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ICI-199,441

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
ICI-199,441
Identifiers
  • 2-(3,4-dichlorophenyl)-N-methyl-N-[(1S)-1-phenyl-2-pyrrolidin-1-ylethyl]acetamide
CAS Number
PubChemCID
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
 ☒NcheckY (what is this?)  (verify)

ICI-199,441 is a drug which acts as a potent and selectiveκ-opioidagonist, and hasanalgesic effects.[1][2] It is abiased agonist of the KOR, and is one of relatively few KOR ligands that isG protein-biased rather thanβ-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):475–478.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.
μ-opioid
(MOR)
Agonists
(abridged;
full list)
Antagonists
δ-opioid
(DOR)
Agonists
Antagonists
κ-opioid
(KOR)
Agonists
Antagonists
Nociceptin
(NOP)
Agonists
Antagonists
Others


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