Tamoxifen, Clomid, Toremifene and Rolaxifene. Which for what?

[Swifto]

Swifto I got a question for you. I realize this probably hasn't been studied so you prob dont have the answer but I figured if anyone knew you prob would... Do any SERMS act as agonist on the AR? I have heard that estrogen can upregulate the ar so this would be very useful if one of them did.

Some SERMs such as Tamoxifen and Toremifene act by reducing AR gene transcription. But only in certain cell types, such as prostate cells, as stated in this study.

To quote from the study, "These results highlight the anti-androgenic aspect of anti-estrogens and estrogens in regard to the AR-mediated transcription of the relevant genes in prostate cancer."

But thats for prostate cells and cancer cells. Not the AR in muscle.

I think I know where your going with your question and taking SERMs wont boost AR gene-transcription when on cycle, I dont think. The only data I've seen is of the contrary. That they will reduce AR gene-transcription in specific tissues.

Estrogen is needed and aromotasation is responsible for the increase in GH and IGF we get when taking exo. testosterone. I think thats what matters more, not whether SERMs increase or decrease AR gene transcription.

I hope that sheds more light on your question.

[Dog-Slime]

Some SERMs such as Tamoxifen and Toremifene act by reducing AR gene transcription. But only in certain cell types, such as prostate cells, as stated in this study.

To quote from the study, "These results highlight the anti-androgenic aspect of anti-estrogens and estrogens in regard to the AR-mediated transcription of the relevant genes in prostate cancer."

But thats for prostate cells and cancer cells. Not the AR in muscle.

I think I know where your going with your question and taking SERMs wont boost AR gene-transcription when on cycle, I dont think. The only data I've seen is of the contrary. That they will reduce AR gene-transcription in specific tissues.

Estrogen is needed and aromotasation is responsible for the increase in GH and IGF we get when taking exo. testosterone. I think thats what matters more, not whether SERMs increase or decrease AR gene transcription.

I hope that sheds more light on your question.

Yes it does. I figured as much but it would be great to have something that could upregulate receptors in my arsenal. Maybe one day such a thing will exist...

[Swifto]

Yes it does. I figured as much but it would be great to have something that could upregulate receptors in my arsenal. Maybe one day such a thing will exist...

Oh, thats where your going...

Well...

Here's something on L-carnitine L-tartrate showing "upregulation of AR content".


Human Performance Laboratory, Department of Kinesiology, University of Connecticut, Storrs, CT 06269-1110, USA. [email protected]

PURPOSE: The purpose of this investigation was to determine the effects of 3 wk of L-carnitine L-tartrate (LCLT) supplementation and post-resistance-exercise (RE) feeding on hormonal and androgen receptor (AR) responses. METHODS: Ten resistance-trained men (mean+/-SD: age, 22+/-1 yr; mass, 86.3+/-15.3 kg; height, 181+/-11 cm) supplemented with LCLT (equivalent to 2 g of L-carnitine per day) or placebo (PL) for 21 d, provided muscle biopsies for AR determinations, then performed two RE protocols: one followed by water intake, and one followed by feeding (8 kcal.kg body mass, consisting of 56% carbohydrate, 16% protein, and 28% fat). RE protocols were randomized and included serial blood draws and a 1-h post-RE biopsy. After a 7-d washout period, subjects crossed over, and all experimental procedures were repeated. RESULTS: LCLT supplementation upregulated (P<0.05) preexercise AR content compared with PL (12.9+/-5.9 vs 11.2+/-4.0 au, respectively). RE increased (P<0.05) AR content compared with pre-RE values in the PL trial only. Post-RE feeding significantly increased AR content compared with baseline and water trials for both LCLT and PL. Serum total testosterone concentrations were suppressed (P<0.05) during feeding trials with respect to corresponding water and pre-RE values. Luteinizing hormone demonstrated subtle, yet significant changes in response to feeding and LCLT. CONCLUSION: In summary, these data demonstrated that: 1) feeding after RE increased AR content, which may result in increased testosterone uptake, and thus enhanced luteinizing hormone secretion via feedback mechanisms; and 2) LCLT supplementation upregulated AR content, which may promote recovery from RE.

Androgenic responses to resistance exercise: effec...[Med Sci Sports Exerc. 2006] - PubMed Result


Hows that?