5-HT2a antagonist downregulation through internalization. How?

[Simfish]

It is known that 5-HT2a antagonists paradoxically downregulate the 5-HT2a receptor via a mechanism that I believe involves internalization and degradation. However, 5-HT2a inverse agonists apparently do not possess this unusual property. What is responsible for the difference?

 

[NeuroPsyence]

I can provide a fairly satisfactory answer to this, but I am too busy to type one up now. I will probably have some free time on Friday, so I'm going to bookmark this thread for now, but I will get back to you on this. FYI, the answer is very complex, and not 100% understood yet.

 

[Simfish]

Oh cool - thanks - I really appreciate it!

 

[Cortexiphan]

This is an excellent review on the subject

 

[NeuroPsyence]

My apologies for the delay. Time has not been a commodity I have had in abundance lately, but I still plan to provide what insight I can on this topic when I get a chance.