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Thursday, February 26, 2015

Ractopamine - Not just another Beta-Adrenergic agonist; But Rather the "Alpha" of Beta Agonists



This article has been exclusively written for TrueLIFE Research - TeamTLR.com and to foster further progress within research of Ractopamine & other beta-adrenergic based anabolic compounds.



Ractopamine is considered a feed additive to promote leanness in animals raised for their meat. Pharmacologically, it is a beta-adrenergic agonist. It is the active ingredient in products known as Paylean for swine and Optaflexx for cattle, developed by Elanco Animal Health, a division of Eli Lilly and Company, for use in food animals for growth promotion.
Ractopamine use has been banned in most countries, including the European Union, mainland China and Russia[1][2] while 27 other countries, such as Japan, the United States, Canada, and South Korea, have deemed meat from livestock fed ractopamine safe for human consumption.[3]

Commercial ractopamine is a mixture of all four possible stereoisomers.[4]

Beyond that fairly vague introduction, lies a much more interesting story, however. Let's first compare another beta-agonist; clenbuterol, with ractopamine.

Clenbuterol is a similar compound, known collectively as "CLEN" - this compound is used by bodybuilders to cut body fat tremendously , and to gain muscle and vascularity as well(!). Clen has a longer-half-life than ractopamine, but this also increases it's risk for toxicity, and makes alternative use of it trickier(!)

Ractopamine's efficacy of beta-agonism and subsequent effects is quite impressive, and this underlies the reason for its use as opposed to other beta-agonists in livestocks...it has fast uptake into desired tissues, and it's effects are reliable even with consistent dosing(!)

Other beta-agonists can run the risk of intertwining with the final product, despite the controversy surrounding ractopamine - it's less likely to appear in consumed meat than other similar chemicals(!)

In terms of muscle growth, ractopamine shares a very potent anabolic effect with other agonists(!)....before we get into that  - lets first talk about WHY and WHAT.  Backtracking a little.


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RACTOPAMINE ; A BETA-ADRENERGIC AGONIST  
PATHWAY EXPLAINED
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A beta-adrenergic agonist is a substance that binds to and activates the beta-adrenergic (adrenaline) receptor - and thus acts similar to adrenaline but without touching the alpha-receptors(!).....most CLINICAL beta-agonists are even more specific, binding with only the beta-2-receptors - which have dense distribution in skeletal muscles and lung tissues(!).

Clinically, beta-2-agonists have efficacy and reliability in treating asthmatic conditions - and may aid in oxygen delivery both to the lungs and to other muscles lacking it(!) (!).

There are other beta-agonists being studied for obesity and for muscle-wasting disorders(!) (!).

Additionally, natural beta-agonists such as "HIGENAMINE" are often being thrown in to pre-workout supplements and being touted to increase the pump one would get from working out, and aid in cellular energy production as well as increasing protein synthesis in muscles(!).

None of this is wrong, however, there's always a question of HOW MUCH and whether half-lives of natural agonists are clinically relevant and / or sustainable for other conditions.

The pathway of beta-adrenergic receptors can be a little confusing, but basically these receptors are considered "POSITIVELY COUPLED" to "G-proteins" - which means when they are activated, they lead to a positive current exerted from G-proteins - which normally ensures and uses the cyclic Adenosine monophosphate (cAMP) system to activate the corresponding signaling cascade(!).

What this means is , essentially, beta-agonists raise cyclic AMP levels similar to forskolin, which then leads to all of the benefits of the cyclic AMP pathway such as enhanced lipolysis (fat-burning) and increased anabolism (muscle promoting/growth) and a higher metabolism - as well as increased steroidogenesis and testosterone secretion(!) (!).,

Cyclic AMP is considered a second messenger; and it leads to calcium channel activation and activation of PROTEIN KINASE A; which is a superfamily of heavy artillery enzymes involved in modulating and / or activating a variety of other subsequent enzymatical pathways(!).

Additionally, when this pathway is activated (such as with a beta-agonist) - nitric oxide levels also increase, which then leads to vasodilation and enhanced muscle protein synthesis and nutrient delivery / uptake into muscles(!).

Ractopamine has proven very effective in doing all of this(!)(!)....

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Ractopamine is NOT SOLELY a beta-agonist; but also a potent
TAAR1 agonist
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The trace-amine associated receptors ("TAAR")  are targets of amphetamines and other major
drugs, of the stimulant class, and this pathway is vital to their euphoric, energizing and anti-depressant effects ---- TAAR1 is a major signaling pathway, which involves the release and modulation of dopaminergic neuron networks - as well as other central signaling pathways(!).

The activation of TAAR1 gives ractopamine an advantage over other beta-agonists; causing it to be more "broad" and having additional anabolic / lipolytic activities than other beta-agonists....it also would have stronger anti-depressant effects - and thus a propensity to allowing more "mental edge" and stamina than other beta-agonists(!)...


Ractopamine may definitely acrue some other site-specific side-effects due to this property, however, reasonable doses are unlikely to carry significant side-effects - and the benefits may still be obtained by means of proper application, where other chemicals are not in the picture - and thus research can be conducted on only the pharmacological utility of ractopamine without the influence of an array of other compounds with variable half-lives(!) (!).


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CONCLUSIONS 
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Cleaner studies will reveal further use of ractopamine as a novel beta-adrenergic agonist; however they have to take into consideration now, the additional TAAR1 activity - and as such, subsequent studies are needed to define biological applications relating to each pharmacological effect...the properties must be isolated and analyzed as well as compared to other similar agents in order to further understand the use of ractopamine in study and in future subjects where not only livestock is involved.

Clearly, given the controversy, ractopamine has had a bad rap - but the environments and impractical/distorted use paradigms have certainly been responsible for coming concerns (though are legit) - it's a separate perspective that is needed under a more stable and less stressful environment in order to declare the verification of anabolic / lipolytic uses.

However, there is enough evidence as it is to see this agent as a powerful anabolic / lipolytic, but separate backgrounds and different subjects will be needed to properly evaluate side-effect profiles apart from mass-studies done in past times.

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