Idk if anyone else has done a thread on this shit but anyway.
First of all, before everyone can listen to how and why forskolin can increase androgen sensitivity, we must first grasp what the second is.
The messenger system is.
Basically, when a hormone like luteinizing hormone (LH), for example, wants a cell to like, do something, it cannot go straight into the
cell. It binds to a receptor on the outside of the cell membrane. The receptor triggers an enzyme within the membrane to be able to send a
second messenger into the nucleus to alter DNA.
Forskolin just bypasses this shit entirely (the outside receptor). Being a highly lipophilic labdane diterpene, forskolin just phases right
through the cell membrane. Once inside, it directly binds to and activates an enzyme called adenyl cyclase (AC) [1].
Once activated, AC grabs ATP and converts it into cAMP (Cyclic adenosine monophosphate). By bypassing the receptor, forskolin forces the
cell's hand and makes the cell flood its own cytoplasm with cAMP, completely detached from the body's natural hormonal commands.
Now you may be asking, how the fuck would this translate to androgen receptor sensitivity?
Well, we should all know that even if we have high test scores, it's worthless if the AR is dormant. So basically, forskolin amplifies the AR through a
master enzyme called:
Protein Kinase A (PKA)
cAMP is the key for PKA. So when cAMP levels fucking surge from the forskolin you're taking, PKA wakes up and begins phosphorylating
(Definition: introducing a phosphate group into a molecule or compound). PKA directly phosphorylates specific serine residues on the
Androgen Receptor itself [2].
When the AR is phosphorylated by PKA, its 3D shape (physical shape) changes. This new shape increases the affinity with which it binds.
Therefore, the receptor is now hypersensitive, meaning it will aggressively bind to whatever amount of testosterone is in your blood, taking
maximum amounts, even if your test is average.
Some even crazier shit is that in some clinical observations, the Forskolin-induced cAMP/PKA cascade is so fucking strong it can force the
ARtravelsl into the nucleus and triggers muscle-building gene transcription even without testosterone attached to it [3].
But it doesn't just make the muscle cells sensitive (like our hearts). It affects the testicles to produce more testosterone in
general.
Normally, the pituitary sends LH to the Leydig cells in the testes. LH binds to the Leydig cell wall, which activates AC, raising cAMP, and
tells the cell to make a test.
Because forskolin raises cAMP everywhere, it mimics a massive pulse of LH inside the Leydig cells, and the brain doesn't have to send a
signal. Now, what's the limiting factor of how many tests your body can make and transport? Well, it's called StAR (Steroidogenic Acute
Regulatory protein) and it's a transport protein [4]. Its job is to carry the raw cholesterol into the mitochondria so it gets turned into
testosterone.
Now, when forskolin induces a surge in cAMP/PKA, it directly forces the transcription of the StAR gene. More of this shit is made, more
cholesterol goes into the mitochondria, and then the Leydig cells become Chinese sweatshop test factories [5].
From looking at it at a certain angle, to me at least, you are aiming for 25mg to 50mg of active, pure Forskolin entering the bloodstream daily; however, dosings can change depending on what you want from it.
---
* [1] Seamon, K. B., et al. (1981). Forskolin: unique diterpene activator of adenylate cyclase in membranes and in intact cells.
Proceedings of the National Academy of Sciences.
* [2] Nazareth, L. V., & Weigel, N. L. (1996). Activation of the human androgen receptor through a protein kinase A signaling pathway.
Journal of Biological Chemistry.
* [3] Sadar, M. D. (1999). Androgen-independent induction of prostate-specific antigen gene expression via cross-talk between the androgen
receptor and protein kinase A signal transduction pathways. Journal of Biological Chemistry.
* [4] Stocco, D. M. (2001). StAR protein and the regulation of steroid hormone biosynthesis. Annual Review of Physiology.
* [5] Godard, M. P., et al. (2005). Body composition and hormonal adaptations associated with forskolin consumption in overweight and
obese men. Obesity Research.
Disclaimer
This is all hypothetical and satire and none of my beliefs reflect what happens here
as always have a great day
First of all, before everyone can listen to how and why forskolin can increase androgen sensitivity, we must first grasp what the second is.
The messenger system is.
Basically, when a hormone like luteinizing hormone (LH), for example, wants a cell to like, do something, it cannot go straight into the
cell. It binds to a receptor on the outside of the cell membrane. The receptor triggers an enzyme within the membrane to be able to send a
second messenger into the nucleus to alter DNA.
Forskolin just bypasses this shit entirely (the outside receptor). Being a highly lipophilic labdane diterpene, forskolin just phases right
through the cell membrane. Once inside, it directly binds to and activates an enzyme called adenyl cyclase (AC) [1].
Once activated, AC grabs ATP and converts it into cAMP (Cyclic adenosine monophosphate). By bypassing the receptor, forskolin forces the
cell's hand and makes the cell flood its own cytoplasm with cAMP, completely detached from the body's natural hormonal commands.
Now you may be asking, how the fuck would this translate to androgen receptor sensitivity?
Well, we should all know that even if we have high test scores, it's worthless if the AR is dormant. So basically, forskolin amplifies the AR through a
master enzyme called:
Protein Kinase A (PKA)
cAMP is the key for PKA. So when cAMP levels fucking surge from the forskolin you're taking, PKA wakes up and begins phosphorylating
(Definition: introducing a phosphate group into a molecule or compound). PKA directly phosphorylates specific serine residues on the
Androgen Receptor itself [2].
When the AR is phosphorylated by PKA, its 3D shape (physical shape) changes. This new shape increases the affinity with which it binds.
Therefore, the receptor is now hypersensitive, meaning it will aggressively bind to whatever amount of testosterone is in your blood, taking
maximum amounts, even if your test is average.
Some even crazier shit is that in some clinical observations, the Forskolin-induced cAMP/PKA cascade is so fucking strong it can force the
ARtravelsl into the nucleus and triggers muscle-building gene transcription even without testosterone attached to it [3].
But it doesn't just make the muscle cells sensitive (like our hearts). It affects the testicles to produce more testosterone in
general.
Normally, the pituitary sends LH to the Leydig cells in the testes. LH binds to the Leydig cell wall, which activates AC, raising cAMP, and
tells the cell to make a test.
Because forskolin raises cAMP everywhere, it mimics a massive pulse of LH inside the Leydig cells, and the brain doesn't have to send a
signal. Now, what's the limiting factor of how many tests your body can make and transport? Well, it's called StAR (Steroidogenic Acute
Regulatory protein) and it's a transport protein [4]. Its job is to carry the raw cholesterol into the mitochondria so it gets turned into
testosterone.
Now, when forskolin induces a surge in cAMP/PKA, it directly forces the transcription of the StAR gene. More of this shit is made, more
cholesterol goes into the mitochondria, and then the Leydig cells become Chinese sweatshop test factories [5].
From looking at it at a certain angle, to me at least, you are aiming for 25mg to 50mg of active, pure Forskolin entering the bloodstream daily; however, dosings can change depending on what you want from it.
---
* [1] Seamon, K. B., et al. (1981). Forskolin: unique diterpene activator of adenylate cyclase in membranes and in intact cells.
Proceedings of the National Academy of Sciences.
* [2] Nazareth, L. V., & Weigel, N. L. (1996). Activation of the human androgen receptor through a protein kinase A signaling pathway.
Journal of Biological Chemistry.
* [3] Sadar, M. D. (1999). Androgen-independent induction of prostate-specific antigen gene expression via cross-talk between the androgen
receptor and protein kinase A signal transduction pathways. Journal of Biological Chemistry.
* [4] Stocco, D. M. (2001). StAR protein and the regulation of steroid hormone biosynthesis. Annual Review of Physiology.
* [5] Godard, M. P., et al. (2005). Body composition and hormonal adaptations associated with forskolin consumption in overweight and
obese men. Obesity Research.
Disclaimer
This is all hypothetical and satire and none of my beliefs reflect what happens here
as always have a great day
