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of the µ-opioid receptor with a Kd value of 5.3 nM compared to 910 nM for the κ-opioid receptor and has around 7.5 x the potency of morphine in animal models.
tructural isomer of the earlie and the result of a great deal of work elucidating the quantitative structure–activity relationship of the scaffold.
Upjohn looked for the key moieties which gave the greatest activity and posted over a dozen patents on related compounds, each optimizing one moiety] until they discovere
U became the lead compound of selective kappa-opioid receptor ligands such as U-50488, U-51754 (containing a single methylene spacer difference) and U-69,593, which share very similar structures. Although not used medically, the selective kappa ligands are used in research.
is selective for the µ-opioid receptor, with various sources claiming 7.5x the potency of morphine.
Opioids exert their effects by binding to and activating the μ-opioid receptor. This occurs because opioids structurally mimic endogenous endorphins which are naturally found within the body and also work upon the μ-opioid receptor set.
The way in which opioids structurally mimic these natural endorphins results in their euphoria, pain relief and anxiolytic effects. This is because endorphins are responsible for reducing pain, causing sleepiness, and feelings of pleasure. They can be released in response to pain, strenuous exercise, orgasm, or general excitement.
U-4 may also be an agonist for the kappa-opioid receptor system. As a result of this, it has become the lead compound of selective kappa-receptor ligands such as , which share very similar structures. Its structure led to other chemists experimenting with it to see if rigid analogues would retain activity. Although not used medically, the selective kappa ligands are used in research.
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