Comment · Sat, December 3, 2022 · ND Owner
Anybody Have a Clue What Ebelin Lactone’s 5-HT2A binding affinity is?
What they were answering
EchoingSimplicity · 3 points
Hey could you point me to any resources to educate myself on binding affinities? I have no context for those numbers, but they seem interesting.
u/MisterYouAreSoDumb · ND Owner
It's not a simple thing, as what makes a "good" (low, moderate, high) binding affinity differs between the various receptors and the actual function of the ligand. If it is a competitive agonist, then the binding affinity would have a lot more relevance, as it needs to displace the endogenous ligand from the active binding site. Too low of binding affinity, then it will never displace the endogenous ligand. However, ebelin lactone is an allosteric modulator. It doesn't need to displace the endogenous ligand from the active binding site to work. It binds allosterically to positively affect the activation by the endogenous ligand. Also, you can generally overcome moderate binding affinity by increasing the dose. Where something with a very high binding affinity might be active in the microgram range, something with a moderate affinity might be active in the milligram range. When it comes to pharmacodynamics and pharmacokinetics, it gets very complicated very quickly.