ICI-199,441

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]

ICI-199,441
Identifiers
  • 2-(3,4-dichlorophenyl)-N-methyl-N-[(1S)-1-phenyl-2-pyrrolidin-1-ylethyl]acetamide
CAS Number
PubChem CID
IUPHAR/BPS
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
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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): 475–478. doi:10.1016/0014-2999(88)90546-8. PMID 2850924.
  2. Narita M, Kaneko C, Miyoshi K, Nagumo Y, Kuzumaki N, Nakajima M, et al. (April 2006). "Chronic pain induces anxiety with concomitant changes in opioidergic function in the amygdala". Neuropsychopharmacology. 31 (4): 739–750. doi:10.1038/sj.npp.1300858. PMID 16123756.
  3. DiMattio KM, Ehlert FJ, Liu-Chen LY (August 2015). "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. doi:10.1016/j.ejphar.2015.05.054. PMC 4532598. PMID 26057692.
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