4 ms·
Buprenorphine is a partial agonist of the Mu receptor (the one which causes the most physical dependency) and is antagonist for the rest, it’s also has a very h
by dogma1138 8y ago
Buprenorphine is a partial agonist of the Mu receptor (the one which causes the most physical dependency) and is antagonist for the rest, it’s also has a very high affinity which displaces other opioids which is why it’s used in addiction treatment.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2581407/ https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2581407/
Yes is more to this than just affinity the type and level of the binding to each receptor is also important but on the grand scheme of things in this context it’s not because all the opioids which are primarily used for pain relief are full Mu receptor agonists which is when the simple affinity strength estimate is pretty much sufficient to estimate potency and potential harm.
Also last time I checked the potency is derived directly from the Ki value of the Mu receptor which represents the affinity (regardless of agonism) of the opioid, so these are essentially interchangeable.