Methylene Blue (MB) Is A Potent Aromatase Inhibitor

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haidut

haidut

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Have you tried inosine at all? Is the Uric acid increase a concern in people prone to gout?

Yes, I have tried it and it is quite potent as a mood lifter and also as a heart protector. The increase in uric acid requires doses of 2g+ daily and most benefits are seen from even <500mg doses. So, it should be pretty safe even for those people.
Inosine : a naturally occurring cardiotonic agent. - PubMed - NCBI
Positive inotropic response to inosine in the in situ canine heart. - PubMed - NCBI
https://www.hindawi.com/journals/isrn/2012/326809/
 

Tarmander

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Yes, I have tried it and it is quite potent as a mood lifter and also as a heart protector. The increase in uric acid requires doses of 2g+ daily and most benefits are seen from even <500mg doses. So, it should be pretty safe even for those people.
Inosine : a naturally occurring cardiotonic agent. - PubMed - NCBI
Positive inotropic response to inosine in the in situ canine heart. - PubMed - NCBI
https://www.hindawi.com/journals/isrn/2012/326809/
Appreciate your response man
 

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I think progesterone in higher doses antagonizes aldosterone and thus can cause sodium loss. Drop in sodium levels can lead to adreanline increase and thus insomnia. The dose would be unique for everybody but I have always liked progesterone more in sub 10mg doses. As far as sleep, try inosine. Not only is is a powerful adenosine agonist and thus promoted restorative sleep, it cures depression and rewires even traumatically damaged brain in doses as little as 1g daily. The depression studies used even less than that - about ~100mg daily for a human. Google "inosine depression" or "inosine brain damage".
I have come across inosine and never heard much about it. I'll definitely look into; thanks very much haidut!
 

ddjd

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@haidut do you think there would be anything wrong with taking 100mg pregnenolone with methylene blue? i thought maybe as its an aromatase inhibitor it might help the pregnenolone turn into all the positive things like progesterone etc. and avoid any potential estrogen channels etc.

what do you think
 
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@haidut do you think there would be anything wrong with taking 100mg pregnenolone with methylene blue? i thought maybe as its an aromatase inhibitor it might help the pregnenolone turn into all the positive things like progesterone etc. and avoid any potential estrogen channels etc.

what do you think

It is probably OK to take this combo but I think most people do not need more than 30mg pregnenolone daily. Lower doses convert more easily into DHEA and progesterone.
 
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"...Further evaluations showed miconazole [81] and methylene blue [82] are very potent aromatase inhibitors with IC50 values of 0.04 and 0.55 uM respectively."

While the pharmacokinetics of MB differ wildly from a person to person, an oral dose of about 10mg should achieve concentrations of at least 0.5uM in most people, and in fact probably closer to 1uM. Given that MB also uncouples mitochondria starting at concentrations of 0.5uM, it looks like you can get the weight loss and anti-estrogen benefits with a fairly low oral dose.

Are you sure you meant oral dose and are not extrapolating data from i.v. dose? Keep in mind oral dose has about 50% absorption at the gut compared with IV.
 
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Are you sure you meant oral dose and are not extrapolating data from i.v. dose? Keep in mind oral dose has about 50% absorption at the gut compared with IV.

A concentration of 0.55uM/L is not high at all. Every substance has its own so-called volume of distribution (VOD) but given the molar mass and pharmacokinetics of MB it is quite possible that even <5mg will achieve that concentration in vivo. For most steroids and vitamins a dose of 3mg-5mg achieves 1uM/L and MB is not much different.
 
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A concentration of 0.55uM/L is not high at all. Every substance has its own so-called volume of distribution (VOD) but given the molar mass and pharmacokinetics of MB it is quite possible that even <5mg will achieve that concentration in vivo. For most steroids and vitamins a dose of 3mg-5mg achieves 1uM/L and MB is not much different.

Thanks haidut.
 

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I can't find the original reference on PubMed or anywhere else, so if someone can dig that up for me I'd really appreciate it. For now, we'll have to accept the following statement from the book (the book seems rather legit btw).

https://books.google.com/books?id=plBoB ... se&f=false

"...Further evaluations showed miconazole [81] and methylene blue [82] are very potent aromatase inhibitors with IC50 values of 0.04 and 0.55 uM respectively."

While the pharmacokinetics of MB differ wildly from a person to person, an oral dose of about 10mg should achieve concentrations of at least 0.5uM in most people, and in fact probably closer to 1uM. Given that MB also uncouples mitochondria starting at concentrations of 0.5uM, it looks like you can get the weight loss and anti-estrogen benefits with a fairly low oral dose.
I know some people have reported that they cannot tolerate a dose over 1mg. I had the same experience originally, but just like cyproheptadine I found that it is a matter of acclimatization, at least for me. Now I can take 10mg three times a day and with the exception of intense sweating and high body temperatures I don't really notice any other side effects.
I'm wondering if MB is used as an aromatase inhibitor: would the MAO-Inhibition outweight it's benefits at those dosages?
 
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I'm wondering if MB is used as an aromatase inhibitor: would the MAO-Inhibition outweight it's benefits at those dosages?

Ironically, the IC50 for both aromatase and MAO-A is aroung 0.5 uM/L. But Peat said MB is probably safe in doses up to 15mg daily, as used in human studies for mental issues. So, I think using 5mg daily should be a good tradeoff but I would still avoid foods like aged cheese, chocolate and wine a few hours before/after the MB usage.
 

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Well, my experience on MB:
Started with 1 or 2 mg a day. I think the first couple days rat felt slight headaches (like the ones rat felt on low dose cyproheptadine), but it seems that tolerance is quickly build up, I'm using 10 mg a day, 5 mg morning and 5 mg night.
I feel like I can stand cold weather a lot better. In the day I feel fine, awake.
Urine after a few hours after oral administration comes out green or blueish color.
 

vulture

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I can't find the original reference on PubMed or anywhere else, so if someone can dig that up for me I'd really appreciate it. For now, we'll have to accept the following statement from the book (the book seems rather legit btw).

https://books.google.com/books?id=plBoB ... se&f=false

"...Further evaluations showed miconazole [81] and methylene blue [82] are very potent aromatase inhibitors with IC50 values of 0.04 and 0.55 uM respectively."

While the pharmacokinetics of MB differ wildly from a person to person, an oral dose of about 10mg should achieve concentrations of at least 0.5uM in most people, and in fact probably closer to 1uM. Given that MB also uncouples mitochondria starting at concentrations of 0.5uM, it looks like you can get the weight loss and anti-estrogen benefits with a fairly low oral dose.
I know some people have reported that they cannot tolerate a dose over 1mg. I had the same experience originally, but just like cyproheptadine I found that it is a matter of acclimatization, at least for me. Now I can take 10mg three times a day and with the exception of intense sweating and high body temperatures I don't really notice any other side effects.
https://monographs.iarc.fr/ENG/Monographs/vol108/mono108-06.pdf
Methylene blue penetrates cellular and mitochondrial membranes, accumulates within mitochondria, and improves mitochondrial respiration at low concentrations (0.5–2 μM) by shuttling electrons to oxygen in the electron transport chain.
Seems that reaching 0.5 to 1 μM gives two benefits: improved mitochondrial respiration along with aromatase inhibition.
If dosage for this is around 10 mg (would be nice to know mg/Kg to be more accurate), seems it's a pretty safe dose according to studies I've crossed with.
DNA and cromosome damage seems to happen only in vitro. Although would be nice if someone have read something about this.

I'm currently taking 4 to 10 mg of MB a day. Bought a local one that states topical use only ("non esterile") but so far I haven't felt anything bad, besides of maybe not so good sleeping (I take a night dose of 5 mg), but I couldn't seriously say it's the MB right now.
Specially at the beggining I felt slight headaches and then they starting to cease (few days) and also felt like more resistant to cold temperatures.
 
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https://monographs.iarc.fr/ENG/Monographs/vol108/mono108-06.pdf

Seems that reaching 0.5 to 1 μM gives two benefits: improved mitochondrial respiration along with aromatase inhibition.
If dosage for this is around 10 mg (would be nice to know mg/Kg to be more accurate), seems it's a pretty safe dose according to studies I've crossed with.
DNA and cromosome damage seems to happen only in vitro. Although would be nice if someone have read something about this.

I'm currently taking 4 to 10 mg of MB a day. Bought a local one that states topical use only ("non esterile") but so far I haven't felt anything bad, besides of maybe not so good sleeping (I take a night dose of 5 mg), but I couldn't seriously say it's the MB right now.
Specially at the beggining I felt slight headaches and then they starting to cease (few days) and also felt like more resistant to cold temperatures.

A human dose of 0.05mg/kg is thought to achieve about 1uM/L concentrations in most people. The sleep issues could be from uncoupling. MB can uncouple similar to DNP and it seems the EC50 is again 0.5uM/L. So, a lot of good things happening in the <1uM/L concentrations.
 

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A human dose of 0.05mg/kg is thought to achieve about 1uM/L concentrations in most people. The sleep issues could be from uncoupling. MB can uncouple similar to DNP and it seems the EC50 is again 0.5uM/L. So, a lot of good things happening in the <1uM/L concentrations.
How much could it cost to asses the MB concentration in blood after oral use in humans? might be a nice test to asses if dosage is correct.
 
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How much could it cost to asses the MB concentration in blood after oral use in humans? might be a nice test to asses if dosage is correct.

I don't know if major labs like LabCorp and Quest have this test in their inventory. Studies done with humans do this test routinely, but since MB is not yet approved as a drug to take chronically, the major labs probably do not see a need to offer such a test yet. Maybe you can email some of the authors of one of these MB studies and ask how/where they did the testing. I would be very interested to know if such a test is offered commercially. Maybe @Dan Wich can chime in?? He checks all kinds of labs to see if they offer some of the more obscure tests we discuss on the forum.
 

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Seeing if .5mg daily will help me with lowering aromatase, and perhaps increase thyroid function
 

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Then you will not know if it lowered aromatase, you will get just subjective symptoms attributable to a lot of other things
 

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