Cyproheptadine - Liquid Serotonin Antagonist For Lab/R&D

[chimdp]

Thanks Haidut and Dave. I do drink coffee so I will continue that. I think I will need to take the Mirtazapine at a higher dose as I'm needing more for it's antidepressant qualities than just helping sleep and appetite. For an added boost I'll look at experimenting with small doses of cypro and lisuride

 

[PhilParma]

in a 2oz bottle, what % cypro would work best? 1%, 4% more?

Here is something haidut wrote in another thread:

Cyproheptadine is probably enough so that you have about 1mg/ml as most people end up spraying a few ml SolBan on their heads or body, which would give them a few mg of cypro.

 

[PhilParma]

This is the first report like that we are getting. I think it is due to the Hcl salt of cypro being used for the product. I asked a pharmacist about it and he said it is probably benign if it disappears without much skin damage. He said other Hcl salts like pyridoxine Hcl (vitamin B6) or thiamine Hcl (vitamin B1) would do the same when applied to the skin in a DMSO solution. I think some people already reported minor irritation with topical Energin, so matches what the pharmacist said.

I applied cypro to the crook of my rat's elbow for a few weeks (my rat has elbows), and now the skin is persistently red in that area. I've went back to applying the drops to the top of the rat's foot. That area is also red, but it seems less bothersome.

 

[Squatrat]

@haidut
A question came up in another thread and I thought I'd ask it here: What does Cypro offer over other antihistamines? There are many to choose from, often cheap and OTC.

 

[haidut]

in a 2oz bottle, what % cypro would work best? 1%, 4% more?

I don't know what concentration would work best as that has not been tried experimentally. I would be more careful about

@haidut
A question came up in another thread and I thought I'd ask it here: What does Cypro offer over other antihistamines? There are many to choose from, often cheap and OTC.

Most of them do not have direct serotonin antagonism. Cypro also seems to be aldosterone antagonist, as well as estrogen receptor antagonist and some other interesting properties. If you look at the thread "cyproheptadine wonder drug" these are mentioned there. Most of the newer antihistamines are just anthistamines even though some of them have other interesting properties. The decades of clinical use for cypriheptadine is invaluable too. It is the only true indicator of safety, which no other antihistamine can match, except maybe Benadryl.

 

[Wagner83]

Has anyone tried the cypro on scrotum?
@DaveFoster

 

[DaveFoster]

Has anyone tried the cypro on scrotum?
@DaveFoster

I have not. Feel free to let us know how it goes.

 

[cardochav]

Haidut,

My experimenting with cypro in the pill form has always ended in me having a migraine with aura by the end of the 2nd or 3rd day, even with doses as low as 1/2mg. Any reason to believe that I could have different results with this liquid dmso form?

 

[haidut]

Haidut,

My experimenting with cypro in the pill form has always ended in me having a migraine with aura by the end of the 2nd or 3rd day, even with doses as low as 1/2mg. Any reason to believe that I could have different results with this liquid dmso form?

Some people get headaches from cypro, it is a known side effect. I would try another antihistamine like Benadryl and if you get headaches from it too then a liquid cypro is probably not going to be any different.

 

[DaveFoster]

@haidut

I get good effects from higher doses of cypro (8 mg+), bur Ray doses under 3-4 mg. Do you think the dopamine antagonism is a problem long-term?

I remember you mentioning that even though cypro antagonizes the dopamine "receptor" it sufficiently opposes serotonin so as to end with a net increase in dopamine.

 

[haidut]

@haidut

I get good effects from higher doses of cypro (8 mg+), bur Ray doses under 3-4 mg. Do you think the dopamine antagonism is a problem long-term?

I remember you mentioning that even though cypro antagonizes the dopamine "receptor" it sufficiently opposes serotonin so as to end with a net increase in dopamine.

My experience a few years back was also that higher doses than 4mg were needed to suppress serotonin and cortisol sufficiently to get that blissful feeling of a highschooler. But the higher doses have been linked to elevated liver enzymes and Peat told some people over email recently that cypro can affect the bile ducts and change urine color to brown, so he advised using no more than 1mg. I think ketotifen, which is almost the same molecule, may be a safer cypro alternative in higher doses as it actually helps liver health but I don't know how well it overlaps with the anti-serotonin profile of cypro. Maybe somebody can ask Peat about this.
As far as dopamine antagonism - I don't think it is a big issue as if it was cypro will have Parkinsonism as a side effect but it does not even in doses as high as 32mg+ daily. So, whatever it does to dopamine receptors seems to not cause much damage.

 

[Tarmander]

My experience a few years back was also that higher doses than 4mg were needed to suppress serotonin and cortisol sufficiently to get that blissful feeling of a highschooler. But the higher doses have been linked to elevated liver enzymes and Peat told some people over email recently that cypro can affect the bile ducts and change urine color to brown, so he advised using no more than 1mg. I think ketotifen, which is almost the same molecule, may be a safer cypro alternative in higher doses as it actually helps liver health but I don't know how well it overlaps with the anti-serotonin profile of cypro. Maybe somebody can ask Peat about this.
As far as dopamine antagonism - I don't think it is a big issue as if it was cypro will have Parkinsonism as a side effect but it does not even in doses as high as 32mg+ daily. So, whatever it does to dopamine receptors seems to not cause much damage.

Do you think the liver enzymes would be from lowering choline/Acetlycholine?

 

[haidut]

Do you think the liver enzymes would be from lowering choline/Acetlycholine?

No, I think the cypro molecule may have some direct negative effects on liver metabolism when used in higher doses. Interestingly, ketotifen (which is almost the same molecule) not only does not have any cases of liver side effects but has been used to even reverse liver fibrosis. Not sure why, so maybe somebody could ask Peat.

 

[Regina]

No, I think the cypro molecule may have some direct negative effects on liver metabolism when used in higher doses. Interestingly, ketotifen (which is almost the same molecule) not only does not have any cases of liver side effects but has been used to even reverse liver fibrosis. Not sure why, so maybe somebody could ask Peat.

Would you consider making a version? (Fibronon?)

 

[haidut]

Would you consider making a version? (Fibronon?)

I actually have an anti-fibrosis supplement that will be released tonight or at the latest tomorrow morning

 

[Regina]

I actually have an anti-fibrosis supplement that will be released tonight or at the latest tomorrow morning :)

 

[haidut]

Here it is:
DeFibron - Liquid Supplement For R&D

 

[DaveFoster]

I actually have an anti-fibrosis supplement that will be released tonight or at the latest tomorrow morning :)

Incredible timing @Regina . I was aware of the negative effects on liver metabolism, but I thought it could be avoided with topical application. Ketotifen has anxiolytic effects (not surprising): The effect of ketotifen in rodent models of anxiety and on the behavioural consequences of withdrawing from treatment with drugs of abuse

Source: Cyproheptadine binding affinity table

Here's a partial list of the binding affinities for ketotifen; I was compiling a table, but there's not a whole lot of info:

ketotifen | Activity data visualisation tool | IUPHAR/BPS Guide to PHARMACOLOGY

It binds to H1 strongly like both cypro and mirtazapine, so it likely stimulates the appetite, but it doesn't have the strong anticholinergic biding profile of cypro. It also antagonizes 5HT-2B, so there's a minimal risk of cardiac fibrosis.

 

[haidut]

Incredible timing @Regina . I was aware of the negative effects on liver metabolism, but I thought it could be avoided with topical application. Ketotifen has anxiolytic effects (not surprising): The effect of ketotifen in rodent models of anxiety and on the behavioural consequences of withdrawing from treatment with drugs of abuse

Source: Cyproheptadine binding affinity table

Here's a partial list of the binding affinities for ketotifen; I was compiling a table, but there's not a whole lot of info:

ketotifen | Activity data visualisation tool | IUPHAR/BPS Guide to PHARMACOLOGY

It binds to H1 strongly like both cypro and mirtazapine, so it likely stimulates the appetite, but it doesn't have the strong anticholinergic biding profile of cypro. It also antagonizes 5HT-2B, so there's a minimal risk of cardiac fibrosis.

The 5-HT2B antagonism explains why ketotifen not only does not hurt the liver but can treat liver disease and systemic sclerosis (another fibrotic condition). Also, anything that blocks 5-HT2B may treat cancer.
The Serotonin Receptor 5-HT2B Is Required For Cancer; Can Be Blocked
Btw, the link you provided shows that ketotifen is also 5-HT2A antagonist and actually with slight preference of 5-HT2A over 5-HT2B.
All 5-HT2B/A antagonists seem to be potent antidepressants in animal studies and a few pharma companies have 5-HT2B/A blockers in trials for depression.
Finally, 5-HT2A antagonists are likely potent immunostimulants as per the study below, which would explain why drugs of the cypro family can fight viral infections so well and it certainly contributes to their anti-cancer effects.
Effects of 5-HT2A receptor stimulation and blocking on immune response. - PubMed - NCBI

 

[DaveFoster]

The 5-HT2B antagonism explains why ketotifen not only does not hurt the liver but can treat liver disease and systemic sclerosis (another fibrotic condition). Also, anything that blocks 5-HT2B may treat cancer.
The Serotonin Receptor 5-HT2B Is Required For Cancer; Can Be Blocked
Btw, the link you provided shows that ketotifen is also 5-HT2A antagonist and actually with slight preference of 5-HT2A over 5-HT2B.
All 5-HT2B/A antagonists seem to be potent antidepressants in animal studies and a few pharma companies have 5-HT2B/A blockers in trials for depression.
Finally, 5-HT2A antagonists are likely potent immunostimulants as per the study below, which would explain why drugs of the cypro family can fight viral infections so well and it certainly contributes to their anti-cancer effects.
Effects of 5-HT2A receptor stimulation and blocking on immune response. - PubMed - NCBI

Indeed, very interesting information, thanks for the provision.

The therapeutic role of 5-HT1A and 5-HT2A receptors in depression

Among the drugs that are 5-HT2A antagonists include trazodone, mirtazapine, and nefazodone. It's unfortunate that mirtazapine has higher incidences of cardiac side effects (even compared to other antidepressants): Cardiovascular Considerations in Antidepressant Therapy: An Evidence-Based Review