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I think I can be of assistance here concerning receptors...
Dr. Christopher Sinal offers up a great synopsis and dichotomy of what receptor theory is all about (found in the link to the powerpoint below). It will take most of you some time to read this so I'll breifly explain a few thoughts, however if you read anything, skip to the part where it discusses "receptor desensitization"
http://pharmacology.medicine.dal.ca/undergraduate/Sinal_Receptors.pdf
I have used this powerpoint to illustrate the basics of how receptors work in the past and I believe it can also benefit your understanding as a general population or "brotherhood" if you will.
Terms to look up that will help you:
Ligand
Desensitization
Agonist
Antagonist
Pharmacokinetics
Now, to get started we must first understand that all receptors are not alike, but do function in a similar manner when considering ineteraction and binding process. Sinal defines a receptor as:
The term “receptor” specifically refers to proteins that participate in intracellular
communication via chemical signals
The three basic parts in a receptor reaction are the receptor itself, a ligand, and an ion channel. Ligands can be hormones or neurotransmitters that look for a "target" cell in order to accomplish their programmed function. Please see the slide that diagrams the Lock and Key Model Ligand-Receptor Interaction (which is a brilliant analogy by the way!)
Drugs are either Agonists or Antagonists. Agonists mimick the response of a naturally occuring ligand to get the target cells to perform the specific action they are designed to do because they may currently be underperforming. An Antagonist is just the opposite, it forces itself into a binding position to prevent the naturally ocurring target cells from joining with natural ligands or agenst that may be "overactive". An example of an Antagonist would be an Aromatase Inhibitor like Arimidex.
Now, as far as receptors being "saturated", that is untrue. Receptors automatically upregulate as more and more andrigens enter your body. Old cells die and new ones are born. However, the effectiveness of the existing cells can diminish over time and also the effectiveness of NEW cells can be diminished by the "reduction of receptor-coupled signaling components." In effect, it is talking about the ion channels losing their efficiency because they do not upregulate like the cells do. Liken it to a highway with a regular amount of cars and no guard rails. As the highway becomes more crowded and cars fall off the road, there will be room for new cars. However, after a period of time, the road will wear down and more cars will fall victim to the highway and it will be an even less effective at doing it's job of transporting cars. To stem this, you shut the highway down, make some repairs and then reopen the road
That last analogy is the one I'm most proud of because it makes perfect sense and I thought of it after many months of research
The next part is very important, so listen up. There is a constant battle within your body between outside forces and homeostasis. After a period of time, everyone's healthy body strives to achieve this homeostatic state. This "fight" will have some casualties, usually in the form of diminished results (very closely related to the economic platform of the Law of Diminishing Marginal Value for you business majors out there). Another aspect along the same line is Physiological Adaptation. If your body reacted the same to a drug every time you used it, then there would be no need ever to create new drugs with the same purpose. Dr. Sinal describes this adaptation as:
"reduction or amelioration of drug effects due to opposing homeostatic response"
For a more clear picture, you have to consider the fact that androgens are already present in the body. The agonist or exogenous agent enters the body and tricks the target cells into thinking the body is naturally producing more. So, the receptor function changes or "adapts" into more of a short term plan as far as individual receptor effectiveness. The focus shifts to creating new receptors to keep up with the demand. As the incoming squadron of androgens begins to level off (peak blood plasma levels), the body will once again search for a route to homeostasis. As upregulation slowly falls, the body realizes that it can adapt to the incoming hoard and it doesn't need to utilize all of the incoming androgens to be "successful." This sounds like bad news, but it's not all bad. If the body did not react in such a way it really would be possible to "fry" receptors because of overuse.
I hope everyone can understand this and please feel free to let me know if you have questions. BTW, all of these words are mine through research unless otherwise stated (specifically quotes or when I use Dr. Sinal's name to give credit). If you are interested at all please look at the powerpoint as it is a fantastic read and includes invaluable diagrams.
Overview and Thoughts
- Receptors upregulate with exogenous androgen introduction
- Receptors lose their efficiency through damaged or overused passageways known as ion-channels
- The body can adapt to an onslaught over time
- "rest" or non-use for a period of time will allow the same upregulation again, but the body will likely recover homeostasis quicker
- this is why some people get the same results at different dosages
- it is my advice that you exhaust each drug before moving on to the next one so you can maximize the results of each cycle
- homeostasis CAN be achieved with TRT
- balsting and cruising can be effective if you are switching up compounds and monitoring your bloods regularly
- I CAN'T STRESS THIS ENOUGH.... GET REGULAR BLOOD TESTS TO SEE WHERE YOU ARE AT!
Dr. Christopher Sinal offers up a great synopsis and dichotomy of what receptor theory is all about (found in the link to the powerpoint below). It will take most of you some time to read this so I'll breifly explain a few thoughts, however if you read anything, skip to the part where it discusses "receptor desensitization"
http://pharmacology.medicine.dal.ca/undergraduate/Sinal_Receptors.pdf
I have used this powerpoint to illustrate the basics of how receptors work in the past and I believe it can also benefit your understanding as a general population or "brotherhood" if you will.
Terms to look up that will help you:
Ligand
Desensitization
Agonist
Antagonist
Pharmacokinetics
Now, to get started we must first understand that all receptors are not alike, but do function in a similar manner when considering ineteraction and binding process. Sinal defines a receptor as:
The term “receptor” specifically refers to proteins that participate in intracellular
communication via chemical signals
The three basic parts in a receptor reaction are the receptor itself, a ligand, and an ion channel. Ligands can be hormones or neurotransmitters that look for a "target" cell in order to accomplish their programmed function. Please see the slide that diagrams the Lock and Key Model Ligand-Receptor Interaction (which is a brilliant analogy by the way!)
Drugs are either Agonists or Antagonists. Agonists mimick the response of a naturally occuring ligand to get the target cells to perform the specific action they are designed to do because they may currently be underperforming. An Antagonist is just the opposite, it forces itself into a binding position to prevent the naturally ocurring target cells from joining with natural ligands or agenst that may be "overactive". An example of an Antagonist would be an Aromatase Inhibitor like Arimidex.
Now, as far as receptors being "saturated", that is untrue. Receptors automatically upregulate as more and more andrigens enter your body. Old cells die and new ones are born. However, the effectiveness of the existing cells can diminish over time and also the effectiveness of NEW cells can be diminished by the "reduction of receptor-coupled signaling components." In effect, it is talking about the ion channels losing their efficiency because they do not upregulate like the cells do. Liken it to a highway with a regular amount of cars and no guard rails. As the highway becomes more crowded and cars fall off the road, there will be room for new cars. However, after a period of time, the road will wear down and more cars will fall victim to the highway and it will be an even less effective at doing it's job of transporting cars. To stem this, you shut the highway down, make some repairs and then reopen the road
That last analogy is the one I'm most proud of because it makes perfect sense and I thought of it after many months of research
The next part is very important, so listen up. There is a constant battle within your body between outside forces and homeostasis. After a period of time, everyone's healthy body strives to achieve this homeostatic state. This "fight" will have some casualties, usually in the form of diminished results (very closely related to the economic platform of the Law of Diminishing Marginal Value for you business majors out there). Another aspect along the same line is Physiological Adaptation. If your body reacted the same to a drug every time you used it, then there would be no need ever to create new drugs with the same purpose. Dr. Sinal describes this adaptation as:
"reduction or amelioration of drug effects due to opposing homeostatic response"
For a more clear picture, you have to consider the fact that androgens are already present in the body. The agonist or exogenous agent enters the body and tricks the target cells into thinking the body is naturally producing more. So, the receptor function changes or "adapts" into more of a short term plan as far as individual receptor effectiveness. The focus shifts to creating new receptors to keep up with the demand. As the incoming squadron of androgens begins to level off (peak blood plasma levels), the body will once again search for a route to homeostasis. As upregulation slowly falls, the body realizes that it can adapt to the incoming hoard and it doesn't need to utilize all of the incoming androgens to be "successful." This sounds like bad news, but it's not all bad. If the body did not react in such a way it really would be possible to "fry" receptors because of overuse.
I hope everyone can understand this and please feel free to let me know if you have questions. BTW, all of these words are mine through research unless otherwise stated (specifically quotes or when I use Dr. Sinal's name to give credit). If you are interested at all please look at the powerpoint as it is a fantastic read and includes invaluable diagrams.
Overview and Thoughts
- Receptors upregulate with exogenous androgen introduction
- Receptors lose their efficiency through damaged or overused passageways known as ion-channels
- The body can adapt to an onslaught over time
- "rest" or non-use for a period of time will allow the same upregulation again, but the body will likely recover homeostasis quicker
- this is why some people get the same results at different dosages
- it is my advice that you exhaust each drug before moving on to the next one so you can maximize the results of each cycle
- homeostasis CAN be achieved with TRT
- balsting and cruising can be effective if you are switching up compounds and monitoring your bloods regularly
- I CAN'T STRESS THIS ENOUGH.... GET REGULAR BLOOD TESTS TO SEE WHERE YOU ARE AT!
