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Cyproheptadine - serotonin antagonist QUESTION

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1 Cyproheptadine - serotonin antagonist QUESTION on Thu May 19, 2016 11:57 pm

Austria


Hello area,

I have a question about Cyproheptadin.

As we can see on the wikipedia-page it antagonises many serotonin receptors, including 5ht1a, which is very good for pssd, but unfortunately it also blocks dopamine receptors, which isnt good for sexuality...

As you said at longevity,it wouldn't help much WHILE you take it.... but wouldn't the antagonisation of 5ht1a and the dopamine receptors eventually cause upregulation?
Couldn't it be that AFTER stopping the cyproheptadine the libido returns?

Thank you very much

Area-1255

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Austria wrote:Hello area,

I have a question about Cyproheptadin.

As we can see on the wikipedia-page it antagonises many serotonin receptors, including  5ht1a, which is very good for pssd, but unfortunately it also blocks dopamine receptors, which isnt good for sexuality...

It also is an anticholinergic, it antagonizes muscarinic acetylcholine receptors which can lead to heart problems in the long run, specifically fast heart rate and stress issues. I would avoid most of all anticholinergics in the long-run, they kill your memory as well.

http://www.ncbi.nlm.nih.gov/pubmed/15627436
http://www.drugbank.ca/drugs/DB00434
http://www.cvphysiology.com/Blood%20Pressure/BP010.htm
http://www.ncbi.nlm.nih.gov/pubmed/22222704
http://journal.frontiersin.org/article/10.3389/fnagi.2014.00063/full
Austria wrote:
but wouldn't the antagonisation of 5ht1a and the dopamine receptors eventually cause upregulation?
Not necessarily, no. Antagonism of a given receptor doesn't always result in the same effect.
There are other factors that come into play.
For example, whether the supposed 'antagonist' is actually an 'inverse agonist' or a 'true antagonist' also called a 'silent antagonist'.
For certain receptors there are what is 'irreversible inactivator' which means that the blockade effects last typically days or 1-2 weeks even after the drug is discontinued.
Risperidone (Risperdal) is an example of this, it blocks the serotonin 5-HT7 receptor irreversibly (one of the few good effects of that drug) and in doing so causes a relative anti-depressant effect (though the anti-dopamine effect often overrides that making it useless in most cases).


For receptor expression regulation, we have to consider the above but also which receptor is being targeted. Inverse agonists tend not to regulate transcription because they reduce constitutive activity at the receptor, which simply means they are actually causing the opposite effect or reversing the 'constitutive' effect of the receptor.
By inverting the effect we get the opposite G-protein effect.
So if a receptor being activated normally increases cyclic AMP (cAMP) then an inverse agonist would decrease cAMP, and vice versa.

cAMP links to the KREBS cycle in humans and animals, which happens to be the reason why certain drugs or supplements influence gene expression, often handles back to the cyclic adenosine-monophosphate/PKA pathway which then confers to the KREBS-energy cycle and this pathway recruits minerals like Zinc, Manganese, Magnesium, Chromium, Iron and Folate to invigorate or modulate the next system in the targeted pathway.

To answer your question more simply, no I don't think cyproheptadine would do this because it is a 'dirty drug' and targets many different receptors, we would want a 'clean' antagonist.

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Austria


As always, incredible knowledge, thank you
Same for mianserin, i guess, but how do you think louis syfer has permanent cured pssd? And I have seen 2 other men, zero and rdza to got their libido back with mianserin... It has to be worth a try?

Area-1255

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Austria wrote:As always, incredible knowledge,  thank you
Same for mianserin, i guess, but how do you think louis syfer has permanent cured pssd? And I have seen 2 other men, zero and rdza to got their libido back with mianserin... It has to be worth a try?

Mianserin has powerful antagonist actions at multiple serotonin subtypes, it's a very good medication. It also can boost memory. The only thing to be careful of is if you have norepinephrine excess or too much adrenaline, then I would avoid it. Also, it would not be good for someone with low histamine levels.

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1427877/
http://www.ncbi.nlm.nih.gov/pubmed/6282060
https://en.wikipedia.org/wiki/Mianserin#Pharmacology

It probably cured Mr.Louis Syfer by shifting the balance of dopamine:serotonin to the proper proportion.

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Austria


Area,I hope I get it right, mianserin doesn't increase serotonin, it decreases it an pushes norepinephrin and dopamine....  And when I look at wikipedia, it looks for me mianserin antagonises 5ht1a (1500 ki) also, is that right?
Then I could absolutely understand it's helping ability Smile

This study also saysthat it antagonises 5ht1a  I think :

http://www.sciencedirect.com/science/article/pii/0278584694900337

Would you generelly say mianserin increases sex drive?
I couldn't find much of experiences with mianserin...

But with mirtazapin,  which is only little different and there are many who say it decreases libido and some how get an increase in sex drive. Hmm

I somewhere read that with mianserin you only get raw dopamine and norepinephrine action and with mirtrazapin you get also serotonin action.

Can you may shed light on that please?

So my questions are:
1. Is mianserin a 5ht1a antagonist? (even if only a little)
2. Does mianserin increase libido?
3. What is the difference between mianserin and mirtazapin, and what is the better choice for sex drive?
4. Can you get pssd from mianserin amd mirtazapin?

Area, I am very thankful for everything you do for pssd sufferers... can you give me your email-adress? I want to send you a  voucher.

Area-1255

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Austria wrote:Area,I hope I get it right, mianserin doesn't increase serotonin, it decreases it an pushes norepinephrin and dopamine....  
Mianserin blocks multiple serotonin subtypes, that is correct, and it boosts dopamine and norepinephrine, but by different mechanisms. Mianserin essentially 'traps' the norepinephrine in synapse, leaving it active longer.

Austria wrote:
And when I look at wikipedia, it looks for me mianserin antagonises 5ht1a (1500 ki) also, is that right?
Then I could absolutely understand it's helping ability Smile
Yes, but it is stronger as an antagonist at 5-HT2A/2C.



Austria wrote:
Would you generelly say mianserin increases sex drive?
I couldn't find much of experiences with mianserin...
It does, yes.

Austria wrote:
But with mirtazapin,  which is only little different and there are many who say it decreases libido and some how get an increase in sex drive. Hmm
Mirtazapine is similar to mianserin, but lacks the NET inhibiting property, thus, it doesn't raise norepinephrine as much. Mirtazapine is hit or miss, it can boost sex drive for some users, others it decreases it. It does rapidly decrease cortisol, and is good for male bodybuilders.
Mirtazapine helps most, if it is combined with a 'true' 5-HT1A antagonist, and would be more valuable for PSSD sufferers, if there were 5-HT1A/1B antagonists available for us.

Arrow http://www.ncbi.nlm.nih.gov/pubmed/11965359
Arrow http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1573454/

Austria wrote:
I somewhere read that with mianserin you only get raw dopamine and norepinephrine action and with mirtrazapin you get also serotonin action.

Can you may shed light on that please?
No, Mirtazapine isn't serotonergic necessarily, it just blocks some serotonin receptors, effectively 'redirecting' the serotonin already in one's system to the type 1 receptors. It may mildly* boost serotonin release in certain brain areas like the frontal cortex, by blocking alpha-2-autoreceptors which regulate both serotonin and norepinephrine, by blocking those receptors, the medication may boost both norepinephrine and serotonin release.

Exclamation http://www.ncbi.nlm.nih.gov/pubmed/9007838 Exclamation
Austria wrote:
So my questions are:
1. Is mianserin a 5ht1a antagonist? (even if only a little)
2. Does mianserin increase libido?
3. What is the difference between mianserin and mirtazapin, and what is the better choice for sex drive?
4. Can you get pssd from mianserin amd mirtazapin?
1.) A very weak one, yes.
2.) In some people, yes.
3.) Mianserin increases norepinephrine more than mirtazapine.
4.) No, but some people might not like the effects of them in general. They are good drugs though, some of the few that are actually safe and effective for depression and have positive effects on hormones as opposed to almost every other anti-depressant.
Austria wrote:
Area, I am very thankful for everything you do for pssd sufferers... can you give me your email-adress? I want to send you a  voucher.

Thank you for the kind words.
Exclamation area1255x@gmail.com Exclamation

http://area-1255.forumotion.info

Brooks W. Esq


Cyproheptadine will probably put you to-sleep before it will do anything. Although it is said to antagonize serotonin receptors, it is really hard to tell to what extent it antagonizes the receptors, as most data on the drug is years; sometimes decades old, and the credibility of the studies is only secondary.
I tried it years ago with no success, I couldn't take the fatigue and it provided no benefit.

Area-1255

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Brooks W. Esq wrote:Cyproheptadine will probably put you to-sleep before it will do anything. Although it is said to antagonize serotonin receptors, it is really hard to tell to what extent it antagonizes the receptors, as most data on the drug is years; sometimes decades old, and the credibility of the studies is only secondary.
I tried it years ago with no success, I couldn't take the fatigue and it provided no benefit.

Yeah, like I said, it's antihistamine and anti-muscarinic properties make it almost useless. It's value is still needed in a medical system though, particularly in cases of serotonin syndrome - but overall it is not suitable for daily use.

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