I didn't realize this stuff has been around for a while. I grabbed this article from MD,
Cimaterol is a relatively unknown beta-adrenergic agonist (β-agonist). However, it shouldn't be. This compound's real name is 2-amino-5-1-hydroxy-2-1-methylethyl-aminoethyl, also known as anthranilonitrile, so, since that is more than a mouthful, we'll simply use the popular name, Cimaterol. This β-agonist is in the family of phenylethanolamines. You may be aware of this class of pharmaceutics through such popular fat loss agents as clenbuterol, or even ephedrine. Enough about the nomenclature and chemical stuff; what's more impressive is how Cimaterol may be the best fat burner currently not being used.
Tender or Tough?
As we age, the efficiency at which our bodies absorb the nutrients from the food we eat wanes. The decline in nutrient absorption is partially predicated on your genetics, gender, health status and the quality of the food you eat. One mechanism of optimizing nutrition status is to attempt to "partition" where the food (nutrients) gets absorbed and stored. For example, diets high in simple sugars will increase the storage of triglycerides (fat), whereas diets higher in protein will enhance the loss of body fat over time.1
Besides altering diet, one can administer metabolic modifiers such as somatotropin (growth hormone), growth hormone releasing factor (GHRF), anabolic steroids (testosterone or its derivatives) and/or beta-adrenergic agonists. Of course, it should not be thought that since any of the aforementioned agents can act as "nutrient partitioners" that they are equivalent. The magnitude and time-course response is different between these metabolic modifiers. The goal in using any of these agents is to increase or enhance amino acid availability. Enhancing protein retention and synthesis translates into new muscle growth. So where does Cimaterol come into play?
In 1993, the Department of Applied Biochemistry at the University of Nottingham, England, started to wonder how Cimaterol might affect meat tenderness. While meat tenderness is important for us when we're eating at The Palm or even at Outback Steakhouse, believe it or not, the way Cimaterol affects the enzymes that dictate meat tenderness (or toughness) is of importance in understanding how this fat burning drug works.2
Within muscle, there are proteolytic (protein breaking) enzymes collectively known as calpains. As with everything in the body, if there's a proteolytic enzyme, that enzyme will have something that will inhibit it; in this case it's calpastatin. In the Nottingham study, it was found that short-term administration of Cimaterol increased calpastatin activity and induced muscle hypertrophy (growth). In other words, one mechanism by which Cimaterol aids in muscle gains is by inhibiting muscle breakdown (acting as an anti-catabolic catalyst). One interesting side note is that when you eat red meat (or pork) that tastes or chews as if it is a tough cut, the animal may have been treated with Cimaterol in order to increase its price on the market. Of note is that when animals were given Cimaterol and a high protein diet consisting of fishmeal or soymeal, those receiving the fish protein achieved muscle weight gains 15 to 20 percent better than those receiving soy.3 Yet another reason not to eat soy!
Medical Wonders of Cimaterol
As unfortunate as it is, when cancer strikes someone we know or love, we immediately get a picture in our mind's eye of that person looking like a bag of bones. In other words, wasted of muscle. In bodybuilding, there is a fear of being in catabolism. That catabolism, while not as extreme as the cachexia (emaciation) of cancer, is a no-no if you want to build or retain any significant muscle. The Department of Surgery at the University of Cincinnati Medical Center, in Ohio, studied whether Cimaterol could aid in reducing the amount of muscle lost in a common model of cancer testing (tumor-bearing animals).4 Furthermore, the doctors wanted to examine if Cimaterol could positively affect protein synthesis (a good thing for those who want bigger muscles). The results strongly indicated that Cimaterol acted as both an anti-catabolic and an anabolic aid. The researchers were so impressed that they concluded Cimaterol and other similar beta-2-agonists might be useful in preventing cancer-induced muscle loss. Imagine what it would do in a healthy weightlifting person.
As bad as cancer may be, I hope none of you ever experiences a serious burn. Burn injuries are characterized by high rates of muscle catabolism, increased energy expenditure, weight loss and massive protein losses. The body fights hard when it suffers burns and the more severe the burn, the harder it is for the body to fight off infections, keep pain in some semblance of control and so much more. In other words, having bodily burns may be the ultimate catabolic condition. (You can't even get out of bed to weight lift or for some, even be conscious). Scientists at the Shriner's Burns Institute tested how Cimaterol infusion (bolus) given twice per day for 14 days would affect muscle catabolism.5 Interestingly enough, only those receiving the Cimaterol gained muscle weight, protein retention and overall body weight. (This, in spite of burns over 30 percent of the body). Yet again, another study demonstrating the anabolic and anti-catabolic properties of Cimaterol.
As Cimaterol is a great anti-catabolic, many wonder how anabolic it is. It should not be overlooked that the more muscle a person has, the greater amount of calories the body burns over a day's time. This being the case it is easy to see how a more muscular person stays leaner easier than a skinny one who does not workout. If your asking how does this tie in to how Cimaterol can be beneficial for bodybuilders, I hope that the following study helps in revealing the facts. Researchers examined the effects of 20-day treatment with Cimaterol on skeletal muscle protein kinetics (6). Over the 20-days, compared to control (no treatment), the group receiving the Cimaterol experienced a significant increase in net amino acid uptake (absorption), which reached a 80% increase rate by the 14th day. Furthermore, when compared to basal (starting) amino acid uptake levels, those treated with Cimaterol experienced a whopping 260% increase. To assess the anabolic properties of Cimaterol, the researchers examined the weight and muscle mass of those receiving the drug compared to those in the control group. In all, the average muscle weight gain over the 20-days was 10%. A 10% muscle size and weight gain is very impressive; picture yourself with 10% more muscle, would you be strikingly bigger than you are now?
So, is This Stuff Available?
The answer is a resounding yes! Yes, it is available; the question remains, is it legal in the United States? From what I can tell, the answer is no, it is not legal in the U.S. However, within the agriculture world, simple legalities have not stopped it from being imported from the United Kingdom. In fact, even American companies such as American Cyanamid have it, but, last I could tell, it's only available for "research purposes." Of course, it could probably be purified for home use by those in the know, but that is for another time.
The version American Cyanamid sells is a 20 percent Cimaterol solution, whereas Tocris, a UK company, retails it in 10-milligram and 50-milligram unit sizes. It's important to understand what a possible human dose might be. The LD50 dose is an average of 1,859 milligrams per kilogram of body weight for both sexes of the rat. The LD50 is the 50 percent dose that is lethal. The animal data translates into an approximate human dose of 20 milligrams and the cost is less than $1 per day.
Keep in mind that Cimaterol has not yet been tested in humans, nor is the approximate dose confirmed. If you do decide to use Cimaterol as an anabolic and fat loss agent and you compete in a drug-tested event, the Ridascreen® drug screen test can detect its presence. (It's the same test that's used for clenbuterol).7 Of course, the drug-screening test is only of concern for those who get drug tested.
To Recap:
- Cimaterol is a more powerful beta-agonist than clenbuterol.
- Cimaterol promotes protein retention and accretion.
- Cimaterol plus a high-protein diet equals more muscle growth than Cimaterol or a high protein diet alone.
- Cimaterol is a very powerful anti-catabolic, even in the face of cancer or burns.
- Daily cimaterol use can promote very visible muscle growth within a very short 20-day period.
- As of right now, Cimaterol is available for animal research and in research grade class only.
- Before long, Cimaterol should be available for human use and on the market.
Doug Kalman is a Director at Miami Research Associates (MRA), an independent research organization specializing in Phase II through Post-Market Clinical Trials for the pharmaceutical and nutraceutical industries.
