Androgens such as testosterone and DHT exert their beneficial action on the tissue by binding to androgen receptors. Testosterone and DHT are both anabolic to muscle and boosts muscle growth. A recent study found that, although androgens are needed for muscle growth, it is the androgen receptors that are essential for hypertrophy. There is a linear relationship between androgen receptor content and change in lean body mass following weightlifting (18).
The more androgen receptors there are on a certain site, for example in the muscle, the more testosterone can bind and the more powerful effect androgens can exert.
1) Increase DHT
DHT, the more potent form of testosterone, cannot be aromatized and has four times the affinity to androgen receptors as well as takes 5 times as long to dislocate from androgen receptors, thus exerting a much more potent androgenic effect than testosterone. DHT is also able to increase androgen receptors. More on boosting DHT here…
2) Increase Testosterone
Testosterone automatically increases its own receptors (1). When you stimulate a muscle via exercise, testosterone is synthesized locally as well as in the testes. Androgen receptors in that muscle then increase to compensate for the rise in androgens, thus increasing binding sites and interactions so that greater anabolic adaption can take place. In this rat study, testosterone plus progesterone prevented lordosis, and the researchers say that it may be due to an upregulation of androgen receptors by progesterone (15). Read more on 75 ways to boost testosterone here…
3) Decrease Estrogen
Estrogen antagonizes testosterone, increases serotonin and inflammation as well as prolactin. Estrogen is negatively correlated with androgen receptors.
4) Decrease cortisol
Cortisol is catabolic to cellular proteins. Hence, elevated cortisol degrades AR, increases the aromatase and inflammation and can lead to many ailments. Cortisol is effectively countered with adaptogens.
- Suggested reading: Lower cortisol
5) Weight training
Heavy resistance exercise (8-10 reps) increases serum total testosterone and is very effective at up-regulating AR mRNA and protein expression after just 3 exercise sessions (2).
But be careful to not push yourself too hard as too much metabolic stress for overtraining will decrease testosterone, increase cortisol and reduce androgen receptors (15).
- For comprehensive guides on getting swole, strong and shredded, check out my programs on the subject.
6) Eat food
Eating directly post-working is the best thing you can do for gains. This is the time when muscle protein synthesis is the highest and also when your body is able to utilize all the protein you ingest. Massive amounts of protein can be absorbed and utilized directly post-workout. Protein also decreases SHBG, which increases free testosterone and also increases IGF-1 (which is an anabolic growth factor). The insulin that is then produced (with eating) inhibits muscle catabolism, lowers cortisol, increases free testosterone by lowering SHBG and increases IGF-1, which also increases muscle protein synthesis. Eating post-workout also increases androgen receptors (3). By eating a meal post-workout, you increase muscle protein synthesis, inhibit muscle catabolism, provide amino acids for hungry muscles, increase androgen receptors, increase free testosterone, thus enhancing testosterone and DHT uptake by the tissue to exert an anabolic effect.
The problem is that most people have digestive issues and cannot digest and/or utilize all the amino acids from the foods they eat. A great way to bypass this is to use very easily digestible protein such as whey or amino acids. Combine some creatine and gelatin with your amino acids or whey to aid in recovery and boost hypertrophy.
L-carnitine is responsible for transporting long-chain fatty acids into the mitochondria to be used as fuel. The form, L-carnitine-L-tartrate (LCLT), has been found to increase androgen receptors. Androgen receptors were shown to increase by 15% in 3 weeks with LCLT (4).
8) Vitamin D
This is actually a steroid hormone, rather than a vitamin. It increases total testosterone, free testosterone, DHT, lowers estrogen, blocks the aromatase, increases dopamine and inhibits the glucuronidation (deactivation) of androgens from their receptors, thus giving androgens longer binding time to exert a stronger action. More on vitamin D here…
Vitamin D increases the duration that the androgens activate the androgen receptors, by inhibiting glucuronidase.
Drinking coffee promotes mental effectiveness, well-being, increases testosterone, DHT, inhibits the aromatase and increases androgen receptors. More on coffee here…
Forskolin is a natural compound (diterpene) found in the root of the Coleus Forskohlii plant, which is part of the mint family. It’s able to increase total and free testosterone (lower SHBG) as well as increase androgen receptors via the protein kinase A pathway (5), but is also shown to be able to increase the aromatase (6) and prolactin (7) (in vitro evidence only). So maybe it would be best to take with an aromatase inhibitor just to be sure.
Forskolin increases androgen receptors by increasing PKA.
11) Increase Dopamine & lower serotonin
Serotonin is able to increase estrogen, appose dopamine and down-regulate androgen receptors. High serotonin is associated with: anti-social behaviour, depressed well-being, anti-adventure, not focused or goal-orientated, anger/irritability, low energy, struggle to concentrate, OCD, etc… More on lowering serotonin here…
Dopamine is the opposite of serotonin, and it increases testosterone, decreases cortisol, enhances well-being and also up-regulates AR. More on boosting dopamine here…
Zinc lowers the aromatase, is anti-estrogen, lowers SHBG, increases total testosterone, DHT and androgen receptors. Many people consume way too little zinc. You could start with 22mg a day and go up or down from there depending on how you feel. More on zinc here…
Selenium is a trace mineral that is involved in the glutathione redox cycle. It keeps your immunity strong and helps the liver to metabolize and excrete toxins. Selenium and glutathione are both involved in the conversion of thyroid hormone T4 to T3, and T3 increases androgen receptors. Rather rely on selenium from food sources as too much selenium can reduce androgen receptors (15).
Selenium boosts thyroid hormone conversion, which increases androgen receptors.
14) Eat saturated fat & avoid polyunsaturated fats
Polyunsaturated fatty acids (PUFA) potently decreases testosterone, increases aromatase and prolactin as well as inhibits 5-alpha reductase. All polyunsaturated fatty acids must be kept as low as possible, and this includes omega 3. Sea sources, like shrimp and oysters are still ok as the selenium and iodine in the food saturate the PUFAs and protect against its harmful effects. PUFAs also inhibit the binding of androgens to androgen receptors (16).
Saturated fat increase androgen receptors and enhance androgens binding strength, whereas PUFAs decrease androgen receptors and inhibit androgens from binding to their receptors (17).
15) Avoid soy
Soy is rich in isoflavones powerfully decreases testosterone and increases estrogen and it also significantly decreases androgen receptors (8).
Magnesium is a cofactor in over 300 enzymatic reactions and biological processes, including protein and nucleic acid synthesis (androgen receptors are a type of nuclear receptor), neuromuscular excitability, and its receptors are found in every tissue of the body. It increases testosterone, DHT, lowers SHBG, aromatase, and estrogen. It also aids in cellular energy (ATP) production, muscle relaxation, etc…
When a nerve impulse stimulates a muscle, calcium and sodium enter the cells, and magnesium and potassium exit the cells, this results in muscle contraction. So when you have an inadequate amount of magnesium (as well as insufficient thyroid hormones), a muscle cannot fully relax as some of the intracellular calcium remains inside the cell. This constant elevated intra-cellular calcium decreases androgen receptors (10). More on magnesium here…
Magnesium prevents the degeneration of androgen receptors, by reducing intracellular calcium.
Thyroid hormones increase metabolism, testosterone synthesis, 5-alpha reductase, muscle protein synthesis, beard growth, and blood sugar stability. It also up-regulates androgen receptors, and down-regulates estrogen receptors (11). I would try to optimize thyroid function normally before trying thyroid supplement. However, if you feel like you want to try some thyroid, here is TyroMix (3mcg T3 & 6mcg T4 per serving), Tyronene (8mcg T3 per serving) and TyroMax (natural desiccated bovine thyroid)
18) Amino acids: Glycine & Glutamine
Glycine and glutamine are components of ARs. The need for glycine and glutamine increases during periods of metabolic demand, such as with exercise, recovery and stress. The body cannot keep up with the required demand, and by ingesting glycine and glutamine, will spare essential amino acids for muscle protein synthesis and growth, rather than synthesizing glycine and glutamine. More on glycine here…
19) Intermittent Fasting
Fasting short-term (an overnight fast – of a good night’s rest) showed to increase the GnRH-elicited LH response by 67% in the non-obese group, and the corresponding testosterone response by 180%, meaning increased androgen sensitivity (12).
Niacinamide, a form of vitamin B3, powerfully lowers cortisol, decreases estrogen receptors and increases androgen receptor expression through SIRT1 inhibition (13). Start with 100mg a day. It also goes synergistically with gelatin to lower cortisol, estrogen, aromatase, prolactin and increases testosterone and DHT (glycine increase 5-AR). More on niacinamide here…
21) Eat those chilli peppers
Capsaicin, the hot component of chilli peppers, increases androgen receptor expression (14).
22) Win more
Perhaps easier said than done, but winning more increases brain androgen receptors (16). This does not mean to pick more fights, as aggression and fight initiation behaviour is associated with higher estrogen and cortisol, and is not a sign of mature manliness.
23) Tribulus Terrestris
Tribulus Terrestris (TT) is a herb usually used in testosterone boosters, yet are not very effective for that purpose. Instead, it potently increases DHEA, DHT and even dopamine as well as androgen receptors while potently lowering prolactin (19). More on TT here…
- Tribulus Terrestris – 90% saponin, 40% protodioscin
Dihydroepiandrotestsoterone (DHEA), which is a hormone primarily made in the adrenal glands, significantly increases androgen receptors. This is because DHEA converts mainly to DHT (20). More on boosting DHEA here…
- DHEA – take 5mg daily