What Is Ru58841 Affinity For Androgen Receptors Compared To Testosterone?

[persistentone]

I found a table in a study, and the original study it references, that claim that RU58841 has only 5% of the affinity for the androgen receptor that DHT has. In other words, RU58841 would not be that effective in blocking DHT, if those numbers were true for hair follicle receptors.

Does anyone have data on how well RU58841 competes against testosterone for the same receptors? If DHT is 10 times more potent in binding against receptors than testosterone, that would imply that RU58841 and testosterone compete about equally well for receptor access? It would be good to have hard data, if a study exists.

If the above is even close to true, that might imply that the effectiveness of RU58841 is more tied to its ability to block testosterone than DHT.

 

[Ollie]

I found a table in a study, and the original study it references, that claim that RU58841 has only 5% of the affinity for the androgen receptor that DHT has. In other words, RU58841 would not be that effective in blocking DHT, if those numbers were true for hair follicle receptors.

Does anyone have data on how well RU58841 competes against testosterone for the same receptors? If DHT is 10 times more potent in binding against receptors than testosterone, that would imply that RU58841 and testosterone compete about equally well for receptor access? It would be good to have hard data, if a study exists.

If the above is even close to true, that might imply that the effectiveness of RU58841 is more tied to its ability to block testosterone than DHT.

There is no anti-androgen in the world that is anywhere remotely close to the binding affinity to that of even test let alone DHT. That however doesn't matter as long as a great enough concentration of the drug is used.

 

[Zel_[]]

There is no anti-androgen in the world that is anywhere remotely close to the binding affinity to that of even test let alone DHT. That however doesn't matter as long as a great enough concentration of the drug is used.

what concentration is needed?

 

[jd_uk]

There is no anti-androgen in the world that is anywhere remotely close to the binding affinity to that of even test let alone DHT. That however doesn't matter as long as a great enough concentration of the drug is used.

Can you explain that? Wouldn't the DHT beat the antiandrogen regardless of the concentration? I've been holding out for CB but I hear its a lot weaker than RU even.

 

[BetaBoy]

Can you explain that? Wouldn't the DHT beat the antiandrogen regardless of the concentration? I've been holding out for CB but I hear its a lot weaker than RU even.

Some DHT and T will no doubt bind but ultimately it won't have much chance of competing for the AR if RU has saturated the cells.

 

[jd_uk]

Some DHT and T will no doubt bind but ultimately it won't have much chance of competing for the AR if RU has saturated the cells.

Do you think it can work longer term (on its own)? What about other topical AA's?

 

[BetaBoy]

Do you think it can work longer term (on its own)? What about other topical AA's?

I mean anecdotally it has in some individuals but it's all speculation without studies and they won't happen till a topical AA has been market approved.

 

[xaragedom]

In this video is your answer

 

[PuzzleheadedNote3]

From what i recall from.a study its binding affinity is roughly equal or slightly greater than testosterone. Once its metabolized after one half life its binding affinity drops.

The dosage question you have is dependent on competitive inhibition. If 2 ligands have equal binding affinities and are at equal concentration then equal proportions bind to the receptor. If the RU is competing with DHT the only way to outcompete it with its lower binding affinity is to overwhelm it by sheer volume. The higher the proportion the better it can compete with the higher binding affinity ligand.

 

[trialAcc]

I mean anecdotally it has in some individuals but it's all speculation without studies and they won't happen till a topical AA has been market approved.

Kintor topical AA phase 2 will be completed by end of June at the latest. If they publish the data we'll get a great idea of what's possible.

 

[Valkyyr]

Except dht is converted from testosterone directly in the hair follicle.