ICI-199,441
Identifiers
  • 2-(3,4-dichlorophenyl)-N-methyl-N-[(1S)-1-phenyl-2-pyrrolidin-1-ylethyl]acetamide
CAS Number
  • 116508-24-8 checkY
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC21H24Cl2N2O
Molar mass391.34 g·mol−1
3D model (JSmol)
  • CN([C@H](CN1CCCC1)c2ccccc2)C(=O)Cc3ccc(c(c3)Cl)Cl
  • InChI=1S/C21H24Cl2N2O/c1-24(21(26)14-16-9-10-18(22)19(23)13-16)20(15-25-11-5-6-12-25)17-7-3-2-4-8-17/h2-4,7-10,13,20H,5-6,11-12,14-15H2,1H3/t20-/m1/s1 ☒N
  • Key:AEJOEPSMZCEYJN-HXUWFJFHSA-N ☒N
 ☒NcheckY (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 a relatively few KOR ligands that is G protein-biased rather than β-arrestin-biased.[3]

See also

References

  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.