+ 5 How to Upregulate Beta-Adrenergic Receptors; not another ketotifen dub!
ORIGINAL ARTICLE SITE --> http://www.area1255.blogspot.de/2015/06/how-to-upregulate-beta-adrenergi... <----
~I declare I am the rightful owner and publisher/writer of Area-1255 and this following article~
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. Though some do prefer other forms of transdermals or even making their own! This may be smarter in some ways.
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 Forskolin 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....
http://www.ncbi.nlm.nih.gov/pubmed/11415856
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.
ORIGINAL ARTICLE --> http://www.area1255.blogspot.de/2015/06/how-to-upregulate-beta-adrenergi...
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-adre...
http://www.ncbi.nlm.nih.gov/pubmed/8789956
In Faith & Fitness I pray, Amen.
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Area-1255Bump.
Area-1255If anybody finds any other study relevant to beta-adrenergic sensitivity, let me know!
Area-1255Opioid-receptors seem to play a role as well. Kappa-opioid receptors negatively regulate beta-adrenergic actions and receptors, in the heart and nervous system.
-http://www.ncbi.nlm.nih.gov/pubmed/11134510
-http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3698859/
-http://www.fasebj.org/content/4/11/2881.abstract
Area-1255Thyroid hormone regulation of beta-adrenergic receptor number.
L T Williams, R J Lefkowitz, A M Watanabe, D R Hathaway and H R Besch, Jr
Abstract
The effects of exogenous thyroid hormones (thyroxine and triiodothyronine) on beta-adrenergic receptors in the rat myocardium were investigated. The potent beta-adrenergic antagonist, (-)-[3H]dihydroalprenolol, was used to directly estimate the number and affinity of beta-adrenergic receptors in rat heart membranes from control and hyperthyroid rats. Cardiac membranes from hyperthyroid rats contained 196 +/- 7 fmol of (-)-[3H]dihydroalprenolol binding sites/mg of protein which was significantly (p less than 0.005) greater than the number of binding sites (89 +/- 5 fmol/mg of protein) present in control membranes. The equilibrium dissociation constant (KD) for the interaction of receptors with dihydroalprenolol was the same (2 to 15 nM) in membranes from control and hyperthyroid rats. Similarly, there was no significant difference between the control and hyperthyroid membranes in the affinity of the beta-adrenergic receptor binding sites for the beta-adrenergic agonist isoproterenol. The results of this study demonstrate that thyroid hormones can regulate the number of cardiac beta-adrenergic receptors. The increased numbers of receptors may be responsible, at least in part, for the enhanced catecholamine sensitivity of beta-adrenergic-coupled cardiac responses in the hyperthyroid state.
Hey bro, I just sent you a FR. Please accept. It would be an honor.
Area-1255Done!
Area-1255Zinc (Zn2+) also increases the function of beta-receptors by acting as a ''positive allosteric modulator''.
http://www.ncbi.nlm.nih.gov/pubmed/11752207
Dose at 30-35 mg a day or 50 mg a day.
Fr sent bro...few questions for you
Area-1255Ask away!
interesting article.
Would you recommend keto in conjunction with the above suggestions or ditch the keto completely. I just haven't come across anything as effective as keto. My test is high, my estro low, I am on plenty of DHT compounds. I haven't played around with any histamine compounds or DHEA much. So I am already doing a lot of those things but the only thing that works in a big way for me to upreg the beta receptors is keto or benadryl.
Area-1255You could use Keto - but , it may not be necessary. Zinc as well helps as it acts as a ((PAM)) ; Positive Allosteric Modulator of the beta-adrenergic site...
http://molpharm.aspetjournals.org/content/61/1/65.full
Area-1255Everyone get a chance to read this?