Posted by MB on May 11, 2003, at 2:22:54
In reply to Re: 5-HT2c Receptor, posted by Caleb462 on May 8, 2003, at 14:35:33
> > > When you take an SSRI, the 5-HT2c receptors become activated to a much greater degree due to all the excess serotonin, which means a larger inhibition of dopamine.
> >
> > Interesting. But how does serzone avoid hitting this receptor, is it even more selective? Does remeron hit this receptor? Are there any other seratonergic drugs that do not hit this receptor? Perhaps this explains why Celexa pooped out on me?? What do you think?
> >
> > JACK
> >
> >
>
> Serzone avoids this effect by also being a 5-HT2 antagonist. Meaning it blocks this receptor and prevents the widespread dopamine ihhibition that would otherwise occur if all the serotonin was allowed to bind to it. Remeron is also a 5-HT2 antagonist.
>
> As for why Celexa pooped out... who knows? But I do believe that SSRIs can induce a depressive state, that may or may not be different from the previous depressive state, by inhibiting dopamine release.
Serzone blocks 5HT-2a receptors, but one of its active metabolites is mCPP (metachlorophenylpiperazine) which is a 5HT-2c agonist. So you actually are getting some 5HT-2c agonism. Trazodone, Serzone's cousin, is also metabolized into the 5HT-2c agonist mCPP, which is why it has been tried as a treatment for weight gain induced by atypical antipsychotics (which are thought to induce weight gain not only by blocking H-1 receptors, but by blocking 5HT-2c receptors as well).Treating atypical AP weight gain with trazodone:
http://www.nimh.nih.gov/ncdeu/abstracts2001/ncdeu3080.cfmIt's Serzone's ability to block 5HT-2a receptors that keeps the dopamine levels from dropping, and why there are fewer incidences of akathisia with nefazodone:
http://www.antidepressantsfacts.com/07-2001-SSRI-Induced%20Akathisia.htmA great paper written on the different serotonin receptor subtypes and their functions can be found here:
http://www.biotrend.com/pdf/serot.pdfMB
poster:MB
thread:225001
URL: http://www.dr-bob.org/babble/20030505/msgs/225748.html