Androgen Receptors

[DTW]

I've read a lot about specific drugs preventing DHT from binding to the androgen receptors in the scalp/hair follicle, but are there any known treatments that actually reduce the number of androgen receptors themselves?..And is it possible that the body may generate more receptors to compensate when beginning a medication like finasteride or dutasteride?

For example- when I initially began using Avodart I had very good results, even noticeable within the first month. However, the results have already slowly began to taper off. By all accounts, my DHT levels must be fairly low based on all the Avodart I've ingested. So why would my hair continue to thin in such a short period of time? This leads me to believe that more androgen receptors are attaching to my hair follicles resulting in even small amounts of DHT attacking my scalp

Any ideas?

 

[Bryan]

I've read a lot about specific drugs preventing DHT from binding to the androgen receptors in the scalp/hair follicle, but are there any known treatments that actually reduce the number of androgen receptors themselves?

I know that the patent information for "fluridil" claims such a reduction in androgen receptors, and there may be other substances that supposedly do that, too. The only problem I have with it is that I don't fully trust what they say about fluridil.

..And is it possible that the body may generate more receptors to compensate when beginning a medication like finasteride or dutasteride?

Yes, it's possible. Dr. Sawaya claimed in a statement read to doctors at a medical conference that finasteride caused an "intense upregulation" of androgen receptors in the men she examined.

For example- when I initially began using Avodart I had very good results, even noticeable within the first month. However, the results have already slowly began to taper off. By all accounts, my DHT levels must be fairly low based on all the Avodart I've ingested. So why would my hair continue to thin in such a short period of time? This leads me to believe that more androgen receptors are attaching to my hair follicles resulting in even small amounts of DHT attacking my scalp

I doubt that that has anything to do with an upregulation of androgen receptors.

 

[2020]

And is it possible that the body may generate more receptors to compensate when beginning a medication like finasteride or dutasteride?

most definitely.... that is the reason why DHT blockers eventually lose their efficacy over time

 

[brian liles]

maybe it is a possibility. but not proven

 

[antman]

Maybe more androgen receptors were activated in your scalp. JHDM2A exhibits hormone-dependent recruitment to androgen-receptor target genes, resulting in H3K9 demethylation and transcriptional activation.


I imagine that there is a possibility that these will silence the androgen receptors on your head.

Lipid nanoparticle siRNA systems for silencing the androgen receptor in human prostate cancer In Vivo.


Inhibition of LSD1 by Namoline leads to silencing of AR-regulated gene expression and severely impairs androgen-dependent proliferation in vitro and in vivo. Thus, Namoline is a novel promising starting compound for the development of therapeutics to treat androgen-dependent prostate cancer.


pargyline ia an inhibitor of LSD1. Pargyline blocks demethylation of H3-K9 by LSD1 and consequently androgen-receptor-dependent transcription. Thus, modulation of LSD1 activity offers a new strategy to regulate androgen receptor functions.

 

[DTW]

Thanks for the input guys. This new info definitely concerns me and how I approach my regimen going forward.

Hey Bryan - Why do you think that my accelerated thinning would not be attributed to the up regulation of androgen receptors? I understand that dutasteride reduces serum DHT by 90% and scalp DHT by 55% or something close, so there's still a percentage of DHT circulating. Thanks

 

[Bryan]

Hey Bryan - Why do you think that my accelerated thinning would not be attributed to the up regulation of androgen receptors? I understand that dutasteride reduces serum DHT by 90% and scalp DHT by 55% or something close, so there's still a percentage of DHT circulating. Thanks

Oh, I don't know. I've just never had much interest in the numbers of androgen receptors, compared to the guys who have talked about that subject incessantly on hairloss forums over the years. Personally, I think that the supposed "upregulation" of androgen receptors from finasteride usage happens RAPIDLY (days or weeks), it doesn't happen gradually over a period of a year or two.

 

[abcdefg]

What about trying propecia and then quitting? Would the increase in receptors go back to normal after you quit and if it didnt would that mean your more sensitive to the normal DHT then you were before you used the drug?

 

[Bryan]

What about trying propecia and then quitting? Would the increase in receptors go back to normal after you quit and if it didnt would that mean your more sensitive to the normal DHT then you were before you used the drug?

Yes; my assumption is that the increase in receptors would go back to normal after quitting finasteride.

 

[abcdefg]

Is that increase in receptors just evenly distributed around the whole head or is it more concentrated in the crown then in the front? Do the pseudohermaphradites also have that increase in receptors maybe that is why propecia does not stop hair loss for us like it does for people with no 5-ar2 enzyme?

 

[Bryan]

Is that increase in receptors just evenly distributed around the whole head or is it more concentrated in the crown then in the front?

Good question! I wish Dr. Sawaya had tested that, so she could give us a definitive answer! For all I know, it might actually be more concentrated in the front, than in the crown. (Levels of DHT are apparently higher in the front, according to past studies by Sawaya.)

Do the pseudohermaphradites also have that increase in receptors maybe that is why propecia does not stop hair loss for us like it does for people with no 5-ar2 enzyme?

A really EXCELLENT question!! I wish Dr. Sawaya had tested the hair follicles of pseudohermaphrodites!

 

[DTW]

Interesting...Would the next logical step then to add a topical such as, fluridil or RU?

 

[hammer2012]

bryan are you talking about this dr sawaya

https://docs.google.com/viewer?a=v&q=ca ... jtM5vONv7Q


:woot:

 

[Bryan]

That does appear to be the Dr. Marty Sawaya that I'm talking about! :woot:

 

[abcdefg]

Since Dr. Sawaya was convicted of a felony it seems maybe her studies are not the most reliable sources of information.

 

[abcdefg]

The idea of propecia significantly raising receptors makes me pretty nervous when I still have most of my hair. I mean the number of receptors is basically why we go bald in the first place (also sensitivity) increasing the amount of them just sounds like its going to make your hair loss worse and I would like to see some proof those receptors go back to normal after you stop which I doubt there exists any.
I think a case could be made in younger guys with most of their hair propecia could make it worse. The merck study was mainly on men with some serious hair loss in only certain parts.

 

[abcdefg]

Bryan what are your thoughts on the theoretical approach of CB or ascj 9 by targeting the receptors? A few studies I read from their trials they said it could block not only DHT but also testosterone and maybe other forms of androgens from binding to hair. Do you think if that was the case and nearly all androgens were blocked that male pattern baldness would stop completely or would you still get a mature hair line with age?
Of course this assumes these turn out powerful enough to do this and everything works out which if a big if in the world of science and of course the money to make it all happen.

 

[Bryan]

Bryan what are your thoughts on the theoretical approach of CB or ascj 9 by targeting the receptors?

I'm all for such approaches, as long as they actually work by binding androgen receptors...

A few studies I read from their trials they said it could block not only DHT but also testosterone and maybe other forms of androgens from binding to hair. Do you think if that was the case and nearly all androgens were blocked that male pattern baldness would stop completely or would you still get a mature hair line with age?

Even pseudohermaphrodites appear to maintain their original hair lines, so yeah, if these new treatments really do block "nearly all androgens", I would expect male pattern baldness to stop completely.

Of course this assumes these turn out powerful enough to do this and everything works out which if a big if in the world of science and of course the money to make it all happen.

Agreed. Let's see how well they actually work in practice, not just in theory.

 

[zeroes]

I presume binding is safer than blocking? In theory you wouldn't get the sexual sides you do from finasteride?