#119

I’ve moved on from 17 alpha…

The next candidate on my list is Acarbose. Any thoughts on obtaining this compound and dosage?

I think I’ve read the beginning therapeutic dose is 25mg with each meal. Since I eat twice per day, that would bring me to 50mg/day. Does this seem reasonable to anyone with actual knowledge and/or experience.

Thanks again for your thoughts.

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#120

Given all the possible, undesirable side effects, maybe 10 to 25mcg would be more prudent.

Then again, I love sardines and can tolerate grapefruit juice without mutating. :grin:

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#121

YOU WROTE…I think I’ve read the beginning therapeutic dose is 25mg with each meal.

It is actually 50 mg per meal.

Still a lot lower than 500 mg Metformin 4 times a day… couldn’t do even 1 a day. My phenotype.

On Acarbose now starting 4 months. All good.

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#122

Lots on Acarbose in this thread: Acarbose Dose That Folks are Taking?

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#124

Thanks for the feedback.

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#125

A post was merged into an existing topic: 17 Alpha Estradiol: Use and Dosing Experiences

#126

I have moved all the discussion about people’s experiences dosing and using 17-alpha estradiol to a new thread here: 17 Alpha Estradiol: Use and Dosing Experiences

Please use this thread (17 alpha estradiol - Another Top Anti-aging Drug) only for new science / studies / research related to 17 alpha estradiol. Use all the other thread for discussion related to the practical issues of how to use it, dose it, and results from using it.

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#128

The solution 0.025% Ell-Cranell® alpha (17α-estradiol, Galderma Korea, Co., Seoul, Korea) is a stereoisomer of the female hormone 17β-estradiol and has been used for the past 30 years in Europe, as well as in South America. The drug inhibits the conversion of testosterone to the metabolite dihydrotestosterone (DHT) by suppressing 5α-reductase activity5. In addition, by inhibiting 17β-dehydrogenase, it impedes the conversion process of androstenedione to testosterone, resulting in a reduction in the syntheses of testosterone and DHT6. It also accelerates the conversion of testosterone to estradiol by stimulating aromatase, decreasing the level of testosterone and leading to a reduction in DHT7. In addition, the drug has been reported to stimulate the generation of hair follicular matrix cells8. Clearly the use of 0.025% Ell-Cranell® alphasolution on decreased hair loss in patients with androgenetic alopecia has been shown both effective and safe. Nonetheless, the drug is not imported into Korea, and studies on Korean patients have not been conducted. Therefore, we conducted this study to assess the safety and effectiveness of 0.025% Ell-Cranell® alphasolution in Korean patients with female pattern hair loss.

17-Alpha estradiol inhibits conversion of testosterone to DHT (dihydrotestosterone), reduces synthesis of testosterone and DHT. They also linked to the study above about increase in aromatase in hair follicles ex vivo.

17-B-estradiol (Estrogen) cream topically:

A more accurate blood test of estrogen, using LC MS which is more expensive:

Same test, higher end in estrogen reference range, and the complete opposite result, with the more accurate test.

ECLIA (standard):

image
image1237×80 27.7 KB

LC MS:

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image1242×159 74.7 KB

  • If measuring estradiol levels in patients on fulvestrant consider alternative methods, such as Liquid Chromatography-Mass Spectrometry (LC-MS).

It is also suggested for drugs like Fulvestrant to use the LC MS assay to measure estradiol levels.

This might be the same for 17-Alpha Estradiol.

In my country the difference is $34 USD vs. $60, it says also the more sensitive method is suggested to men.

I find it a bit complicated with different threads for 17-Alpha-E IMO, when the ‘use and experience’ thread started with scientific studies too.

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17 Alpha Estradiol: Use and Dosing Experiences
#129

Awesome, thanks for that. The difference in the tests is news to me, but makes sense.

For Marek the prices are $8 and $50.

Search: 10 results found for "estr" – MarekDiagnostics*

I tacked on some other tests when I did my first Sirolimus level test there, and sure enough my Estradiol read high, but so did my Free Testosterone, so it was on my list to look into.

My leading theory was that Biotin I had taken messed up those two tests:

which may still be the case, but maybe the Estradiol test was just garbage to begin with?

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#130

Recent work suggests that the effects of e2-alpha are simply through the normal estrogen receptors.

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#131

From a new study in rhesus macaques:

We found that our dosing regimens (0.30 and 0.20 mg/kg/day) were tolerable as evidenced by a lack of GI distress, changes in blood chemistry or complete blood counts, and unaffected vital signs. We also found that the higher dose did elicit mild benefits on metabolic parameters including body mass, adiposity, and glycosylated hemoglobin.

“Both of our 17α-estradiol trial doses elicited significant feminization to include testicular atrophy, increased circulating estrogens, and suppressed circulating androgens and gonadotropins.”

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#132

We suspect that the observed level of feminization results from a saturation of the endogenous conjugation enzymes, thereby promoting a greater concentration of unconjugated 17α-estradiol in serum, which has more biological activity. We also surmise that the elevated level of unconjugated 17α-estradiol was subjected to a greater degree of isomerization to 17β-estradiol, which is aligned with the sevenfold increase in serum 17β-estradiol in 17α-estradiol treated animals in our first trial. Future studies in monkeys, and certainly humans, would likely benefit from the development and implementation of 17α-estradiol transdermal patches, which are commonly prescribed in humans and would circumvent potential issues with bolus dosing effects.

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#133

These are pretty high dosing levels… for a 70kg person, thats 14mg to 20mg a day. I wonder how they determined that dosing level. I’ll shoot an email to the paper author.

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#134

Using standard allometric scaling, the dose would be divided by 3.1 to determine the human equivalent.

0.2 ÷ 3.1 × (your weight in kg).

For a 175 lb man:

0.2 ÷ 3.1 × 79.3787 = 5.12 mg

So using the most typical scaling formula, their lower dose in the macaques would be about 5 mg in a 175 lb man.

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#135

Some other recent studies on 17 alpha-estradiol:

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#136

Here is the full Macaque estradiol paper:

Assessing tolerability and physiological responses to 17α-estradiol administration in male rhesus macaques

Stout et al. 2023 (17a Macaques).pdf (915.8 KB)

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17-alpha-Estradiol Study in Marmosets
#137

I’ve been in contact with the authors of this paper, and I’m thinking it might be valuable to talk with them and get some questions about this paper answered. If you’ve had a chance to review the paper and have some questions - please post them here.

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#138

17α-estradiol Alleviates High-Fat Diet-Induced Inflammatory and Metabolic Dysfunction in Skeletal Muscle of Male and Female Mice

Skeletal muscle has a central role in maintaining metabolic homeostasis. 17α-estradiol (17α-E2), a naturally-occurring non-feminizing diastereomer of 17β-estradiol that demonstrates efficacy for improving metabolic outcomes in male, but not female, mice. Despite several lines of evidence showing that 17α-E2 treatment improves metabolic parameters in middle-aged obese and old male mice through effects in brain, liver, and white adipose tissue little is known about how 17α-E2 alters skeletal muscle metabolism, and what role this may play in mitigating metabolic declines. Therefore, this study aimed to determine if 17α-E2 treatment improves metabolic outcomes in skeletal muscle from obese male and female mice following chronic high fat diet (HFD) administration. We hypothesized that male, but not female, mice, would benefit from 17α-E2 treatment during HFD. To test this hypothesis, we used a multi-omics approach to determine changes in lipotoxic lipid intermediates, metabolites, and proteins related to metabolic homeostasis. In male mice, we show that 17α-E2 alleviates HFD-induced metabolic detriments of skeletal muscle by reducing the accumulation of diacylglycerol (DAGs) and ceramides, inflammatory cytokine levels, and reduced the abundance of most of the proteins related to lipolysis and beta-oxidation. In contrast to males, 17α-E2 treatment in female mice had little effect on the DAGs and ceramides content, muscle inflammatory cytokine levels, or changes to the relative abundance of proteins involved in beta-oxidation. These data support to the growing evidence that 17α-E2 treatment could be beneficial for overall metabolic health in male mammals.

bioRxiv. posted 1 June 2023, 10.1101/2023.05.30.542870

http://biorxiv.org/content/early/2023/06/01/2023.05.30.542870

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#139

Still hoping that 17-Alpha Estradiol is semi-permeable of the scalp. Have been using Pantostin for a month now. Difficult to find any evidence from Google searches about the permeability of this hormone. However, given that other hormones are often delivered through skin patches have assumed it would work. Wish I could find out, if it isn’t working would like to know so I could start taking it orally (Dissolve chemical and mix with oil). Do you know where I can find information about the skin permeability of 17-Alpha?

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#140

17α-estradiol Alleviates High-Fat Diet-Induced Inflammatory and Metabolic Dysfunction in Skeletal Muscle of Male and Female Mice

Skeletal muscle has a central role in maintaining metabolic homeostasis. 17α-estradiol (17α-E2), a naturally-occurring non-feminizing diastereomer of 17β-estradiol that demonstrates efficacy for improving metabolic outcomes in male, but not female, mice. Despite several lines of evidence showing that 17α-E2 treatment improves metabolic parameters in middle-aged obese and old male mice through effects in brain, liver, and white adipose tissue little is known about how 17α-E2 alters skeletal muscle metabolism, and what role this may play in mitigating metabolic declines. Therefore, this study aimed to determine if 17α-E2 treatment improves metabolic outcomes in skeletal muscle from obese male and female mice following chronic high fat diet (HFD) administration. We hypothesized that male, but not female, mice, would benefit from 17α-E2 treatment during HFD. To test this hypothesis, we used a multi-omics approach to determine changes in lipotoxic lipid intermediates, metabolites, and proteins related to metabolic homeostasis. In male mice, we show that 17α-E2 alleviates HFD-induced metabolic detriments of skeletal muscle by reducing the accumulation of diacylglycerol (DAGs) and ceramides, inflammatory cytokine levels, and reduced the abundance of most of the proteins related to lipolysis and beta-oxidation. In contrast to males, 17α-E2 treatment in female mice had little effect on the DAGs and ceramides content, muscle inflammatory cytokine levels, or changes to the relative abundance of proteins involved in beta-oxidation. These data support to the growing evidence that 17α-E2 treatment could be beneficial for overall metabolic health in male mammals.

2023.05.30.542870v2.full.pdf (2.9 MB)

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