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 to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ago ...
, and has
analgesic
An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It ...
effects.
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
Arrestins (abbreviated Arr) are a small family of proteins important for regulating signal transduction at G protein-coupled receptors.
Arrestins were first discovered as a part of a conserved two-step mechanism for regulating the activity of ...
-biased.
See also
*
U-47700
U-47700, also known as U4, pink heroin, pinky, and pink, is an opioid analgesic drug developed by a team at Upjohn in the 1970s which has around 7.5 times the potency of morphine in animal models.
U-47700 is a structural isomer of the earlier o ...
*
U-50488
U-50488 is a drug which acts as a highly selective κ-opioid agonist, but without any μ-opioid antagonist effects. It has analgesic, diuretic and antitussive effects, and reverses the memory impairment produced by anticholinergic
Anticholi ...
*
U-69,593
U-69,593 is a drug which acts as a potent and selective κ1-opioid receptor agonist. In animal studies it has been shown to produce antinociception, anti-inflammation, anxiolysis (at low doses), respiratory depression, and diuresis, while ...
References
Acetamides
Biased ligands
Chloroarenes
Kappa-opioid receptor agonists
Pyrrolidines
Synthetic opioids
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