Posted by PaulB on June 6, 2001, at 12:17:00
Hello, I am trying to find out more about the differences in the 5-HT2 antagonist properties of the similar antidepressants Nefazadone and Trazadone as I think it may be of relevance in regards to these drugs metabolite mCPP, 5-HT agonist
Nefazadone and Trazadone are both augmentors as well as antidepressants and when augmented with the popular SSRI's Paroxetine and Fluoxetine the levels of the metabolite mCPP can increase to a therapeutic level because the metabolising enzyme P450 CYP2D6 is potently inhibited by both these drugs. mCPP at higher levels would cause antidepressant/anxiolytic effects and 5-HT side-effects too.
What I wanted to find out is whether it is true that Nefazadone is a full antagonist at the 5-HT2 receptors and Trazadone blocks only 5-HT2a. If this were true Nefazadone may well block mCPP which is agonist at 5-HT2c and Trazadone wouldnt block mCPP from acting as an agonist at this particular receptor subtype.
poster:PaulB
thread:65545
URL: http://www.dr-bob.org/babble/20010605/msgs/65545.html