It's weak as pointed out, but it can work in high doses. My problem is, what is the binding affinity for estrogen receptor alpha. It has 1% affinity of estradiol for beta, but if it's 2% for alpha then this would seem to be bad. If it's also 1% or less then it would be good.
Methyl Estadiol Propanoate (MEP)- ER agonist completely w/o side effects
- Thread starter FollicleGuardian
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@ChemHead What if we find/design a molecule that is dependent on a special environment. Like dependent a hydrophobic gel like substance that doesn’t go systemic.
Example: Gel X hydrophobic applied topically. Then modified estrogen that is only active in or in the precense of Gel X (specific ph or something dependent).
Example: Gel X hydrophobic applied topically. Then modified estrogen that is only active in or in the precense of Gel X (specific ph or something dependent).
It's not. Techniques and even a couple pharmaceuticals like this already exist and have for quite awhile now. It's just that no one cares enough to start developing something like this for the hair loss industry. And honestly the skin and hair are the best uses for these types of drugs because they're so easily accessible from the outside compared to internal organs. Getting light to the skin from the outside is easy. Getting it to an internal organ required surgery or implantation of a light emitting device of some sort.
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An o-nitrobenzyl-based photocleavable antitumor prodrug with a terminal carboxyl group was designed and synthesized. The photolysis properties of the prodrug were investigated by means of 1H NMR, HPLC, UV, and MTT methods. The results showed that the toxicity of the anticancer drug was...
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Request PDF | A photochemical approach for controlled drug release in targeted drug delivery | Photochemistry provides a unique mechanism that enables the active control of drug release in cancer-targeting drug delivery. This study... | Find, read and cite all the research you need on ResearchGate
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Using photolabile ligands in drug discovery and development
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Here's a good overview of the state of the art:
Recent advances in light-responsive on-demand drug-delivery systems
The convergence of wearable sensors and personalized medicine enhance the ability to sense and control the drug composition and dosage, as well as location and timing of administration. To date, numerous stimuli-triggered smart drug-delivery systems have ...
www.ncbi.nlm.nih.gov
There are already a couple FDA approved drugs for cancer that make use of this technique. I can't remember the names of them, though.
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I have asked them. They said they would investigate and get back to me.
Also based on the results the test subject got in terms of bettering of dryness, sweating, wrinkles etc points that although it’s binding affinity is weak. The upregulation done by MEP seems pretty potent.
See the last link in my previous post. It has a good overview of properties that can be taken advantage of to release caged molecules, including the use of ultrasound.
The numbers are impressive, but I don't see any difference in those pictures.
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Also found out the cream is 2% concentration
Right, those are the impressive numbers I was talking about. I don't put a lot of stock in numbers from cosmetic company trials. The pictures show 0 improvement.
You're controlling dose with light... You don't need to have a light source on your head 24/7. If the dose isn't high enough with a reasonable amount of light, you just take more of the drug.
Does this seriously seem like an inconvenience to you lol? There are people slathering oils on their heads every night and stabbing themselves in the scalp. I think I'd take a little 15 minute light session once or twice or three times (God forbid) a day. Especially if it means I don't have to be chemically castrated by the current drugs of choice.
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Remember that fine lines/wrinkles (I suppose this is what you were looking for) was the least effective indication for MEP
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How would that work in practice? Let’s say I take oral estradiol-photocaged (EP). Then I shine the light 15 minutes. It activates the estradiol in the hair follicle. This won’t stay in the hair follicle forever? The activated EP would circulate around. So you would need a drug that
1) Needs continous light
or,
2) Have a very short half life
I don't have the answers to these questions because we don't know how long steroids hang around in the cell. There's not enough research and literature that would answer these questions because it just hasn't been done enough. There's a need for it now more than ever, though, and I suspect it will become more common.
When estradiol gets used up in the cell, it's not supposed to just remain estradiol and float around in the blood. It's supposed to be metabolized and then eliminated. The only estrogens that would be of any concern are the ones the end up being released outside of the cell because they happen to be in the path of the light. And then, honestly, how much are we talking about here... Nanograms? Picograms? Whatever it would be, I doubt it would be anything remotely close to the side effects you would experience by taking estradiol systemically.
If you think about it, all you're trying to do is bypass and replace the body's inability to create estrogens intrafollicularly. The light is acting as the "enzyme", since balding scalps are deficient in aromatase expression, except that you're releasing estradiol rather than metabolizing testosterone to yield it. Will you be able to keep the concentration within the follicle uniform? Probably not. You'll have to get your activation treatment a couple times a day and you would have to adjust the dosage of the drug such that each activation session causes a spike in intrafollicular concentration a little beyond normal so that the peaks throughout the day average to some threshold concentration that works.
This hair loss problem is not going to be fixed by a topical. It's too complex of a problem to fix for a traditional pharmaceutical or topical. It's just going to require smarter, more sophisticated technology. Genetic engineering is the best option, but it's not actually an option until we actually figure out the true pathology of hair loss. And even then, experimenting with genome changes already has its ethical challenges. A smart drug like what I've described would've be a good tool and compromise leading up to the eventual genetic fix.
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I'm looking at everything. I don't see any difference. Estriol works on fine lines.
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Legends
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I personally apply estradiol cream on my scalp and dont really see an issue with it. It is said in the MTF community that around 2mg of estradiol is a replacement dose for a male. I apply around 0.3-0.5mg on my scalp. The marginal increase in serum concentration of my E2 is not significant enough to cause side effects, or atleast not in my experience. But 0.3-0.5mg of estradiol on the scalp is alot of the hormone for such a tiny area, which is why i think its extremely benefical for stopping hairloss and regrowing hair. The only unsure factor is how long does that topically applied estradiol stay on my scalp, and how long does the hormone stay attached to the ER once it has bind to it. I have a feeling that perhaps i need split my daily topical estradiol dose and apply it more often throughout the day. Anyways i stand by my point that i see no issue with applying a small amount of topical estradiol on your scalp
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MtF take 2 pills of E2 sublingually a day, one in the morning, one in the evening.
So yeah, I agree on your point that it would make sense to apply more often the Estrogel on your scalp, but it's such a hassle tbh.
Do you know if the effect is localized or will it go anyways systemic? I think the latter one makes more sense lol
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It does go systemic. Topical estradiol exists because oral E2 tabs convert to estriol almost completely. Thats why MTFs take E2 tabs sublingually. Any estradiol cream you is intended to increase your serum concentration of estradiol. Its just a different route of administration, an alternative to injections.
Your body is not that sensitive to an increase in E2 as some people might like to think. And its not like i plan to use topical E2 for the rest of my life. Rather i "blast" it for a period of time to give myself a boost in hair growth.
I like this tactic. Use estrogen topically 1-2mg estradiol or 10-20mg estriol, and no systemic AA only topical. Estrogen is most dangerous in combination with a systemic AA.
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Yes. And even if i did get side effects, im okay with living with higher blood pressure or whatever for some time if it means i can grow back 500 hairs on my hairline.