Cyproheptadine - Liquid Serotonin Antagonist For Lab/R&D

[Waynish]

Other supplements with DMSO don't do this to me, but cypro burns and itches a bit for about 20m after application. Goes away eventually, but it seems pretty uncomfortable not to have long term side effects...

 

[haidut]

@haidut is doxylamine also anti-serotonin?

There is some evidence that it is. Not a strong as cypro, but similarly to ketotifen which is derived from cypro, doxylamine is derived from Benadryl and is in fact almost the same molecule with similar pharmacological profile. As such, in lower doses (<50mg daily) it probably has anti-serotonin effects but in higher doses it may be serotonergic. The mild anti-serotonin effects of doxylamine is what led to its marketing for nausea in pregnant women in combination with vitamin B6. Google "Diclegis" for more info.

 

[haidut]

@haidut which IdeaLabs supplement would pair well with Cyproheptadine? I'm leaning towards Lisuride to increase dopamine but would the combo inhibit serotonin too much?

Yes, I would say lisuride would pair best with cypro. Or using metergoline on its own if pure serotonin antagonism is what's needed.

 

[haidut]

Other supplements with DMSO don't do this to me, but cypro burns and itches a bit for about 20m after application. Goes away eventually, but it seems pretty uncomfortable not to have long term side effects...

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.

 

[lampofred]

Probably dumb question but do you drop this on skin or in mouth? if topically, what part of skin?

 

[Nokoni]

Probably dumb question but do you drop this on skin or in mouth? if topically, what part of skin?

I use it topically and find just about anywhere is effective. Have used back of hand, forearm, crook of elbow, and chest. Currently applying it on my back over an inflamed disk.

 

[LUH 3417]

Due to popular demand, we have released the well-known chemical cyproheptadine as a product for R&D use only. I don't think cyproheptadine needs any introduction here, so I have simply provided the Wikipedia links and some relevant links from the forum.
Cyproheptadine - Wikipedia

Please note that similar to the products sold by companies like BluePeptides, this product if for lab/research use only. The product can be ordered from the link below:
IdeaLabs Online Store - Worldwide Ordering And Delivery - Laboratory Research Chemicals

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Cyproheptadine is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties. It is one of the oldest synthetic antihistamine and antiserotonin drugs, with use spanning more than 5 decades. As such, cyproheptadine is second to none in terms of known properties, risks, and dose-response effects.

Units per container: about 30
Unit size: 12 drops
Each unit contains the following ingredients:

Cyproheptadine (Hcl): 6 mg

Other ingredients: DMSO, ethanol
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References:
Blocking Serotonin Extends Lifespan By 40%, Triples Youthspan
Serotonin Antagonists Extend Lifespan, SSRI Dramatically Shorten It
Serotonin Causes Autism; Blocking It May Treat Autism
Cyproheptadine, LSD-based Drugs Can Regenerate Damaged Liver
Benadryl and cyproheptadine protect from endotoxin poisoning
Cyproheptadine - A Wonder Drug?
Cyproheptadine prevents exercise-induced leaky brain
Cyproheptadine Is Anti-inflammatory
How cyproheptadine lowers stress
Cyproheptadine May Treat Ebola Infection
Cyproheptadine as a fertility drug in old males
Cyproheptadine As A Powerful Antidepressant
Cyproheptadine Prevents / Reverses Soft Tissue Calcification
Cyproheptadine Lowers Cortisol, Endorphins, HGH, Aldosterone
Cyproheptadine Effective For Functional GI Disorders

Hi haidut,
I am experiencing some tremors today in my hand. When I hold a glass up to drink, my hand shakes quite a bit. Do you think it's due to cyproheptadine? I've been taking it for ~2 weeks 1-4mg day depending how I feel. Some days I went up to about 6mg but followed with 1mg for the next few days.

I am feeling calm and sleeping a lot better. Small things that shouldn't be bothering me have stopped being bothersome. I feel like I can just let things go.

On a few med sites that mention cypro, I noticed tremor listed as a serious side effect, so I am wondering if I should be concerned about the shaking. Do you have any thoughts on the systemic process that may be occurring and causing this tremor if it is in fact related to cypro?

 

[haidut]

Hi haidut,
I am experiencing some tremors today in my hand. When I hold a glass up to drink, my hand shakes quite a bit. Do you think it's due to cyproheptadine? I've been taking it for ~2 weeks 1-4mg day depending how I feel. Some days I went up to about 6mg but followed with 1mg for the next few days.

I am feeling calm and sleeping a lot better. Small things that shouldn't be bothering me have stopped being bothersome. I feel like I can just let things go.

On a few med sites that mention cypro, I noticed tremor listed as a serious side effect, so I am wondering if I should be concerned about the shaking. Do you have any thoughts on the systemic process that may be occurring and causing this tremor if it is in fact related to cypro?

I don't know if it is cypro. If you think it is then stop using for a few days. Cypro has so many systemic effects it is hard to say what is causing this. It can lower blood sugar, and make some people restless. Either one of these can bring about tremors. Also, 4mg is probably too much. For most people Peat says 1mg is plenty and even in people with cancer he recommends no more than 2mg daily.

 

[LUH 3417]

I don't know if it is cypro. If you think it is then stop using for a few days. Cypro has so many systemic effects it is hard to say what is causing this. It can lower blood sugar, and make some people restless. Either one of these can bring about tremors. Also, 4mg is probably too much. For most people Peat says 1mg is plenty and even in people with cancer he recommends no more than 2mg daily.

thanks. i took 1mg today and the tremors are not present. with that, i think it was due to low blood sugar + lots of caffeine.

 

[ecstatichamster]

i find 1mg is PLENTY.

Incidentally, tremors are often caused by low magnesium. Magnesium glycinate takes them away in a few minutes, quite often.

 

[LUH 3417]

i find 1mg is PLENTY.

Incidentally, tremors are often caused by low magnesium. Magnesium glycinate takes them away in a few minutes, quite often.

Coincidentally, I also took magnesium carbonate today. Thank you!

 

[ddjd]

How cyproheptadine lowers stress

haidut ive unfortunately been having very frequent panic attacks over the last few months and the only thing that really calms me down and restores my mood from extremely bad to normal again, is cyproheptadine. I was wondering, do you think the positive effects it has are due to the serotonin reduction, or is is just because it reduces cortisol/ adrenaline. would be great to hear your view

 

[ecstatichamster]

I take a different form of cypro. I'm using it for allergies. I take 1mg per day, in the evening. I do get more "tired" and low stress hormones make me REALLY relaxed but it does kill allergies pretty well. Not 100% but makes it more than bearable.

I think it is reducing cortisol and adrenaline, mostly adrenaline. It isn't that simple. It is probably reducing serotonin as well, in a way. The point is, I'm very relaxed, kind of sleep-relaxed, but it doesn't cause my joints to ache like lower cortisol would.

I cut back Androsterone to 1 drop from 2 because my muscles were aching and it hurt to walk. I think that's not the cypro but perhaps it all contributes.

 

[haidut]

haidut ive unfortunately been having very frequent panic attacks over the last few months and the only thing that really calms me down and restores my mood from extremely bad to normal again, is cyproheptadine. I was wondering, do you think the positive effects it has are due to the serotonin reduction, or is is just because it reduces cortisol/ adrenaline. would be great to hear your view

Serotonin, cortisol, adrenaline, acetylcholine, and histamine are all involved in the panic reaction and stress response. Cyproheptadine opposes them all, so it is hard to say which one specifically was the issue. The issue of panic attacks is systemic and cyproheptadine is a systemically beneficial drug. Pregnenolone may also help as it lowers CRH, which is the initial signal of the panic response.

 

[ddjd]

Serotonin, cortisol, adrenaline, acetylcholine, and histamine are all involved in the panic reaction and stress response. Cyproheptadine opposes them all, so it is hard to say which one specifically was the issue. The issue of panic attacks is systemic and cyproheptadine is a systemically beneficial drug. Pregnenolone may also help as it lowers CRH, which is the initial signal of the panic response.

thanks haidut, do you think progesterone would help also with reducing panic attack symptoms?

 

[haidut]

thanks haidut, do you think progesterone would help also with reducing panic attack symptoms?

Yes, the study I posted I think mentioned allopregnanolone and progesterone as also effective but pregnenolone was the most effective. See below.
Pregnenolone Is The Most Potent Inhibitor Of The Stress Signal (CRH)

 

[chimdp]

@haidut , @DaveFoster , I've read a lot of your posts regarding mirtazapine, cypro, lisuride, etc. In my battle with PFS and having underlying mild depression most of my adult life I'm trying to figure out a few combo's worth trying. Given my condition I believe I will need something I can take long term. I feel part of my brain fog issues are coming from excessive ACh. When I looked up symptoms of excessive ACh it described my issues pretty well... I'm debating whether I should take the mirtazapine prescribed to me (i was taking 15mg before for 3 weeks with benefits of reduced brain fog in the form of brain "overheating" from overthinking it, somewhat reduced anxiety, but still had issues with anhedonia and motivation, especially in the morning).

Any thoughts on the combo of Mirtazapine plus cypro when needed for added anticholinergic and anti-serotonin benefits. Or mirtazapine plus ritanserin or lisuride to combat the dopamine antaganism of mirtazapine? I thought I remember some studies of mirtazapine raising dopamine in some areas of the brain but on wikipedia it shows it being a strong dopamine antagonist/inverse agonist for the dopamine receptors?

Molecular target Binding affinity, Ki(nM)[85] Notes
5-HT2A receptor 69 The (S)-(+)-enantiomer is responsible for this antagonism.[8]
5-HT2B receptor ? ~20-fold lower than for 5-HT2A/5-HT2C[86]
5-HT2C receptor 39 Inverse agonist[87] The (S)-(+)-enantiomer is responsible for this action.[8]
5-HT3 receptor ? Similar to 5-HT2A/5-HT2C (mouse neuroblastoma cell)[88] (R)-(–)-enantiomer antagonises the 5-HT3 receptor.[8]
5-HT7 receptor 265
α1 adrenergic receptor 500 [89]
α2A adrenergic receptor 20 The (S)-(+)-enantiomer is responsible for this antagonism at autoreceptors.[8] Heteroreceptors are blocked by both the (S)-(+)- and (R)-(–)-enantiomers.[4]
α2C adrenergic receptor 18 The (S)-(+)-enantiomer is responsible for this antagonism at autoreceptors.[8] Heteroreceptors are blocked by both the (S)-(+)- and (R)-(–)-enantiomers.[4]
D1 receptor 4167
D2 receptor >5454
D3 receptor 5723
H1 receptor 1.6 [90]
mACh receptors 670 [89]

 

[haidut]

@haidut , @DaveFoster , I've read a lot of your posts regarding mirtazapine, cypro, lisuride, etc. In my battle with PFS and having underlying mild depression most of my adult life I'm trying to figure out a few combo's worth trying. Given my condition I believe I will need something I can take long term. I feel part of my brain fog issues are coming from excessive ACh. When I looked up symptoms of excessive ACh it described my issues pretty well... I'm debating whether I should take the mirtazapine prescribed to me (i was taking 15mg before for 3 weeks with benefits of reduced brain fog in the form of brain "overheating" from overthinking it, somewhat reduced anxiety, but still had issues with anhedonia and motivation, especially in the morning).

Any thoughts on the combo of Mirtazapine plus cypro when needed for added anticholinergic and anti-serotonin benefits. Or mirtazapine plus ritanserin or lisuride to combat the dopamine antaganism of mirtazapine? I thought I remember some studies of mirtazapine raising dopamine in some areas of the brain but on wikipedia it shows it being a strong dopamine antagonist/inverse agonist for the dopamine receptors?

Molecular target Binding affinity, Ki(nM)[85] Notes
5-HT2A receptor 69 The (S)-(+)-enantiomer is responsible for this antagonism.[8]
5-HT2B receptor ? ~20-fold lower than for 5-HT2A/5-HT2C[86]
5-HT2C receptor 39 Inverse agonist[87] The (S)-(+)-enantiomer is responsible for this action.[8]
5-HT3 receptor ? Similar to 5-HT2A/5-HT2C (mouse neuroblastoma cell)[88] (R)-(–)-enantiomer antagonises the 5-HT3 receptor.[8]
5-HT7 receptor 265
α1 adrenergic receptor 500 [89]
α2A adrenergic receptor 20 The (S)-(+)-enantiomer is responsible for this antagonism at autoreceptors.[8] Heteroreceptors are blocked by both the (S)-(+)- and (R)-(–)-enantiomers.[4]
α2C adrenergic receptor 18 The (S)-(+)-enantiomer is responsible for this antagonism at autoreceptors.[8] Heteroreceptors are blocked by both the (S)-(+)- and (R)-(–)-enantiomers.[4]
D1 receptor 4167
D2 receptor >5454
D3 receptor 5723
H1 receptor 1.6 [90]
mACh receptors 670 [89]

Actually, the data you posted shows it is a weak dopamine antagonist. Antagonizing the dopamine receptors requires concentrations thousands of times higher than the ones needed to antagonist the serotonin or histamine receptors. So, the affinity of the drug for these receptors is probably considered negligible if taken in the prescribed doses. I think much less than 15mg may be sufficient, but I'll let Dave speak to that as he has direct experience with taking it.

 

[Philomath]

Yes, agree on this. Just have to find a way to sell it legally as a spray bottle is hard to pass as a lab product.

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

 

[DaveFoster]

@haidut , @DaveFoster , I've read a lot of your posts regarding mirtazapine, cypro, lisuride, etc. In my battle with PFS and having underlying mild depression most of my adult life I'm trying to figure out a few combo's worth trying. Given my condition I believe I will need something I can take long term. I feel part of my brain fog issues are coming from excessive ACh. When I looked up symptoms of excessive ACh it described my issues pretty well... I'm debating whether I should take the mirtazapine prescribed to me (i was taking 15mg before for 3 weeks with benefits of reduced brain fog in the form of brain "overheating" from overthinking it, somewhat reduced anxiety, but still had issues with anhedonia and motivation, especially in the morning).

Any thoughts on the combo of Mirtazapine plus cypro when needed for added anticholinergic and anti-serotonin benefits. Or mirtazapine plus ritanserin or lisuride to combat the dopamine antaganism of mirtazapine? I thought I remember some studies of mirtazapine raising dopamine in some areas of the brain but on wikipedia it shows it being a strong dopamine antagonist/inverse agonist for the dopamine receptors?

Molecular target Binding affinity, Ki(nM)[85] Notes
5-HT2A receptor 69 The (S)-(+)-enantiomer is responsible for this antagonism.[8]
5-HT2B receptor ? ~20-fold lower than for 5-HT2A/5-HT2C[86]
5-HT2C receptor 39 Inverse agonist[87] The (S)-(+)-enantiomer is responsible for this action.[8]
5-HT3 receptor ? Similar to 5-HT2A/5-HT2C (mouse neuroblastoma cell)[88] (R)-(–)-enantiomer antagonises the 5-HT3 receptor.[8]
5-HT7 receptor 265
α1 adrenergic receptor 500 [89]
α2A adrenergic receptor 20 The (S)-(+)-enantiomer is responsible for this antagonism at autoreceptors.[8] Heteroreceptors are blocked by both the (S)-(+)- and (R)-(–)-enantiomers.[4]
α2C adrenergic receptor 18 The (S)-(+)-enantiomer is responsible for this antagonism at autoreceptors.[8] Heteroreceptors are blocked by both the (S)-(+)- and (R)-(–)-enantiomers.[4]
D1 receptor 4167
D2 receptor >5454
D3 receptor 5723
H1 receptor 1.6 [90]
mACh receptors 670 [89]

Cypro (or any 5HT2B antagonist) will reduce the likelihood of developing cardiac fibrosis.

Have you had hormonal panels and do you drink coffee? Mirtazapine and coffee are very synergistic, but you need to consume a lot of carbohydrate (sugar). A lower dose of mirtazapine <3.75 mg will be more sedating and offer the appetite-stimulating benefits, and caffeine can be used as stimulant.