Posted by mtdewcmu on April 7, 2011, at 20:48:20
In reply to Re: For serious 5ht2C-antagonism, LOW doses are needed, posted by desolationrower on April 7, 2011, at 17:28:14
> > 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.
poster:mtdewcmu
thread:982000
URL: http://www.dr-bob.org/babble/20110406/msgs/982216.html