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Saturday, June 6, 2015

How to Upregulate Beta-Adrenergic Receptors (To improve Energy , Fat Loss etc) (Increasing B3,B2 Receptors)


When it comes to Adrenergic (adrenaline) receptors - alpha is not better. No, Beta is the king of adrenergic biology. And beta activation makes you Alpha. Well, maybe not quite.That.simple. Beta-receptors do however promote fat loss and are crucial for energy production..hence the euphoric Zen of clenbuterol and related agents. Unfortunately, if you use albuterol, clenbuterol, higenamine or any other beta agonist every.single.day.of.the.week - eventually, the receptors will respond to what they perceive as 'Excess Agonism'...the receptors chicken out and shrink (well, downregulate).

Beta receptor downregulation is not a good thing for those who seek energy for their workouts and fat loss. It also can play a role like cavalry attempting to conquer our muscle building goals.

We need to decimate this oppositional strike and upregulate the beta receptors to keep our fitness goals on point!!


In order to upregulate the beta receptors, we need to find out the molecular regulators or really, the promoters of this occurrence

1.) DHEA : As simple as it may sound, DHEA is cited in multiple studies (1) (2) (3) to increase fat loss and upregulate beta-adrenergic 3 densities(4). Beta-3-receptors , if you recall, are very prominent in their fat loss role(5)(6)(7).

So before you discard the other uses of DHEA (including the anti-cortisol effects and glucagon modulating effects) , at least consider it's ultimate betaempowering-empower you potential! !!

If you aren't convinced or aren't a fan of oral DHEA supplements, you can always go with a transdermal version such as RS Transaderm which is currently heading the leap in more bioavailable alternatives. It definitely works quicker from my experience and in itself also contains an anti-estrogen complex and some other neat ingredients which can further spur fat loss.


2.) Increase Testosterone :  How many times do I have to say it ?? Testosterone, this is the hormone you want to keep around in Large Quantities, you want to maximize the level of by any means necessary. Testosterone is shown to amplify the beta receptor induced cyclic AMP accumulation and supports the metabolic rate and central energy production by this mechanism, among others. (8)(9)(10)(11).

Above on link {8} , it is shown that testosterone directly upregulates the beta-receptor density / expression. Using something like PhytoSERMs or something simple like Tongkat Ali could significantly be a game changer in your fat loss or muscle growth routine...testosterone also helps protect the heart (!) (!) and helps to prevent cardiac issues (!) from a multitude of substances as long as it is in the proper ratio with estrogen. (another reason to draw blood and take an anti-estrogen if necessary).

Testosterone also decreases alpha-2-receptors in the brain (mainly frontal cortex) which leads to improved circulation, oxygen delivery and increased memory and motivation(12) (13) (14).


3.) DHT Gel or Products ;)
DHT treatment is shown to reverse both castration caused (15) and GPC deprivation (16) related beta receptor downregulation - and it is one of the best forms of testosterone for improving memory function(17)

In conclusion fellas, neursteroids and prosteroids/precursors are the 'conversion factor' and more for ultimate results, including restoring sensitivity to Clen or other beta agonists. 

Testosterone, DHEA, DHT - these are the keys to keeping your beta receptors on the up and up, literally.

4.) Minimize Estrogen and Progesterone
Estrogen and progesterone can both promote fat retention and can decrease metabolism and specifically make your body retain love-handle and abdominal/trunkal fat, this is confirmed in a multitude of studies but this specific study elucidates estrogen and progesterone's anti-beta-receptor role....



Thus, what should be common sense for experienced fitness enthusiasts may also cause us to ---re-evaluate how much 'extra' modulation is really necessary--- - i.e ketotifen and other anti-histamines.



5.) - Histamine H1R vs Histamine H3R

A final mechanism we may employ are the histamine H3R antagonists; namely Pitolisant, Clobenpropit or alike drugs - they can increase NMDAR function and improve wakefulness and memory, about on par of modafanil, and additionally their effects on cAMP-Ca2+ allow for a potentiation of beta-mediated transmission and recurring increase in synaptogenesis regionalized on / around beta-adrenergic terminals.

http://www.ncbi.nlm.nih.gov/pubmed/9353362

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3111674/

http://www.researchgate.net/publication/20681526_Regulation_of_beta-adrenergic_receptors_and_calcium_channel_agonist_binding_sites_in_cultured_human_embryonal_smooth_muscle_cells

http://www.ncbi.nlm.nih.gov/pubmed/8789956




In Faith & Fitness I pray, Amen. 







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