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 Anabolic Discussion Board
 Receptor Downgrading (hmmm)
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| Author | Topic: Receptor Downgrading (hmmm) | ||
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Pro Bodybuilder 
Posts: 488 |
Im glad the subject of Receptor Downgrading is finally being broached. Many of us feel that this is not the case, and is an assumption made without giving consideration to the facts. Endocrinologicly speaking it doesnt make much sense for the anabolic receptors to downgrade so quickly. After all, we are basically creating an intense "second pueberty" when using gear. As you know, when you went through pueberty, it was quite a bit longer than an 8 week ordeal. So whats happening then to cause diminished returns?? Well, as far as can be seen so far, its a case of the body playing hormonal catch up. When the point occurs that gains are slowing (or stopping), it has been assumed that the receptors were clogging, and not responding as well to the AS. This is quite possibly NOT the case! In fact, this may be what occurs... You initially make gains due to the high exogenous testosterone in your system. Then the gains slow. What is occuring is that your endocrine system has noticed the high levels of testosterone in your body. In response, it begins to up estrogen productions to strike the equalibrium it loves so much. (At this point we assume our receptors has down regulated and we cycle off the gear.) What can we do??? Thats a toughie. The obvious answer is anti estrogens, but that isnt neccessarily the best way. Armidex in this case is NOT the best answer (in my opinion), as it is non competatove, and just wipes out estrogen. As we all know, the estrogen works WITH the testosterone to cause muscle growth. So mabye Nolvadex? As a competative inhibitor, it may leave enough free estrogen in the system to be beneficial. I believe this is the reason bridging works, though most of us never looked at it from this angle.     | ||
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Elite Bodybuilder 
Posts: 791 |
Those auxilliaries only come into play with respect to esterefied testosterone. That being said your theory is flawed. The fact of the matter is that the optimal anabolic condition for the body is one where free flowing testosterone is maximized in conjunction with the static elimination of estrogen. For thae explicit purpose Arimidex is the only choice. 1mg table is responsible for as much as a 90% decrease in estrogen. I agree the complete absense of estrogen for a long period of time may not be necessary, it may not be healthy, but then no one told us to take the entire 1mg tablet of Arimidex. The fact of the matter is that proviron and novaldex will always have a place due to their relative expense. There cheap as shit, even with my contacts 2O tablets of Arimidex is close to $200. That was no implicit attempt to advertise myself as a source for Arimidex, e-mail me a request for it, I will simply delete the post without hesitation. ------------------  | ||
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Pro Bodybuilder
Posts: 488 |
LIST ME! Heh heh, you make a good point. I dont use anti estrogens, so I dont really know their best uses. I have nolvadex on hand all the time, but have never needed it. | ||
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Elite Bodybuilder
Posts: 642 |
Interesting subject... I don't have any smart info to provide... Bump! for E2, Macro, GymRat...others | ||
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Elite Bodybuilder
Posts: 791 |
I think receptor down regulation is an unfortunate fact of life. When any receptor sight is bombarded by above than normal stimuli, there is going to have to be a period of rest for the body and all which that encumpases to return to normal. Even persons using therapeutic doses with over the counter medication inevitable meet point where the effectivness of the drug is lessened. ------------------ | ||
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Elite Bodybuilder
Posts: 642 |
Hey guys, I know most people are against the diamond shaped cycles but what do you think of them? When I start a cycle I gain the most weight on week 1 followed by week 2 and then week 3 the other weeks its almost no gains. I was thinking of doing a cycle starting wiht low dosages and work up as the gains slow... week---Sust---dbol What do you think? [This message has been edited by DREXX (edited August 31, 2000).] | ||
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Elite Bodybuilder
Posts: 1229 |
I am the same way Drexx. I always seem to gain really fast at first and then just maintain. That is one of the main reasons I am looking into doing a 2 on/4 off cycle program like Bill Roberts reccommends. One problem with your idea though is that this is not the best way to pyramid up with sust. Let's say for example, you were to take 500 mg per week for 8 weeks. By the time you hit the middle of the cycle you have over a gram of test floating around in your body. With the long acting esters in sust, you would be better off just staying at a consistent level throughout and the sust would pyramid itself up and down without changing doses. But I don't know if pyramiding up and then down would be beneficial with another type of drug. I just know that with sust you do this automatically by staying at a consistent dose. I have never tried tapering up because I have consistantly been told that it is best to start high and stay level with your dosages. So I have never tried it. Maybe someone else has some idea on this.. | ||
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Pro Bodybuilder
Posts: 333 |
I'm with you on this one Monster. I think bridging with a high anabolic and proviron and/or nolvadex is a good idea. I'm gonna give it try when I start bulking again. Later, | ||
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Elite Bodybuilder
Posts: 642 |
I am considering a 4 week cycle as well since my gains are always better at first... WEEK___ENANTHATE___ANADROL I know that sust adds up as it is active for 21 days. I realise this I am not a newbie... When I just inject small dosages there is not much floating around... by the time I start tapering down the test is still very high... This last cycle I did 750mg for 6 weeks and as the weeks went by more test available but less gains... I want to use the min possible and get slow gains at first and then add gear to get more gains... Maybe it will work maybe not... | ||
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Elite Bodybuilder
Posts: 1229 |
I know you are not a newbie, Drexx. Didn't mean to imply that if I did. I was just trying to offer a little assistance, no harm intended. Keep us updated if you decide to try the diamond pattern you described. Peace...Mav | ||
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Elite Bodybuilder
Posts: 642 |
Sorry dude! Didn't mean to rant! I am working 4 to midnight doing tech support for an internet company and I am really fucking stressed out with these fucking stupid people calling me | ||
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Pro Bodybuilder
Posts: 339 |
This was an interesting thread as Monster and Twisted Steel started working it over. Good move, Monster, to get a good, dialectic kind of thread going. I've noted a number of nice posts from you, now that I think about it. I've got nothing to add. Haven't done a cycle yet, myself. Just reading it. Shame none of the mods are jumping in on this. I'll just bump it, and check back on it in awhile. Bjaarki ------------------ BECOME SOMEONE'S HERO! | ||
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Moderator 
Posts: 1697 |
I would jump in...but, in actuality...Twisted_Steele and I discussed this very topic on icq before it was posted...for the record, I do agree with TS.... ------------------ Ranger | ||
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Cool Novice 
Posts: 12 |
I'm interested in this as I am 41 and am almost 2 months off of a sust cycle. 250 per week for twelve weeks. First real cycle and was impressed with the increased strength and loss of body fat. Am interested in the short cycle theory using sust and d-bols along with proviron, only never getting off of the proviron. What do y'all think about this? | ||
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Moderator
Posts: 1512 |
Monster, Where are you getting this info from? The logic of your arguments is not only erroneous but it in fact seems to be Borreson-ian. What I am trying to say is that wherever you are getting your info from you need to find a different source. This is the second EXTREMELY misinformed post that you have made- the first being with regard to anabolic/androgenic ratio of steroids being affected by the type of ester that they are attached to.(which of course they are not) Peace ------------------ | ||
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Pro Bodybuilder
Posts: 330 |
Come on MP, quit sugar coating it - tell us how you really feel. | ||
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Amateur Bodybuilder 
Posts: 292 |
Androgen receptors are always a topic of speculation and misconception. I will NOT tell you that I am an expert on this subject, but I have tried to do a little research on this area. Studies on modulation of the AR are conflicting, since it has been shown to both up-regulate and down-regulate, but researchers believe this observation maybe tissue specific or related to the testing procedures used to observe AR modulation. Also, some researchers have shown down-regulation of AR mRNA expression with an increase in AR protein expression, which is believed to be due to increase in AR protein stability. So new AR production may decrease, but the receptors that form are more stable. Factors that have been shown to up-regulate AR production: FSH, GH, prolactin and epidermal GF. MONSTER has a misconception that I have heard others state, and that is that the body "senses" a high androgen state and attempts to maintain some ratio of test to estrogen. This is not the case. It is simply a matter of chemistry, most notably Le`Chatelier's principle. As you increase the concentration of androgen in the body you drive the reaction forward that governs estrogen production. This is not a true homeostatic effect. What people don't realize about steroids is that their effects are mediated through DNA levels, which takes a bit of time to occur. The drug has to bind the DNA and cause a whole slew of effects before the final effects (muscle gains) are manifested. This maybe the true reason for slower gains during the end of a cycle: the body is simply not able to process all the necessary nucleic material and proteins fast enough, or it is slowing down some of these processes to restore homeostasis. So we maybe beating a dead horse in staring at the AR for the answer, when it maybe a process downstream, that is the rate limiter. | ||
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Elite Bodybuilder
Posts: 642 |
So cockdezl, Would it be better to stick to short cycles 3-5 weeks and when the results slow down. Just stop and take your clomid. Wait till the drugs clear and then a couple more weeks and start another short cycle. I am wondering if I should start doing 4 week cycles followed by 8-9 weeks off and then start over again??? I guess I will have to give it a try. The bulk of my gains (70% +) happen in the first 3 weeks. I will try and see if I can maintain the weight gain on such a short cycle. Lots of people say longer cycles helps solidify your gains... I guess I will have to see for myself what is better... Any opinions.. | ||
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Pro Bodybuilder
Posts: 339 |
Bjaarki says "I knew this would get interesting. Drive on, bros! C'mon Ranger, Twisted Steel! Cockdezl's giving you something to chew on!" <as he thinks to himself "Threads like these are a lot more fun to follow than the usual 'Git Some! Har Har!' stuff we see on this board."> | ||
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Pro Bodybuilder
Posts: 443 |
Interesting.. Now how about steroids like stanozolol and methandienone ? it is said that these have a "weak" binding to the AR. Does that mean that the whole concept of up/downregulating of the AR does not apply to them ?? | ||
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Elite Bodybuilder
Posts: 791 |
Yet another misconception not vocalized by any person on this particular thread, but prevalent enough within the bodybuilding to cause me an axiety attack is the theory of multiple androgen receptors which bind to different form/types of AAS. WROOOOOOOOOOOOOOONG, the differenct betweeen say testosterone and stanazol obviously is within the chemical makeup of each compound. These particular difference will induce divergent rates with respect to receptor up/down regulation. Thirdly, the entire process by which accelerated muscular hypertrophy begins and ends is relative to the individual. Thus, explaining the variance between gains of some relative to others with respect to the begining or ending phase of a cycle. I personally have witnessed within myself and others the obvious stagnation effect which occurs at some given point during an individuals cycle. This is the nature of our body, and the rate by which it changes. Exogenous stimule can cause temporary drastc responses, but our anatomies ingenious design institutes a down regulation of those responses in order to achieve a measure stasis. This is where the issue of continued variance comes into play. Not only with respect to diet and training, but also hormonally. I have not even begun to research the efficacy of shortened cycles to satisfy me. However, something in my minds eye tells me that in theory the idea is sound. Short moderatly intense doses of a particular compound followed by a brief period of cession, then recontinued in an entirely different form. The only question for me is, what is considered a brief period of cessesion, what is enough time to allow a measure of significant receptor down regulation, to best maximize the effectivness of the preceeding short cycle. HMMMMMM ------------------ [This message has been edited by Twisted_Steel (edited September 01, 2000).] | ||
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Amateur Bodybuilder
Posts: 283 |
Don't forget that in an "intense second puberty" thyroid hormone levels, growth hormone levels, and insulin levels would also be significantly increased... ------------------ | ||
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Pro Bodybuilder
Posts: 488 |
Im not even saying I agree with myself! As a matter of fact it was something Borrenson said somewhere... he has some interesting ideas, but a lot of kooky shit too. I honestly just wanted to get a good post going. I just kind of thought of it from a "what if" perspective. I AM interested in bridging and longer cycles,, though. ]Actually Twisted, I agree with you... but its a hell of a thread we got going! | ||
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Pro Bodybuilder
Posts: 443 |
Thanks Twisted.. this is very difficult for me to understand (the language makes it even harder). But i like to know, so thanks for trying  It just sounded logical to me that if a particular as has a very "weak" or "strong" binding to the AR, the up/downregulation would be affected by it..ah well...
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Elite Bodybuilder
Posts: 662 |
Another interesting component (since were taking about DNA binding domains of steroid receptors), is that metal complexation is crucial for the activity of androgenous steroid receptors. Each DNA binding domain has been shown to bind reversibly with two zinc ions. These zinc atoms are also coordinated tetrahedrally by 4 cysteines (amino acids). In rat studies it has been demonstrated that "extremely" elevated estrogen levels resulted in loss of binding capacity with these metal ions, thus a hypothetical loss in binding of the androgen (Samanta). This study is in rats - but DNA (exons) are highly conserved, so it probably has some merit. It should be noted that the steroid hormone expresses itself through conformational changes in the receptor protein, both during and after the binding of that steroid. Thus, it is nearly impossible to make a distinction between the part of the steroid (for example: ring A) responsible for binding and another part (the Pharmacophore) responsible for the expression of the hormone's action. If a steroid binds itself in the proper way - it should always express itself. Then, of course antagonists like Arimidex bind to the receptor leading to a distorted, inactive complex. T.B. Samanta, Steroid Biochemistry., 28 (1987). | ||
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Moderator
Posts: 1697 |
Jack the shit till ya slush when ya walk...take a break, then look in the mirror....don't like what you see...do it again....repeat this process 2 to 3 times per year....see ya at the Mr. " O "!!! Heh heh heh.....Out of my league here bro's, and not ashamed to admit it....this is more along Macro, TS,Cock-whatever, ... etc. ------------------ Ranger | ||
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Elite Bodybuilder
Posts: 642 |
Like to see GymRatSD opinion on this... | ||
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Elite Bodybuilder
Posts: 791 |
What the hell was the point of your post Primo57? ------------------ | ||
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Elite Bodybuilder
Posts: 1229 |
Man, I feel like I am trying to learn a foreign language here. This is way outta my league. | ||
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Freak 
Posts: 1789 |
Great exchange of ideas and information. I would love for this to spin off into Mac's thoughts on dnp and receptors in a new thread. I want to take the stuff, but I cant show up sweating and weak or take 1 week off work. Great thread though. Slopain | ||
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Elite Bodybuilder
Posts: 662 |
TS,Just some crazy shit I was reading the other day, thought it might be interesting, just another piece of info for folks to chew on Basically, it says what you already know (how steroids produce their effects) and gives yet another possible reason why we should take our clomid eod. | ||
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Amateur Bodybuilder
Posts: 251 |
BUMP | ||
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Amateur Bodybuilder
Posts: 212 |
i'm going to throw this into the mix..... Why do some muscle groups have more receptor sites? For me, it's my shoulders...they blow up hard and fast....but my bi's lag no matter what..... | ||
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Amateur Bodybuilder
Posts: 292 |
DREXX, I am sorry, but I really am not the person to give info concerning cycles, since I am not really that experienced with this topic. My experience tends to be longer cycles, since I have had access to longer acting drugs, i.e. Sus, Deca and enanthate. The concept of short cycles is logical and seems to have had good responses in those who I have conversed with. Roberts stated that for those not concerned with HPTA suppression, longer cycles are appropriate since growth is attained faster. DUTCH, the only study I could find showed an up-regulation of AR using oxandrolone, with no increase in IGF-1 levels: Sheffield-Moore M, Urban RJ, Wolf SE, Jiang J, Catlin DH, Herndon DN, Wolfe RR, Ferrando "Short-term oxandrolone administration stimulates net muscle protein synthesis in young men." BILLY, your statement is one I have thought about before also, concerning AR concentrations in the various muscle groups. My conclusion is that these muscle groups are those that tend to be gender phenotypic, i.e. pectorals, deltoids, etc. Since these muscle groups are those that are notably expressive of masculinity (broad shoulders, large flat pectorals, etc.) then they would be those that are most sensitive to the male hormones. Biceps are not that expressive for either sex, then this group would not be as sensitive to hormone stimulation. BUT some have noted that the weak-AR binding steroids, especially methandrostenolone, have a more potent effect on biceps. This maybe due to non-AR related effects in this muscle group. | ||
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Amateur Bodybuilder
Posts: 66 |
I personaly subscribe to the theory of receptor UPREGULATION, pretty much the opposite of the down regulation theory. I think bridges work, I also think that the body copmpensates for the excess tetstosterone by producing MORE receptors (kind of like muscles react to excercise by creating MORE fibers not less in response to the extra stress levels). I probably won't win any scientific arguments with anyone on the subject, I just know what I have seen as effective and not effective in real life...and in my opinion receptors UPREGULATE!!! PEACE! | ||
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Moderator
Posts: 1512 |
more androgen receptors in "good" muscle groups? probably not more sattelite cells in "good" muscle groups? probably ------------------ |
All times are ET (US) | |
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posted August 31, 2000 08:40 PM