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Ideas for 5-HT2a antagonists? They apparently have antidepressant props and play role in memory & cognition

cognition memory antidepressant cognition memory antidepressant

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#1 irony

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Posted 10 October 2021 - 02:55 AM

My psychiatrist has gotten interested in 5-HT2A antagonists lately.   I've read a couple paper summaries on them - seems like a lot of promise.


Problem is finding one.  Mirtazapine is a potent 5-HT2a antagonist, but it is pretty dirty, hits many other things.   The most "pure" one I could find is Pimavanserin but that's a very expensive drug with no generic and it's only approved for  Parkinson's problems.


I have searched around - my doc wants to try asenapine, but that has dopamine antagonism which causes nasty side-effects.


I've searched for others and didn't really come up with much.   Wondering if anyone had any ideas.



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#2 Galaxyshock

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Posted 11 October 2021 - 02:54 PM

Rather naive to pick one specific receptor and think it explains complex mental health issues.

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#3 irony

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Posted 13 October 2021 - 06:48 PM

Rather naive to pick one specific receptor and think it explains complex mental health issues.


to clarify, he wants to augment an SSRI with a 5-HT2a antagonist.

#4 DaveX

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Posted 31 October 2021 - 05:08 AM


I have no idea what psychiatrists and researchers are talking about with their prejudice against 5-HT2A receptors. It seems they can attach anything with a negative label and never need to explain themselves clearly or make sense. And they like to stay unclear about what they want to achieve with antagonism, just a nullification or a long-term upregulation. Even if it's the opposite, it is rarely deemed worth a remark (or an investigation on their own part).

I think if you try anything with a 5-HT2A antagonism, you will probably feel absolutely miserable while it's effective, with a strong feeling of relief and possibly improvement when it has worn off.


White Willow bark (Salix Alba) extract and Feverfew are two examples of strong natural 5-HT2A antagonists. Though Salix Alba also has 5-HT1D agonism, which dampens its effect a litte (not totally), and a much shorter half-life. After 3 or 4 hours one will probably feel fine, but a little down inbetween.

Feverfew is both an antagonist of 5-HT2A and 5-HT2B, and the latter seems to be its intended main effect. Nonethelss both of these natural agents feel fairly similar. Though Feverfew takes about 9 hours to wear off. It also has some other biochemical effects which may give one an "interesting" feeling (or aroused) before the end of 2 hours, but after that to the end of 9 hours it's misery. (At the end of it you might feel aroused again, just to take up that sidenote. Also overall relieved.)


I've tried Mirtazapine too, it's crap, simply crap.


The antagonism has nothing positive about it, nothing whatsoever, it hampers normal psychological functioning and makes one feel cranky, maybe even with pains and headache, and in dire need of some dopamine or happiness/equilibrium. It is a fundamental mechanism with a definite bias towards being positive rather than negative.

Edited by DaveX, 31 October 2021 - 05:13 AM.


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Posted 30 December 2021 - 12:39 PM

I am not completely sure of this. I thought  the antideprresent effect of microdosing  has to do with httting the 5-HT2A ?

#6 kurdishfella

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Posted 31 December 2021 - 08:28 AM

Why would you wanna block that receptor? That receptor is overactive in response to stress not that it is naturally overactivated which leads to stress. So if you have an overactive 5ht2a receptor it's because you are dealing with a lot of stress so it has to be active to deal with it and blocking it could make your mental health worse. its a symptom not the cause. Your brain system changes depending on how you think (you can live in a stressful environment but still not be stressed) and diet.

Edited by kurdishfella, 31 December 2021 - 08:34 AM.

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#7 Allostasist

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Posted 08 January 2022 - 04:27 PM

The only selective 5-HT2a antagonists to come to market are Lumateperone, Pimavanserin, and Pipamperone.

Pipamperone is the only accessible/affordable one because it came out in the 1960s. It was ahead of it's time (having no Dopamine D2 activity) and never made it out of the EU, and was kind of lost to history. You can get it prescribed in Germany, or order from GoldPharma.

At 5mg it's selective for 5-HT2a, after that D4 starts to kick in, then higher Alpha 1a, etc. Just stick with 5mg. Good for calming you down a bit, sleep, etc.

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