How to Reduce/Block Scalp Androgen Receptors -

How to Reduce/Block Scalp Androgen Receptors

Reducing or blocking scalp androgen receptors is possibly the best way to treat male pattern hair loss because it means we can reduce the damaging effect of DHT on the hair without losing the anabolic benefits of DHT.

Androgenic alopecia (AA) is the most prevalent form of hair loss. The pathophysiology of AA is complex. However, one thing is relatively clear: the androgen hormone DHT and scalp androgen receptors are both found in higher levels in bald and balding scalps, compared with healthy scalps.

We also know that reducing scalp DHT and blocking scalp androgen receptors reduces hair loss. Reducing the number of available androgen receptors in the scalp is a smart way to reduce male pattern baldness (MPB). In this article, I’ll explain how you can do that.

How to reduce androgen levels in the scalp

Several chemicals have been shown to block the action of androgen receptors.

Androgen receptor blockers, including spironolactone, cyproterone acetate, and flutamide, have all shown great potential in treating hair loss.


RU58841, in particular, can be applied locally on the scalp, which prevents some serious adverse effects associated with oral administration of androgen receptor blockers and DHT blockers like finasteride.

Several blockers of androgen receptors with non-steroid chemical structure were synthesized recently. They are N-substituted arylthiohydantoins: RU 59063, RU 56187 and RU 58841.[43,44] These are very potent substances. Their affinity for androgen receptors is three times higher than the affinity of testosterone. One of them, RU 58841, is active when applied locally, which is of great benefit considering the significant adverse effects observed after systemic administration. One of the imidazole antimycotics, ketoconazole, is an inhibitor of androgen biosynthesis and also an androgen receptor blocker, however its affinity for androgen receptors is low. Systemic administration of ketoconazole for the treatment of hirsutism requires high doses and is associated with a high incidence of adverse effects.


Retinoic acid (vitamin A derivative)

Numerous factors affect the number and activity of androgen receptors in dermal papilla cells. Retinoic acid (vitamin A derivative), if used for a long time, may reduce the number of androgen receptors by 30 – 40 percent.[29] Vitamin B6 reduces by 35-40% the extent of protein synthesis observed after androgen receptor activation.



EGCG is a polyphenol found in green tea. It’s a powerful antioxidant and has been shown to be very beneficial for reducing hair loss.

Blocking, reducing or ‘blunting’ androgen receptors is an important area of research for treating prostate cancer. The study cited below determined that EGCG has a high affinity for androgen receptors:

EGCG was found to displace Fluormone AL Red from the purified AR-LBD, resulting in a lower FRET ratio, indicating that it competed with a high-affinity labeled AR ligand and physically interacted with the AR-LBD with an IC50 of 0.4 μM


Since EGCG is also an anti-inflammatory and antioxidant, it has great potential as a natural hair loss treatment with no side effects.

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Spironolactone cream for hair loss

Spironolactone is a promising treatment for male pattern hair loss because its a mild androgen receptor blocker as well as a mild DHT blocker.

CB 03 01

CB 03 01 for hair loss

CB 03 01 is perhaps the most exciting of all these potential hair loss treatments. CB 03 01, or Clascoterone, works by competing with DHT for available androgen receptors. Because the chemical has a high affinity for androgen receptor binding it is able to reduce the number of androgen receptors available to DHT and therefore prevent hair loss caused by DHT.