Cyproheptadine as an Uncoupler?

tankasnowgod

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I have been taking cyproheptadine again as a self experiment, in higher doses that when I previously used it. Usually, I am taking 4mg with every meal. After a few days, I started to notice I would often get very warm after a meal, especially in the face and chest area near my thyroid. It doesn't happen all the time, but it's happened frequently enough that I was starting to wonder if cyproheptadine had any uncoupling effects. After some searching, I did find one in vitro study (only a page long) that suggests just that-


Cyproheptadine 3.33-100μM was found to produce a concentration-dependent stimulation of State 4 respiration (substrate and oxygen in excess, ADP absent) during the NAD+-linked oxidation of 5mM glutamate plus 5mM malate by tightly coupled rat hepatic mitochondria, with the rate of respiration increasing from 22.6 f 1.0 to 47.4 f 4.0 ng atoms 02 consumed min-lmg of protein-l (n=4) , resulting in an EC50 value of 28.2pM.

Cyproheptadine was shown to cause a concentration-dependent stimulation of mitochondrial ATPase (E.C.3.6.1.4) activity over the same concentration range that produced a stimulation of State 4 respiration; with the rate of activity increasing from 4.87 f 0.39 to 10.84 f 1.34 nmoles inorganic PO4 released min-lmg of protein-l (n=4). A similar but significantly (pt0.05) more potent effect was observed with DNP (1-1OOpl) with the rate increasing from 4.90 f 0.53 to 16.05 f 0.87 nmoles inorganic PO4 released min-lmg of protein-' (n=4).

I ran the numbers through Sigma Aldrich's Molarity calculator, and it seems like a human might be able to hit the low end of the range with a 5mg dose (or lower if it's already in the body from chronic use). My calculations could be off, and since I was using the lowest molarity (3.3 μM), I didn't use a HED, just what was in the study. Also, I know there can be many issues estimating an in vivo dose from an in vitro dose, and I don't know how to control for that. If anyone would like to check my work, please do.

 

haidut

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I have been taking cyproheptadine again as a self experiment, in higher doses that when I previously used it. Usually, I am taking 4mg with every meal. After a few days, I started to notice I would often get very warm after a meal, especially in the face and chest area near my thyroid. It doesn't happen all the time, but it's happened frequently enough that I was starting to wonder if cyproheptadine had any uncoupling effects. After some searching, I did find one in vitro study (only a page long) that suggests just that-






I ran the numbers through Sigma Aldrich's Molarity calculator, and it seems like a human might be able to hit the low end of the range with a 5mg dose (or lower if it's already in the body from chronic use). My calculations could be off, and since I was using the lowest molarity (3.3 μM), I didn't use a HED, just what was in the study. Also, I know there can be many issues estimating an in vivo dose from an in vitro dose, and I don't know how to control for that. If anyone would like to check my work, please do.


I think it may have a mild uncouple effects, but it would be hard to achieve the higher concentrations in human tissues. The 3.3 uM is probably achievable with a single/bolus dose of 15mg-20mg, but I doubt anybody is taking such bolus doses. Btw, what value are you using the the "desired volume" in the Sigma calculator? The so-called "volume of distribution" (VoD) of cyproheptadine in-vivo is not really known in-vivo, at least AFAIK. The only study I was able to find about that is this one.
 

sugarisgreat

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I have been taking cyproheptadine again as a self experiment, in higher doses that when I previously used it. Usually, I am taking 4mg with every meal. After a few days, I started to notice I would often get very warm after a meal, especially in the face and chest area near my thyroid. It doesn't happen all the time, but it's happened frequently enough that I was starting to wonder if cyproheptadine had any uncoupling effects. After some searching, I did find one in vitro study (only a page long) that suggests just that-






I ran the numbers through Sigma Aldrich's Molarity calculator, and it seems like a human might be able to hit the low end of the range with a 5mg dose (or lower if it's already in the body from chronic use). My calculations could be off, and since I was using the lowest molarity (3.3 μM), I didn't use a HED, just what was in the study. Also, I know there can be many issues estimating an in vivo dose from an in vitro dose, and I don't know how to control for that. If anyone would like to check my work, please do.

Does this dose increase your hunger a great deal?
 

Healthseeker

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@tankasnowgod
This is very interesting. I'd like to understand uncoupling. I some questions. Is it just a name for having an active thyroid? Is this something worth doing. Do you have to take drugs or can do it naturally. What is it. Is it kaioken x2.
 

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