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Thoughts on 5HT1A antagonists?

Posted: Tue Sep 08, 2020 10:04 pm
by Matthias66
I've been looking a lot into 5HT1a antagonists, and how they have the strong potential to reverse sexual side effects, and reverse the desensitization of the autoreceptors of 5HT1a receptor sites:

5-HT1A receptor antagonism reverses and prevents fluoxetine-induced sexual dysfunction in rats:

https://academic.oup.com/ijnp/article/12/8/1045/677907

The 5-HT(1A) receptor antagonist robalzotan completely reverses citalopram-induced inhibition of serotonergic cell firing:

https://pubmed.ncbi.nlm.nih.gov/10528148/

There are a couple other articles I couldn't find, but seem to show a lot of promise in regards to 5HT1A antagonists, which from my understanding, similar to the SARI Trazodone, release more
Serotonin in the Post-Synaptic Cleft because of the blockage of the 5HT1A receptors.

The problem I am running into is that there are plenty of 5HT1A agonists, 5HT1A partial agonists, agonists of 5HT1B, 5HT1C, etc, but very few 5HT1a antagonists. Most are either discontinued or are experimental, and are not open for usage.

I hear good things about CBG oil as a medium strength 5HT1a antagonist.

Have you guys heard anything, or have any suggestions? I have a good feeling about this 5HT1a antagonist, but there needs to be more options for it.

Re: Thoughts on 5HT1A antagonists?

Posted: Wed Sep 09, 2020 2:51 am
by Thomas
https://en.wikipedia.org/wiki/5-HT1A_receptor
Cyproheptadine is frequently quoted here giving some relief (directly or with rebound) but having strong side effects.

Re: Thoughts on 5HT1A antagonists?

Posted: Wed Sep 09, 2020 4:03 am
by Thomas
Besides, some people had improvements with buspirone, which is a 5HT1A agonist.

Re: Thoughts on 5HT1A antagonists?

Posted: Wed Sep 09, 2020 4:48 am
by dann888
Thomas wrote: Wed Sep 09, 2020 4:03 am Besides, some people had improvements with buspirone, which is a 5HT1A antagonist.
Buspirone is an Agonist of 5ht1

Re: Thoughts on 5HT1A antagonists?

Posted: Wed Sep 09, 2020 8:26 am
by Thomas
Sorry, typo corrected

Re: Thoughts on 5HT1A antagonists?

Posted: Wed Sep 09, 2020 11:32 am
by Trazohell
Always the same discussions, we turn in circles...

Re: Thoughts on 5HT1A antagonists?

Posted: Thu Sep 10, 2020 5:02 pm
by capitalCK
Matthias66 wrote: Tue Sep 08, 2020 10:04 pm I've been looking a lot into 5HT1a antagonists, and how they have the strong potential to reverse sexual side effects, and reverse the desensitization of the autoreceptors of 5HT1a receptor sites:

5-HT1A receptor antagonism reverses and prevents fluoxetine-induced sexual dysfunction in rats:

https://academic.oup.com/ijnp/article/12/8/1045/677907

The 5-HT(1A) receptor antagonist robalzotan completely reverses citalopram-induced inhibition of serotonergic cell firing:

https://pubmed.ncbi.nlm.nih.gov/10528148/

There are a couple other articles I couldn't find, but seem to show a lot of promise in regards to 5HT1A antagonists, which from my understanding, similar to the SARI Trazodone, release more
Serotonin in the Post-Synaptic Cleft because of the blockage of the 5HT1A receptors.

The problem I am running into is that there are plenty of 5HT1A agonists, 5HT1A partial agonists, agonists of 5HT1B, 5HT1C, etc, but very few 5HT1a antagonists. Most are either discontinued or are experimental, and are not open for usage.

I hear good things about CBG oil as a medium strength 5HT1a antagonist.

Have you guys heard anything, or have any suggestions? I have a good feeling about this 5HT1a antagonist, but there needs to be more options for it.
I read that Lecozotan is a 5ht1-a antagonist but I don't know how to source it.

You mentioned CBG oil is also a 5ht1-a antagonist, so I wanted to thank you for that. That's rather easy to purchase!

Also, read that pindolol is a 5ht1a antagonist.

Re: Thoughts on 5HT1A antagonists?

Posted: Thu Sep 10, 2020 5:26 pm
by finities infinities
I'm also looking for a 5ht1a postsynaptic antagonist. But I can't find any herbal supplements that do.

Re: Thoughts on 5HT1A antagonists?

Posted: Thu Sep 10, 2020 11:01 pm
by capitalCK
finities infinities wrote: Thu Sep 10, 2020 5:26 pm I'm also looking for a 5ht1a postsynaptic antagonist. But I can't find any herbal supplements that do.
CBG (not CBD). Comes from Hemp plant, so it is herbal.

Re: Thoughts on 5HT1A antagonists?

Posted: Fri Sep 11, 2020 6:06 am
by Lokzo55
I am so SOOOO glad I found this thread.


I am a guy who can be CURED 6 hours after taking St. John's Wort Ze 117 extract.

I did a thread about it here:
https://raypeatforum.com/community/thre ... ine.33599/


NOW.... I am also a guy who gets CURED from a Cyproheptadine REBOUND.... That is, 1mg of cypro will make me NUMB and anhedonic, for 4 days. Then i get a miraculous rebound where I am cured.

So this means that my PSSD is very likely driven by the mofo 5-HT1A receptors. Because ALL MY ISSUES STARTED FROM ASHWAGANDHA. Ash desensitises the 5-ht1a.

So now that you mentioned CBG oil as a medium strength 5HT1a antagonist, this then means that if I respond to this, for SURE my issue is 5-HT1a.

I also get a window with ALCAR (Which is a 5-HT1A agonist... and then I crash).