5HT2C antagonism, is it a good idea?

[Neuroprotection]

hi all.
Just started reading about the 5HT2C receptor which seems to be important in human mood and behaviour regulation. due to its higher affinity for many psychedelic drugs, it is likely this receptor plays a very important role in the overall psychedelic experience, probably not the hallucinations but maybe mood changes?
5HT2C’s main function is thought to be the suppression of dopamine release in certain areas of the brain.
Interestingly, many antidepressants block or downregulate 5HT2C receptors, as do the atypical antipsychotics. this leads to an antidepressant, anxieolitic and mood elevating effect of these medications.

I’m just wondering about the feasibility of very powerful and highly selective antagonist of this receptor in human therapy, for example in depression and anxiety disorders as well as general chronic stress.
Please share your thoughts on why this may be a good or bad idea.

 

[lightsup]

I guess we have to wait for A.I. to design the molecule from the ki value.

 

[MedicinalUser247]

If your really interested in 5-HT2c antagonism take a look at drugs such as Deramciclane and SB-243213.

 

[MedicinalUser247]

https://en.wikipedia.org/wiki/SB-243213

https://en.wikipedia.org/wiki/Deramciclane

 

[Neuroprotection]

thanks to everyone who posted so far. just wondered if anyone has any thoughts on the biological/medical implications of 5HT2C blockade.
I get the point about challenges making selective antagonists, but I would advise leaving drug chemistry out of any further discussions on this thread unless it is briefly referenced to support someone’s Pacific point. I say this because on many of my threads, drug chemistry seems to get all the attention and divert the discussion away from the biological orientated topic of the thread. I do admire those who can go deep into drug chemistry and discuss it, but it just boggles my mind and is usually irrelevant to my topic

 

[Neuroprotection]

Lorcaserin, A 5-HT2C Receptor Agonist, Reduces Body Weight by Decreasing Energy Intake without Influencing Energy Expenditure

Lorcaserin, a selective 5-HT[2C] receptor agonist, reduces body weight through its effects on food intake and appetite, not energy expenditure or substrate oxidation.Lorcaserin, a selective 5-hydroxytryptamine (5-HT)[2C] receptor agonist, reduces body ...

www.ncbi.nlm.nih.gov