ICI-199,441

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ICI-199,441
ICI-199441 structure.png
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC21H24Cl2N2O
Molar mass391.34 g·mol−1
3D model (JSmol)
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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 a relatively few KOR ligands that is G protein-biased rather than β-arrestin-biased.[3]

See also[edit]

References[edit]

  1. ^ Costello GF, Main BG, Barlow JJ, Carroll JA, Shaw JS (July 1988). "A novel series of potent and selective agonists at the opioid kappa-receptor". European Journal of Pharmacology. 151 (3): 475–8. doi:10.1016/0014-2999(88)90546-8. PMID 2850924.
  2. ^ Narita M, Kaneko C, Miyoshi K, Nagumo Y, Kuzumaki N, Nakajima M, Nanjo K, Matsuzawa K, Yamazaki M, Suzuki T (April 2006). "Chronic pain induces anxiety with concomitant changes in opioidergic function in the amygdala". Neuropsychopharmacology. 31 (4): 739–50. doi:10.1038/sj.npp.1300858. PMID 16123756.
  3. ^ DiMattio, Kelly M.; Ehlert, Frederick J.; Liu-Chen, Lee-Yuan (2015-08-15). "Intrinsic Relative Activities of Opioid Agonists in Activating Gα proteins and Internalizing Receptor: Differences between Human and Mouse Receptors". European Journal of Pharmacology. 761: 235–244. doi:10.1016/j.ejphar.2015.05.054. ISSN 0014-2999. PMC 4532598. PMID 26057692.