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So called "bridging" steroids

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Par Deus
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Considering that androgens exert their anabolic effects and the inhibitory effects on the HPTA at the androgen receptors, it seems that their are only two factors that should be looked at when determining the proper bridge steroid, if there is such a thing.

1) What happens to the androgen, as far as enzymes acting on it, centrally vs. in peripherally (particularly muscle tissue). For instance, if 5-alpha reductase activity is higher in the brain than blood and muscle, nandrolone should be a good candidate because it would be a stronger androgen in the muscle than in the CNS.

Likewise, DHT is a bad candidate because it is deactivated in muscle tissue (via 3-alpha). So, ideally, we would have a modest androgen, in the blood, which would become a stronger androgen in the muscle (via 3-alpha HSD) and a weaker androgen in the brain, via 5-alpha reductase.

2) It would cross the BBB poorly vs. entering the muscle cell.

A third would be Bill R.'s so-called "class 2 steroid", which should be ideal, as it would increase protein synthesis outside the AR (where HPTA inhibition would be signalled).

Also, obviously, any candidate should not have estrogenic activity.

Has anyone seen it approached from this perspective, previously?? Can anyone think of any other variables?? Opioid activity maybe (they suppress testosterone).

par deus

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nightop
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Not sure if this is relevant or not, but I remember reading (and later asking) about an article on "non-steroidal androgens" from muscle monthly (i think).

They named two obscure drugs, which I have yet to hear anything further about (anywhere).

Off the top of my head, maybe they would be similiar to what you are talking about in that; if they would be potentially useful for muscle growth and are androgens (they bind to androgen receptors... by definition) yet "non-steroidal" (I'm taking this to mean do not affect the HPTA/CNS although I'm not sure what this means in terms of enzymes/conversions), then possibly they are tissue specific androgens (in this case skeletal muscle specific)???

Regardless, I have often wondered why there have not been further steps in such a direction... My reasoning is that we can design drugs that bind to receptors in target tissues and not in other tissues... for instance, Nolvadex is breast tissue specific... Why are there not "fast-twitch muscle specific androgens" or at least steps towards them?? If such designer androgens/drugs were in fact possible, one could theoretically avoid virtually all of the negatives/side effects and dangers.... the same would hold true for positively controlling many things even from a simple health standpoint (i.e. cholesterol ratios, bone density, heart health, etc.....) Although, IMO it would take quite some time (if ever) to fully understand the biological implications of such (read *ridiculously complex body* as we all know), maybe it would be less so with the androgens....

Thoughts on this?

Personally/morally I would most likely refrain from the more exotic, but the safety of the androgens would be very interesting.

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ChemicalPA
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Posted by: @nightop
Not sure if this is relevant or not, but I remember reading (and later asking) about an article on "non-steroidal androgens" from muscle monthly (i think).

They named two obscure drugs, which I have yet to hear anything further about (anywhere).

Off the top of my head, maybe they would be similiar to what you are talking about in that; if they would be potentially useful for muscle growth and are androgens (they bind to androgen receptors... by definition) yet "non-steroidal" (I'm taking this to mean do not affect the HPTA/CNS although I'm not sure what this means in terms of enzymes/conversions), then possibly they are tissue specific androgens (in this case skeletal muscle specific)???

Regardless, I have often wondered why there have not been further steps in such a direction...  My reasoning is that we can design drugs that bind to receptors in target tissues and not in other tissues... for instance, nolvadex is breast tissue specific...  Why are there not "fast-twitch muscle specific androgens" or at least steps towards them??  If such designer androgens/drugs were in fact possible, one could theoretically avoid virtually all of the negatives/side effects and dangers....  the same would hold true for positively controlling many things even from a simple health standpoint (i.e. cholesterol ratios, bone density, heart health, etc.....)  Although, IMO it would take quite some time (if ever) to fully understand the biological implications of such (read *ridiculously complex body* as we all know), maybe it would be less so with the androgens....

Thoughts on this?

Personally/morally I would most likely refrain from the more exotic, but the safety of the androgens would be very interesting.

I wrote that article and it was based on a patent. Although the patent stated these compounds had a very good ratio of anabolic to suppressive activity, they still were suppressive at high enough dosages. Still, it seemed promising. Doubt they will ever be developed to the point where they hit the market. Never know though

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ChemicalPA
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1) What happens to the androgen, as far as enzymes acting on it, centrally vs. in peripherally (particularly muscle tissue). For instance, if 5-alpha reductase activity is higher in the brain than blood and muscle, nandrolone should be a good candidate because it would be a stronger androgen in the muscle than in the CNS.

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Nandrolone is actually very suppressive. It can aromatize to estrogens (which are very suppressive) and it can also activate progesterone receptors (which will instigate suppression by the progesterone pathway)

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Likewise, DHT is a bad candidate because it is deactivated in muscle tissue (via 3-alpha). So, ideally, we would have a modest androgen, in the blood, which would become a stronger androgen in the muscle (via 3-alpha HSD) and a weaker androgen in the brain, via 5-alpha reductase.

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You completely screwed up your thought process here. Read again. And stop being such a fuck up (slap!!)

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A third would be Bill R.'s so-called "class 2 steroid", which should be ideal, as it would increase protein synthesis outside the AR (where HPTA inhibition would be signalled).

---------

how could their be such steroids? If they actually existed then they would show no androgenic activity, right? Yet D-bol, Abombs'>Anadrol etc. all are quite androgenic. This theory is swiss cheese

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The best bridging steroid would be proviron, as in doses of 100mg a day it shows little or no suppression. Of course, after a suppressive cycle I doubt proviron is gonna make your recovery any better.

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OVRTrainer
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But would proviron actually "assist" in holding on to muscle mass during recovery?

What are your thoughts about low dose Halotestin?


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Par Deus
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Posted by: @PA System
Nandrolone is actually very suppressive.  It can aromatize to estrogens (which are very suppressive) and it can also activate progesterone receptors (which will instigate suppression by the progesterone pathway)

Knew about estrogen. Thought either prolactin or progesterone could lower test, but I was not sure, so I did not comment.

So, now, we can add progesterone agonism, to things we need to avoid.

par deus

Juggernaut, bitch!!


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Par Deus
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Posted by: @PA System
Likewise, DHT is a bad candidate because it is deactivated in muscle tissue (via 3-alpha). So, ideally, we would have a modest androgen, in the blood, which would become a stronger androgen in the muscle (via 3-alpha HSD) and a weaker androgen in the brain, via 5-alpha reductase.

---------------

You completely screwed up your thought process here.  Read again.  And stop being such a fuck up (slap!!)

-----------

A third would be Bill R.'s so-called "class 2 steroid", which should be ideal, as it would increase protein synthesis outside the AR (where HPTA inhibition would be signalled).

---------

how could their be such steroids?  If they actually existed then they would show no androgenic activity, right?  Yet d-bol, anadrol etc. all are quite androgenic.  This theory is swiss cheese

------------

The best bridging steroid would be proviron, as in doses of 100mg a day it shows little or no suppression.  Of course, after a suppressive cycle I doubt proviron is gonna make your recovery any better.

I think I just made it confusing. We do want an androgen that 3-alpha HSD makes more potent, because 3-alpha is present in high concentrations in muscle (where anabolism is stimulated) vs. the CNS, correct??

And, the vice-versa for 5-alpha reductase. It is high in the brain, so we want a steroid that is deactivated by it, because HTPA inhibition occurs there.

I know just the opposite happens to DHT, but I am referring to a theoretical perfect bridging steroid, whose Form (who knew Plato would be useful) may or may not exist.

par deus

Juggernaut, bitch!!


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Par Deus
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Topic starter  
Posted by: @PA System
A third would be Bill R.'s so-called "class 2 steroid", which should be ideal, as it would increase protein synthesis outside the AR (where HPTA inhibition would be signalled).

---------

how could their be such steroids?  If they actually existed then they would show no androgenic activity, right?  Yet d-bol, anadrol etc. all are quite androgenic.  This theory is swiss cheese

I agree completely (thus the "so-called" comment), and for the exact same reason.

par deus

Juggernaut, bitch!!


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vito
 vito
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is there such a thing as a selective androgen receptor antagonist? kinda like clomid or Nolvadex where it would act as an androgen where we want it to but block the effects of androgens in places like the hypothalmus? i would imagine that if such a substance exsisted people would be all over it already but just thought i'd ask anyway.


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Par Deus
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Posted by: @vito
is there such a thing as a selective androgen receptor antagonist?  kinda like clomid or Nolvadex where it would act as an androgen where we want it to but block the effects of androgens in places like the hypothalmus?

I have a theory for getting that done. Pat thinks I am crazy. I think the theory is sound, if an assumption I am making is correct (have to look at some studies), so we will see.

par deus

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RoyHarper
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Posted by: @Par Deus
is there such a thing as a selective androgen receptor antagonist?  kinda like clomid or Nolvadex where it would act as an androgen where we want it to but block the effects of androgens in places like the hypothalmus?

I have a theory for getting that done. Pat thinks I am crazy. I think the theory is sound, if an assumption I am making is correct (have to look at some studies), so we will see.

The first thing to consider, in my opinion, is not the the drug that is acting on the receptor, but the enzymes that act on the drug; simmilar to 5ar.


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nightop
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*Or* even a hypothalamus specific AR antagonist which didn't really act (as an antagonist or agonist) on any other ARs/tissues.... This way one could simply use it in conjunction with a common cycle of 1-test (or other AAS) to prevent HPTA inhibition...

While we are coming up with interesting ideas like this, if such designer drugs do become common/possible, you could even make an AR blocker that is heart/cardiac - tissue specific.... although, I think there might be a few benefits to a stronger heart... so I don't know on this one.

If only the public/medical community understood what could be done with such possibilities.... designer drugs could be a much safer and more powerful means to achieve health goals (use in diseased/wasting patients, aging, etc....).

Just out of curiosity, surely there is another country (europe somewhere?) that is a little further down the road than we are in this regard, has no laws against AAS, and has a better public opinion of such?

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Ex_banana-eater
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If you are getting to the point where you have to bridge to retain mass (obviously competitive bodybuilder), just go like this
1-8 AAS
8-16 Gh and Insulin with proper breaks recquired. (include your HCG and anti-e's at this time)
16-24 AAS & Glucophage
repeating on and on

or you could do 12 week cycles which would probably work better.

"The Cretan Liar." He might have written "This proposition is false" instead of "I am lying." The answer would be: "Very well, but which proposition do you mean?" -- "Well, this proposition." -- "I understand, but which is the proposition mentioned in it?" -- "This one." -- "Good, and which proposition does it refer to?" and so on. Thus he would be unable to explain what he means until he passes to a complete proposition.--Ludwig Wittgenstein, Zettel


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duque21
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Posted by: @Ex_banana-eater
If you are getting to the point where you have to bridge to retain mass (obviously competitive bodybuilder), just go like this
1-8 AAS
8-16 Gh and Insulin with proper breaks recquired. (include your HCG and anti-e's at this time)
16-24 AAS & Glucophage
repeating on and on

or you could do 12 week cycles which would probably work better.

Again will some one ban this kid!

You'r running the wrong way with the ball, GET OFF THE FIELD!!!!


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Dante
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I'm not going to ban him. If his logic isn't sound, then attack that.

Man to his doom goes driving down; a crown of thorns is still a crown!

Crowley


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