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Receptor Saturation.


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Is it true that the modern belief on receptor saturation from AAS is that it does not take place but instead an eventual lack of results at a certain dose is overcome by an increased dose to keep up with the increased muscle mass?

Just asking.

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A contentious issue. Conventional pharmacodynamics would suggest that receptor saturation occurs resulting in no extra benefit to higher dosages past a certain point. However there is evidence to suggest that receptor downgrade doesn't happen with the androgen receptor, in fact there is evidence to the contrary. It appears that androgen receptors are actually up-regulated. In either case principles of pharmacotherapy still apply, use the lowest dose/number of drugs to achieve a desired effect.

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Interesting topic with lots of conflicting views.

When looking at purely testosterone only, if you require more and more test to get the same benefit then are patients on TRT prescribed the same doses year and year or do they have to continually increase their doses?

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A contentious issue. Conventional pharmacodynamics would suggest that receptor saturation occurs resulting in no extra benefit to higher dosages past a certain point. However there is evidence to suggest that receptor downgrade doesn't happen with the androgen receptor, in fact there is evidence to the contrary. It appears that androgen receptors are actually up-regulated. In either case principles of pharmacotherapy still apply, use the lowest dose/number of drugs to achieve a desired effect.

How I understand receptors in general is: most receptors like other cellular proteins are constantly being synthesised and broken down. If a hormone is present in excess the numbers of target-cell receptors may decrease IE: down-regulation...

Down-regulation makes a target cell less sensitive to a hormone.

In contrast when a hormone is deficient, the number of receptors may increase..

That's interesting regarding androgen receptors not following the same protocol Riccardo, I have read similar. Is it because androgen receptors are nuclear and located in the cytosol (intracellular) rather than membrane...?

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