligands that is G protein-biased rather than β-arrestin-biased.[3]

See also

References

  1. "A novel series of potent and selective agonists at the opioid kappa-receptor". European Journal of Pharmacology 151 (3): 475–478. July 1988. doi:10.1016/0014-2999(88)90546-8. PMID 2850924. 
  2. "Chronic pain induces anxiety with concomitant changes in opioidergic function in the amygdala". Neuropsychopharmacology 31 (4): 739–750. April 2006. doi:10.1038/sj.npp.1300858. PMID 16123756. 
  3. "Intrinsic relative activities of κ opioid agonists in activating Gα proteins and internalizing receptor: Differences between human and mouse receptors". European Journal of Pharmacology 761: 235–244. August 2015. doi:10.1016/j.ejphar.2015.05.054. PMID 26057692.