Posted by desolationrower on April 8, 2011, at 13:09:13
In reply to Re: For serious 5ht2C-antagonism, LOW doses are needed, posted by mtdewcmu on April 7, 2011, at 20:48:20
> > > Agomelatine is an effective 5HT2C-antagonist, right? Interestingly, the Ki value for agomelatine's binding affinity to the 5HT2C receptor is way higher than Prozac's: it's 710nM! (http://www.medicographia.com/html/static/html/issues/article_latest.asp?page=issues/99/art_10/p_2) This means that agomelatine's binding affinity for the 5HT2C-receptor is WWWWWWAAAYYYYYYYYYYY lower than fluoxetine's. It'd better be true that only a little antagonism of 5HT2C-receptors yields significant effects, or agomelatine's supposed 5HT2C-antagonism is a scam.
>
> The absolute value for Ki doesn't matter. It only matters what the Ki is relative to the Ki for the other receptors. You can compensate for a low binding affinity by increasing the dose, unless side effects or toxicity become significant.i think it does. The drug doesn't have to bind to a receptor, it can also just float around in your plasma.
I was just guessing based on the dose and bioavalibility and halflife values compared to other drugs. I think you can calculate it somehow, although i don't know if that is too reliable.
-d/r
Better living through chemistry, socialism, and big phallic rockets (with a side of roquette)
poster:desolationrower
thread:982000
URL: http://www.dr-bob.org/babble/20110406/msgs/982257.html