ICI-199,441 is a drug which acts as a potent and selective
κ-opioid agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...
, and has
analgesic
An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in s ...
effects.
It is a
biased agonist of the KOR, and is one of relatively few KOR ligands that is
G protein
G proteins, also known as guanine nucleotide-binding proteins, are a Protein family, family of proteins that act as molecular switches inside cells, and are involved in transmitting signals from a variety of stimuli outside a cell (biology), ...
-biased rather than
β-arrestin-biased.
See also
*
U-47700
*
U-50488
*
U-69,593
References
Acetamides
Biased ligands
Chloroarenes
Kappa-opioid receptor agonists
1-Pyrrolidinyl compounds
Synthetic opioids
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