Prototype Nutrition Ketoforce



Breaking new research on ursolic acid shows increases in brown fat production and confirms muscle building potential

By Patrick Arnold

The most interesting health and fitness related natural compound to come around within the last decade or so has got to be ursolic acid. I have been aware of its benefits for quite some time but it wasn’t until last year that I really became excited. It was then that a landmark study was released by some University of Iowa researchers showing that ursolic acid blocked the muscle wasting effects of nerve injury and starvation, as well as increased muscle mass in healthy animals while simultaneously reducing body fat stores. I reviewed this study in a previous blog entry in case you want to refer back to it

It’s been over a year since then and another study on ursolic acid has been released by these same researchers The data confirm some of the original findings as well as shed more light on how ursolic acid works in the body to build muscle and burn fat. In contrast to the first study, where normal mice were used, this study used mice fed a high fat diet. This mouse model is used to induce obesity. Since obesity is an enormous health concern in our society, any drug or natural substance that can help treat the causes or effects of obesity would be of tremendous value. In other words, researchers aren’t so interested in developing stuff for athletes and healthy people because that’s not where the bucks are at. Still, studies that utilize the mouse obesity model can be of interest and have applicability to non-obese active folks as well.

To gauge the effects of ursolic acid, the mice were split up into groups. One group just ate the high fat diet alone while the other groups ate the high fat diet supplemented with 0.14 or 0.27 percent ursolic acid. They then examined the rats after 6 weeks. Here are some of the interesting things that they saw

Muscle and Exercise

Ursolic acid increased the size of both slow and fast twitch muscle fibers. This was associated with increased Akt signalling (Akt has vital roles in biological processes such as protein synthesis and glucose uptake and metabolism). These rats had greater grip strength than control rats and could run significantly farther on a treadmill. They had slightly lower resting heart rate than controls while demonstrating no differences in blood pressure. Another interesting find is that a substance called vascular endothelial growth factor – A was substantially more active in the ursolic mice, indicating that new blood vessels were being formed to feed the growing muscle tissue.

Bodyfat and Glucose Tolerance

The mice fed the high fat diet supplemented with ursolic acid gained less weight then the control rats and had substantially less stored body fat. Their fasting blood glucose stayed normal compared to the control mice (average 74 mg/dl versus average 109 mg/dl), and their blood glucose levels after a glucose challenge also was substantially lower.

Brown Fat and Energy Expenditure
There are two types of body fat – brown fat and white fat. White fat is more or less metabolically inactive, and its purpose is mostly to store calories. Brown fat on the other hand is full of an enzyme called UCP-1 which stimulates thermogenesis (this is the same enzyme turned on by DNP). Brown fat is rich in blood supply and essentially burns calories and keeps you warm. The researchers found that the ursolic supplement mice had a lot more brown fat, and not surprisingly they were much more resistant to the cold then the control rats.

The ursolic supplemented mice had higher levels of energy expenditure. Even though they ate more food than the control mice, the ursolic mice weighed less – with the difference in weight made up in body fat. This was not an acute effect however and was only seen after chronic administration of ursolic acid. This is entirely consistent with the fact that it required time for the growth of muscle and brown fat to burn the extra calories, and was not due to some immediate stimulant effect.

Ursolic Acid Supplementation

This latest study just adds to the impressive evidence behind the amazing bodybuilding and overall health potential of ursolic acid. Ursolic acid as a supplement has become more and more popular over the last year or so since the evidence first started pouring in on the stuff. It is usually sold in the form of an extract from herbs such as rosemary or loquat leaf. This form has proven to be less than stellar however in the feedback users have been giving. Results have been hit or miss for the most part.

I noticed this high variability in results and less than anticipated feedback early on, and I was quite certain it was due to the terrible solubility of the compound. It basically repels water and is very insoluble in the sort of solvent systems that are similar to the properties of the lining of your gastrointestinal system. If you couple that with the likelihood it is metabolized extensively upon liver first pass, you end up with very poor bioavailabilty. In fact, research suggests that less than one percent of orally ingested ursolic acid actually gets into your system.

I solved this problem however. For the past several months I have synthesized and played with derivatives of ursolic acid that have solubility and dispersability properties magnitudes better than straight ursolic acid. I have found that delivering these derivatives (which simple break down quickly in the body to ursolic acid after being absorbed) via a topical formulation leads to the sort of body fat loss and muscle mass increases in human subjects that we would expect to see from the published mice studies.

The compound I have settled on as the best has absolutely amazing solubility compared to straight ursolic acid. It is called Arginine Ursolic Acetate and this is its chemical structure.

In the body this compound breaks down rapidly to acetic acid (a dietary fatty acid), l-arginine (a dietary amino acid), and ursolic acid. Although I have never (yet) measured blood levels of ursolic acid to prove that this method delivers the compound way better than regular extract capsules, the fact that almost everyone that has tried when formulated topically gets amazing results sort of speaks for itself.

So there you go. If you weren’t excited about ursolic acid before then you should be now. And if you want to try the patent pending form that I worked my butt off to perfect then you can by clicking here



The New Steroid Legislation as seen by Rick Collins, JD, CSCS

By Patrick Arnold

The New Designer Steroid Bill and YOU:

Questions and Answers with Rick Collins

Q: What is the “Designer Anabolic Steroid Control Act of 2012”?

A: It’s a Senate Bill (SB 3431) introduced by Senators Orrin Hatch (R-Utah) and Sheldon Whitehouse (D-R.I.) and referred to the Judiciary Committee. If passed by Congress, it will amend the Controlled Substances Act to more aggressively regulate steroidal substances being sold as dietary supplement ingredients. The clear intent is to remove remaining “prohormone” products from the market and prevent new ones from being introduced. The bill would take such past or present supplement products as ATD, 6-oxo, 6-bromo, Furazadrol, Halodrol, Havoc, and Tren and legally classify them as anabolic steroids and Controlled Substances. Here’s what Sen. Whitehouse said in introducing the bill on July 25th, 2012:

“… I am pleased to join Senator Hatch in introducing the bipartisan Designer Anabolic Steroid Control Act of 2012. This measure will help keep American children and families safe from dangerous designer drugs that masquerade as healthy dietary supplements. This legislation is based on Senator Specter’s work in the previous Congress, and I thank him for his leadership on this issue.

Doctors and scientists have long recognized the health hazards of non-medical use of anabolic steroids. For that reason, Congress has previously acted to ensure that these drugs are listed as controlled substances. Nonetheless, according to investigative reporting and Congressional testimony, a loophole in current law allows for designer anabolic steroids to easily be found on the Internet, in gyms, and even in retail stores.

Designer steroids are produced by reverse engineering existing illegal steroids and then slightly modifying the chemical composition, so that the resulting product is not on the Drug Enforcement Administration’s, DEA, list of controlled substances. When taken by consumers, designer steroids can cause serious medical consequences, including liver injury and increased risk of heart attack and stroke. They may also lead to psychological effects such as aggression, hostility, and addiction.

These designer products can be even more dangerous than traditional steroids because they are often untested, produced from overseas raw materials, and manufactured without quality controls. As one witness testified at a Crime Subcommittee hearing in the last Congress, ‘all it takes to cash in on the storefront steroid craze is a credit card to import raw products from China or India where most of the raw ingredients come from, the ability to pour powders into a bottle or pill and a printer to create shiny, glossy labels.’

The unscrupulous actors responsible for manufacturing and selling these products often market them with misleading and inaccurate labels. That can cause consumers who are looking for a healthy supplement–not just elite athletes, but also high school students, law enforcement personnel, and mainstream Americans–to be deceived into taking these dangerous products.

Loopholes in existing law allow these dangerous designer steroids to evade regulation. Under current law, in order to classify new substances as steroids, the DEA must complete a burdensome and time-consuming series of chemical and pharmacological testing. As a DEA official testified before Congress: ‘in the time that it takes DEA to administratively schedule an anabolic steroid used in a dietary supplement product, several new products can enter the market to take the place of those products.’’

The Designer Anabolic Steroid Control Act of 2012 would quickly protect consumers from these dangerous products. First, it would immediately place 27 known designer anabolic steroids on the list of controlled substances. Second, it would grant the DEA authority to temporarily schedule new designer steroids on the controlled substances list, so that if bad actors develop new variations, these products can be removed from the market. Third, it would create new penalties for importing, manufacturing, or distributing anabolic steroid’s [sic] under false labels.

Senator Hatch and I have worked closely with a range of consumer and industry organizations to ensure that this legislation would not interfere with consumers’ access to legitimate dietary supplements. I am pleased that the measure has been endorsed by the United States Anti-Doping Agency, the Alliance for Natural Health, the Council for Responsible Nutrition, the American Herbal Products Association, the Natural Products Association, the Consumer Health Products Association, and the United Natural Products Alliance.

I thank these organizations for their support, and look forward to working with them, with Senator Hatch, and with colleagues from both sides of the aisle to enact this common sense measure into law.”

Q: Is the bill specific in naming the substances to be added to the list of anabolic steroids?

A: The “Discussion Draft” of the bill that I reviewed would specifically add 27 chemical compounds to the list of substances defined as anabolic steroids in Title 21 of the U.S. Code [21 USC 802(41)]. The bill presents the chemical nomenclature for these substances. Some of the chemical names listed, according to steroidal supplement guru Patrick Arnold, contain errors or refer to compounds that may actually not exist. But any minor mistakes aside, it seems that the drafters of the bill extensively canvassed the supplement market and perhaps even the Internet message boards in an effort to identify and specifically name as many compounds as possible. This isn’t the first time that Congress has expanded the list of anabolic steroids. The original list, compiled in 1990, was amended in 2004 to include androstenedione and a variety of other steroidal products. The DEA later issued a Final Rule (, effective January 2010, classifying three more compounds as anabolic steroids (boldione, desoxymethyltestosterone, and 19-nor-4,9(10)-androstadienedione, along with their salts, esters and ethers). Then the DEA last year published a notice of proposed rulemaking to add yet two more steroidal compounds, prostanozol and methasterone (marketed as Superdrol), along with their salts, esters and ethers, to the list. The Final Rule on these two was issued on July 30th, 2012 (, effective August 29th, 2012. This new bill just follows up by adding a whole bunch more (although now a moot point, it includes the recently scheduled prostanozol and Superdrol) … and by design, misses very few.

Q: What about steroidal substances that are not on the list?

A: The bill changes the way unlisted steroidal compounds are dealt with. It says that “a drug or hormonal substance (other than estrogens, progestins, corticosteroids, and dehydroepiandrosterone) that is not listed … and is derived from, or has a chemical structure substantially similar to, 1 or more [listed] anabolic steroids [is considered an anabolic steroid] if … [it] has been created or manufactured with the intent of [promoting muscle growth or having pharmacological effects like testosterone or] has been, or is intended to be, marketed or otherwise promoted [to suggest it will promote muscle growth or have pharmacological effects like testosterone]. Notice that there’s no proof requirement that the substance actually promote muscle growth or act like testosterone pharmacologically – only that it’s created, manufactured, marketed or promoted with the intent of doing so. So, for supplement industry purposes, a company that markets any product that is derived from or has substantial chemical similarity to a listed anabolic steroid and is also created or marketed to build muscle or have a pharmacological effect like testosterone is marketing an anabolic steroid. An interesting question arises in the following theoretical scenario: Company A markets an ingredient derived from a listed anabolic steroid for health and wellness purposes, and the ingredient has neither anabolic nor androgenic effects. Company B markets the same ingredient but makes the claim, falsely, that the ingredient builds muscle. If Company B is prosecuted and convicted for marketing the ingredient as an anabolic steroid, where does this leave Company A? While it would seem reasonable that the ingredient is an anabolic steroid only with respect to Company B, the issue is not addressed in the language of the bill.

Q: Are there any exemptions provided in the bill?

A: Yes. Unlisted steroidal compounds that are herbs or botanicals are exempted. So are concentrates, metabolites, and extracts of an herb or botanical, or a constituent isolated directly from an herb or botanical. This provision was drafted as an acknowledgement to the current position of the Food and Drug Administration (FDA) articulated with respect to New Dietary Ingredients (NDI’s): that a compound is a “constituent” of a botanical only if it is isolated directly from it, and not if it is instead synthetically created in a lab. The bill further connects the Controlled Substances Act with the Dietary Supplement Health and Education Act (“DSHEA,” a part of the Food, Drug, and Cosmetic Act) by requiring that any exempted substance must be a “dietary ingredient” under DSHEA. And the bill puts the burden of DSHEA compliance on the marketer, by providing that anyone “claiming the benefit of an exemption [has] the burden of going forward with the evidence.” In other words, somebody arrested for selling an anabolic steroid whose defense is that it is an exempted constituent would have the burden of showing evidence of DSHEA compliance.

Q: Does the bill make it easier to add new unlisted substances to the list?

A: It does, by amending a different section of Title 21 [21 USC 811] to provide a fast-track for scheduling. The Attorney General may issue a temporary order, to take effect 30 days after publication, adding a substance to the list if it meets certain criteria. The temporary order “is not subject to judicial review” and a permanent order could be simultaneously sought. But the bill also provides that an unlisted steroidal substance can be considered an anabolic steroid if it’s determined to meet the criteria of an anabolic steroid “in any criminal, civil, or administrative proceeding arising under this Act.” So, while the Attorney General has the power to declare substances to be anabolic steroids through the rulemaking process, unlisted substances can nevertheless be considered to be anabolic steroids without prior rulemaking notice if it’s proven in a court of law, such as during a criminal prosecution of a supplement company or its principals. But the bill also makes it easier for the Attorney General to add new compounds because it changes the criteria and tosses out the rigorous scientific inquiry currently required.

Q: How would the criteria for administrative action change under the proposed new law?

A: Under current requirements, the DEA has to extensively examine peer-reviewed published literature and sometimes even undertake its own pharmacological assay studies to determine if a compound has androgenic and anabolic activity similar to testosterone. This can be a huge, lengthy, complicated endeavor, and the DEA has been far from wild about it. For example, back in September 2009, Joseph Rannazzisi, Deputy Assistant Administrator at DEA’s Office of Diversion Control, testified before the Crime Subcommittee at the hearing (“Body Building Products and Hidden Steroids: Enforcement Barriers”) referenced this month by Sen. Whitehouse in introducing the bill. Mr. Rannazzisi expressed the hurdles imposed by the current law, citing as an example the difficult process of scheduling boldione, desoxymethyltestosterone, and 19-nor-4,9(10)-androstadienedione which was, at that time, in its final stages. He also testified that a review of three (3) additional compounds – methyldrostanolone (methasterone), prostanozol, and adrenosterone (misspelled adrenostreone in his written statement) – had begun. But although three compounds were reviewed, only two were scheduled. Neither the notice of proposed rulemaking in November 2011 nor the Final Rule issued in July 2012 referenced adrenosterone, a compound sold under the name “11-oxo.” Were there problems proving some aspect of the requirements? We don’t know, and the implications from this are open to debate (note also that the substance is also not listed among the specific compounds in the new bill). In any event, under the new definition of an anabolic steroid, the process for scheduling is much easier. If the compound is derived from, or has a chemical structure substantially similar to a listed anabolic steroids, and it’s not an estrogen, progestin, corticosteroid or DHEA, then it’s considered an anabolic steroid merely if it’s been created or manufactured with the intent of being anabolic or androgenic or if it’s marketed or promoted to suggest that it’s anabolic or androgenic. The new definition offers an enormous reduction in the DEA’s burden to schedule a new steroid.

Q: Weren’t many of these supplement products already illegal under the Food, Drug, and Cosmetic Act?

A: Yes. Many of these substances were synthetically created compounds and did not meet the criteria to be sold as dietary supplements under DSHEA. Since they were not DSHEA compliant, they were unapproved and mislabeled “drugs” and the FDA had the authority to investigate and bring charges for federal prosecution. Until recently, however, many in the supplement industry didn’t understand the criminal penalties for non-DSHEA compliance, or didn’t take the threat seriously. But that has changed since a number of sports nutrition companies were prosecuted for selling prohormone products in the wake of the execution of a search warrant on a distributor’s Boise, Idaho facility back in 2009. Some of the same substances now being added to the list of anabolic steroids under the Controlled Substances Act were already declared illegal drugs under the Food, Drug, and Cosmetic Act (FD&CA) … and the companies selling them were prosecuted federally and convicted. The new bill, however, gives the DEA – often viewed as more aggressive at enforcement than the FDA – the authority to take action. Also, by classifying these substances under the Controlled Substances Act, the new bill escalates the severity of potential punishments.

Q: What does the bill say about sentences for steroid crimes?

A: The bill directs the United States Sentencing Commission to “review and amend the Federal sentencing guidelines.” The last time Congress directed this, the Commission brought the hammer down and greatly escalated the punishments for steroid trafficking crimes by re-calculating the way steroids were quantified. As of 2006, injectable and oral steroids became quantified for punishment in a 1:1 ratio to other Schedule III drugs, resulting in a twenty-fold measurement increase for injectable steroid units and a whopping fifty-fold increase for oral steroid units. One “unit” of an oral steroid became one pill, tablet or capsule rather than fifty; one unit of a liquid steroid was reduced to .5ml rather than 10ml, and steroids in other forms (“e.g., patch, topical cream, aerosol”) were to be reasonably estimated based on a consideration of 25mg as one unit. We don’t know exactly what the Commission will do if this new bill passes, but the bill specifically directs that for steroid products where dosage cannot be readily ascertained, such as powders or topical creams, that “the sentence shall be determined based on the entire weight of the mixture or substance.” So, a person trafficking a kilogram of pure testosterone powder would be at the same federal sentencing level as the person who was selling a product that contained a small or even trace amount of testosterone.

Q: What does the bill say about the way products are labeled?

A: The bill introduces a whole new theory by which to prosecute these cases by making it a crime to import, export, manufacture, distribute, dispense, sell, offer to sell, or possess with intent to manufacture or sell any anabolic steroid, or any product containing an anabolic steroid, unless it bears a label clearly identifying the anabolic steroid by accepted (IUPAC) nomenclature. This provision would apply to manufacturers who use deceptive or “creative” ingredient labeling to conceal that the product is an anabolic steroid. It would also apply to distributors and retailers who know, intend, or have reasonable cause to believe that the product contains an anabolic steroid. Criminal penalties can be up to 10 years imprisonment and massive fines (up to $2.5 million on corporations). Civil penalties can be up to $500,000 per product violation for importers, exporters, manufacturers and distributors. Even retailers can be hit with a $25,000 penalty per product violation (and each package size, form, or differently labeled item is a separate product).

Q: What impact would this bill have on consumers?

A: The bill would have a huge impact on consumers. While marketing prohormones that are currently illegal under DSHEA and the FD&CA subject the marketers to criminal sanctions, consumers don’t face charges. Simple possession itself is not illegal. All that changes when a compound becomes classified as a controlled substance. By reclassifying these compounds into controlled substances, this bill criminalizes the consumers as well as the marketers (the DEA’s Final Rule on prostanozol and Superdrol, once effective, will do this on those two compounds). Being in simple possession of a compound that is a controlled substance is a federal crime – a federal misdemeanor that carries with it up to a year of incarceration. But it likely won’t stop there. If the bill passes, it’s quite probable that individual states will view what Congress did as an important step in protecting the public, especially children, and will seek to amend their own laws to be consistent with the new federal law. In some states, though, simple possession of an anabolic steroid is a felony, not a misdemeanor, and in those states the simple possession of any of these compounds would be a felony. If states follow suit, a person caught during a car stop with a single capsule of 6-bromo, for example, would be charged with either a misdemeanor or a felony (depending on his or her state’s law). An old bottle of Superdrol sitting in a gym bag would be like illegally having a bottle of Vicodin.

Q: Do you think this bill will achieve the intended purposes of Congress?

A: Unlike the poorly conceived and drafted 2004 amendment to the Anabolic Steroid Control Act, this bill shows an investment of considerable effort and thought. It’s clear that the intent behind it is to eradicate steroidal ingredients from the retail supplement market. This bill has the potential to accomplish that. It even requires the Administrator of the DEA to keep Congress in the loop by reporting to them every 2 years on what new steroids have been scheduled. Of course, the bigger picture is unclear. Will consumer demand for steroidal substances that may build muscle disappear? Or will the reclassification of these items and their removal from the dietary supplement market lead to the creation of a black market for them … or to an increased demand for the traditional pharmaceutical anabolic steroids already on the black market? The realities of demand and supply and our experience with alcohol Prohibition would suggest that legislative efforts like this one don’t entirely eliminate problems but instead may push them underground. Time will tell.

Q: What do you predict for this bill?

A: Senator Hatch is viewed as a stalwart advocate for dietary supplements. So, when he sponsors legislation to restrict the industry, many in Congress will see it as something that sorely needs to be done. The bill has received the overwhelming support of the large industry trade groups and there is no organized opposition. Unless there’s some unexpected curveball tossed out, or Earth is hit by an asteroid, there’s a high likelihood the bill will pass. For future updates and analysis, visit and or follow me on Twitter (@RickCollinsEsq) and at

Rick Collins, JD, CSCS [] is the lawyer that members of the bodybuilding community and nutritional supplement industry turn to when they need legal help or representation. He and his firm represent dietary supplement companies nationwide, and he has personally defended steroid criminal charges from coast to coast. He can be reached at 516-294-0300. [© Rick Collins, 2012. All rights reserved. For informational purposes only, not to be construed as legal or medical advice.]

2012 Designer Anabolic Steroid Control Act



Two Inadvertant Drug Positives. Two Different Outcomes.

By Patrick Arnold

Zach Lund

In January of 2006 United States Skeleton competitor Zach Lund was at the peak of his career. He was ranked number one in the world and was the obvious favorite to win the gold medal at the olympic games the next month in Turin, Italy. Unfortunately, it was at this time that he received devastating news. He had tested positive for a banned substance.

The banned substance was finasteride. Finasteride is the active substance in the drug Propecia, which is commonly used to combat male pattern baldness. Lund was predisposed to male pattern baldness and had been using Propecia for seven years in an effort to delay the loss of his youthful head of hair for as long as possible. When he received the bad news he was confused – he didn’t know what finasteride was. When he figured out that it was the active ingredient in his balding medication he was even more perplexed, yet he surely figured that this misunderstanding could be easily resolved.

Only very recently had the world anti-doping agency (WADA) added finasteride to their list of banned substances. The reason was not because finasteride offered any performance enhancing benefits, but because its use threw a wrench in the testing methods that the doping chemists used to detect various anabolic steroids. Finasteride blocks an enzyme called 5-alpha reductase which is involved in the metabolism of a variety of steroids. Because of this, the use of finasteride could muddy up the detection of certain steroids and potentially result in a steroid positive urine sample being misidentified as steroid negative. So by adding finasteride to the list of prohibited substances as a “masking agent”, WADA could conveniently solve this dilemma.

Unfortunately, finasteride – as the active ingredient in propecia – had for years been a commonly used medicine by men like Lund who were concerned about hair loss. Guys like Lund don’t know what finasteride is, nor do they have the ability to comb through every update of the banned substances list to match esoteric chemical names to things that might be in their bathroom cabinet. And it’s not like WADA made any effort to make sure athletes were aware of this new addition to the list – as far as they were concerned that’s the athletes problem, not theirs.

WADA demanded a two year suspension for Lund’s finasteride positive. Even though Lund was not aware that finasteride had been added to the list he still had been reporting for several years to the United States Bobsled and Skeleton Federation all the drugs he was taking, including Propecia. Obviously if Lund’s intention was to take steroids and evade detection he would not have been so open about his use of the balding medication.

After some wrangling with USADA, WADA, and the court of arbitration Lund was able to get his punishment reduced to a one year suspension. Still, Lund missed out on his opportunity to take home olympic gold.

Lund never regained is prominence in the sport of skeleton after his doping drama. Although he competed in the 2010 winter olympics in Vancouver he failed to win a medal. And finally, in a cruel twist of irony, in 2009 WADA removed finasteride from the list of prohibited substances.

Hope Solo

Hope Solo is the goaltender for the United States women’s soccer team. The U.S. team has achieved enormous publicity in recent years with their gold medal victory in the 2008 Beijing Olympics and their heartbreaking shootout loss to the Japan team in the finals of the FIFA World Cup in 2011. Girl’s Soccer in the U.S. is huge, and as the most recognized member of Team USA Solo has a huge fan base – especially among young athletic females who look up to her adoringly as a role model. It’s no shocker that sponsors have taken notice of this, and many millions of dollars of advertising money have been made off of the women soccer team phenomenon – with Solo at the center of it all.

So it had to be a moment of panic for all concerned on June 15th when it was discovered that Solo had tested positive for a banned substance – the diuretic Canrenone.

Diuretics are banned for two reasons. First and foremost, they can be used to dilute urine and therefore mask the presence of other controlled substances. Secondly, they can be used to quickly lose weight which can be an advantage in sports where “making weight” is an issue, or in sports where being light and agile are an advantage. [soccer goaltender??]

Like Lund, Solo claimed that the drug was in her system as the result of a medication she was taking. In this case it was a medicine to help alleviate the discomforts associated with pre-menstrual syndrome. The situation with Solo however developed quite differently than the situation with Lund did. After cooperating with USADA, it was agreed that Solo had made an “honest mistake”, and she received a simple public warning. She was allowed to continue to participate in soccer matches, and most importantly she will be able to goaltend for Team USA at the London Olympics.

Gatorade won’t have to worry about blowing their multi-million dollar deal with Solo and there won’t be disillusioned little girls sadly removing Hope Solo posters from their bedroom walls. All remains well in the land of the free.



Is Resveratrol a Performance Enhancing Drug?

By Patrick Arnold

Competitive sports organizations often have policies that ban the use of substances that enhance performance.  Substances include such well known things as steroids and stimulants, but they also include more esoteric ones such as blood boosters and agents that enhance metabolic efficiency.  The granddaddy of doping policing bodies is the World Anti-Doping Agency (WADA) and they have been known to throw just about anything on their list of prohibited substances.  It doesn’t have to be a synthetic drug, or even unhealthy – it just has to have the ability (in their interpretation) to offer an unfair advantage .  All of this makes me wonder whether newly published information regarding an extremely popular natural anti-aging supplement might not result in it being added to the next update of WADA list of prohibited substances.  Furthermore, if it is not added to the list, I would be curious as to why it was not.

The supplement I am referring to is of course resveratrol (it’s in the title – duh).   For those of you unfamiliar with resveratrol it is a compound found in many natural plants.  It is particularly well known for being present in red wine, and as a consequence many of the purported health benefits of red wine have been attributed to resveratrol.  Resveratrol gained particular notoriety due to work by a Harvard University researcher named Dr. David Sinclair in the 2000s.  Sinclair was the first to demonstrate life extension benefits of resveratrol, and he also authored a highly publicized paper showing resveratrol dramatically preventing the harmful effects of a high fat diet on the health of mice.  As a result of all this, resveratrol sales skyrocketed and it is perhaps the top selling anti-aging supplement ingredient on the market today.

Although there have been some studies with data hinting at the exercise benefits of resveratrol, nobody had done a study specifically designed to explore that in depth – until now.   Researchers from University of Alberta explored what effects resveratrol might have on exercise performance in rats.  The study was just recently published in Journal of Physiology.  In the study they subjected rats to training on a treadmill five days a week for 12 weeks.  They used air puffs and electric shock to prod the rats to run and the training was made progressively more difficult over time.  The rats ran essentially to exhaustion (where they couldn’t be prodded anymore).

These exercising rats were divided into two groups.  The first group received resveratrol in their chow (4g per Kg chow) and the second group just ate a control chow.  The resveratrol group experienced a striking 21% increase in exercise performance versus the control group.  The force generation in the slow twitch soleus muscle was also enhanced significantly over control.  Fatty acid metabolism by muscle was enhanced in the resveratrol group versus control as well.  Finally, the efficiency and structural integrity of the heart muscle was improved more so in the resveratrol group.

So it appears that resveratrol at high enough doses can be an effective enhancer of performance (at least as it concerns endurance exercise) and it appears to do this in large part by supporting the efficient utilization of fatty acids for fuel.   Resveratrol has a low oral bioavailbility and extrapolating off the top of my head I would think that a human would need at least 2 grams a day of the compound to come close to matching any of these results.  A topical formulation may be a good alternative to oral resveratrol due to its ability to avoid first pass liver metabolism as well as providing a sustained release effect ( a great topical resveratrol is Prototypes R-Spray

Now back to my original question.  Will this be put on a list of prohibited substances?  People ingest very small amounts of resveratrol in foods every day, however the amounts that were used in this study were orders of magnitude higher.  Might WADA make a rule saying that levels of resveratrol in the urine over a certain low concentration are a violation?  I can’t really think of anything stopping them.  There is certainly no love lost between WADA and the supplement industry.  It will be interesting to see what happens



To Graze or to Gorge??

By Patrick Arnold

Current opinion amongst diet experts regarding frequency of meals tells us that it is healthier to eat fewer small meals a day than one large meal.  It is thought that this leads to more stable blood sugar and lower insulin levels – which leads to less fat gain and the subsequent metabolic consequences thereof, such as high blood pressure and inflammatory related dysfunctions.  This practice of many small frequent meals throughout the day is referred to as “grazing”.

Two apparently unrelated studies were recently released however which seem to fly directly in the face of the grazing philosophy.  The studies used mice and they compared the metabolic effects of a grazing type diet (referred to as ad libitum feeding in science) to a diet where the mice only were allowed to eat during a limited period of the day (referred to as time restricted feeding).

The first study was performed at the University of California, San Diego, La Jolla.  In this study groups of mice were fed either a high fat diet or normal fat diet, with one group eating ad libitum (AL) and the second group practicing time restricted feeding (TR) where they could only eat during 8 hours of the day.  Despite the fact that the animals ate the same amount of food, the TR group eating both the high fat and normal fat diets showed greater energy expenditure than the corresponding AL groups.  The TR group eating the high fat diet seemed to be protected from the adverse effects of that sort of diet such as body fat gain, hyperinsulinemia, and liver dysfunction.  They also showed improved coordination compared to the AL group on the high fat diet.

The second study was done at the Hebrew University of Jersusalem.  The researchers looked at mice over 18 weeks while being fed a high fat diet.  One group was fed AL while the other was fed TR (this time the restriction was for four hours during the day).  There was also a third group that was fed a low fat diet AL.  All groups consumed the same amount of calories.  Compared to the AL low fat group the TR high fat group weighed 12 percent less, had 21 percent lower cholesterol, and had 1.4 times greater insulin sensitivity.  The comparison to the AL high fat group was even more startling, with 18 percent less bodyweight, 30 percent less cholesterol, and a 3.7 times greater insulin sensitivity.  In addition to this, plasma ghrelin (a hunger hormone) was 25% lower in the high fat TR group and plasma corticosterone (the mouse equivalent to the stress hormone cortisol) was 53% lower.

What does this all mean?  This all has to do with circadian rhythms and the apparently important role it has in determining how animals utilize dietary energy.  It’s a pretty complicated subject and has to do with things called clock genes and with all sorts of hormones related to the light/dark cycle.  It’s known that mice and most lower animals are very influenced by circadian rhythms and these studies indicate that circadian rhythms and the timing of dietary intake have a pretty profound connection.  However, we don’t know how this applies to humans.  Yes, humans have circadian rhythms too but we probably are not influenced by them to the extent that a lot of other species are.  In other words, this experiment may not work the same in humans at all.  On the other hand, it might.  My only concern is that most people I know would be so hungry by feeding time they will end up gorging and eating twice as much as they would if they had grazed throughout the day.  Whatever the case, it would be interesting to find out.



SERMs as an alternative to testosterone replacement therapy

By Patrick Arnold

SERM stands for selective estrogen receptor modulator.  Also known as estrogen receptor agonist/ antagonists (or anti-estrogens), these drugs are used by bodybuilders to block the estrogenic effects of anabolic steroids and/or to help stimulate the production of natural testosterone after a steroid cycle.  Examples of SERMs are tamoxifen (Nolvadex), clomiphene (Clomid), and raloxifene (Evista).

These drugs work at the estrogen receptor  to block the effects of estrogen in certain areas of the body (such as the central nervous system and breast)  while in other parts of the body (bone, liver) they act as active estrogens.  Their antagonist properties at the breast make them useful in avoiding or treating anabolic steroid induced gynecomastia, while at the hypothalamus/pituitary the anti-estrogen action helps to block the suppressive effect of estrogens upon luteinizing hormone production (and hence testosterone production).

Lately, some people have explored using SERMs as an alternative to testosterone replacement therapy.  Indeed they do work to stimulate testosterone production in most males and they can restore healthy levels to guys who have lower than normal testosterone blood readings.  The question is however, are you getting the full biological effect of testosterone when you are taking a SERM?

This is an interesting question since it has been observed by many SERM users that the subjective physical response one gets from a SERM often does not correlate with the measured substantial increase in circulating testosterone.  In other words, you don’t feel the same when your blood testosterone is doubled by taking a SERM as compared to when it is doubled by a testosterone injection or testosterone gel.  Why is that?

There are some theories.  Number one, SERMs may act as estrogen antagonists in the brain and it is well known that many of the effects of testosterone upon libido and mood are due to its local conversion to DHT as well as estrogen (estradiol) in the CNS.  Therefore blocking the effects of estrogen upon key levels of the brain may blunt the psychological response one would expect from testosterone.

SERMs also are known to act as estrogen agonists (active estrogens) in the liver.  This can have a couple of relevant effects.  First of all, estrogens strongly promote the production of sex hormone binding globulin (SHBG).  This protein circulates in your blood and irreversibly binds to sex hormones such as testosterone, rendering them inactive.  So with a SERM you may have high total testosterone levels but actual bioactive testosterone may not be so high.

Another consequence of SERM estrogen agonist action in the liver is suppression of IGF-1 production.  IGF-1 is a systemic hormone responsible for whole body anabolism and it is produced in the liver under the positive influence of growth hormone, as well as other hormones such as insulin, thyroid hormone, and androgens.  Estrogens on the other hand suppress IGF-1 production in the liver.  In a recent study* it was directly demonstrated that administration of either tamoxifen or raloxifene to males increased LH and testosterone levels (as expected).  However they also significantly reduced circulating IGF-1 production.  Given the fact that it is well demonstrated that exogenous administration of testosterone increases IGF-1 levels in the blood you begin to see that this may be a big part of the SERM testosterone mystery.  Systemic IGF-1 levels may not do much for contractile muscle tissue growth but they can lead to overall body composition changes and increases in bodyweight.  The difference between the suppressed  IGF-1 state (compared to control) of the SERM user to the heightened IGF-1 state (compared to control) of the exogenous testosterone user may indeed be quite profound.

In conclusion, I suspect that once all this information is considered and digested by people then the use of SERMs may go out of favor as an alternative to testosterone replacement therapy.  It is my personal opinion that carefully titrated estrogen control via use of an aromatase inhibitor (perhaps combined with a proven natural testosterone elevator such as D-Aspartic Acid)  may be a smarter way to achieve the end goal of natural testosterone elevation.




New Steroid Sold as Supplement Part 2

By Patrick Arnold

If you read part one you know I am discussing the mystery steroid in the product known as “Super DMZ”.  I have to warn you, part 2 is going to be a little technical.  I will summarize what is important though in simple language at the end.

The ingredient is referred to most commonly as Ethylene Deltenone,and it is a readily available synthetic intermediate used in china for manufacture of some progesterone derivative drugs.  What it is, in organic chem speak, is the 3,3-ethylene ketal of estra-4,9-diene-3,17-dione.  Estra-4,9-diene-3,17-dione, as you may know, was a popular prohormone ingredient that was commonly (and somewhat erroneously) referred to as “tren”.  “Tren” was made a controlled substance (anabolic steroid) in 2010 as the result of an administrative act by the Department of Health and Human Services.

So what is a “ketal”?  A ketal is a derivative of a ketone.  Chemists use certain derivatives of ketones to protect them during synthesis procedures.  For instance they may want to change another part of the molecule using some reaction but they can’t do that without messing up the ketone.  So they first change the ketone into a derivative that is impervious to the procedure they want to perform on the other part of the molecule.  Then, after the reaction is completed, the protecting group is removed (hydrolyzed) and the ketone is reformed.  Examples of ketone protecting groups other than ketals are thioketals, acetals, oximes, semicarbazones, and many others.

[Note:  this topic of ketone protecting groups has ramifications that go beyond just this product, and I will be discussing that later].

Check out the structures below.  On the left is Ethylene Deltenone.  On the right is what happens when you hydrolyze the ketal protecting group in Ethylene Dienone.  You get “tren” (plus an equivalent of ethylene glycol).  You may be wondering why the double bonds in Ethylene Dienone are shifted to different postitions.  This is just something which commonly happens when ketals are formed from ketones with conjugated double bonds (alpha-enones).  I don’t recall the explanation for this nor would it serve us to explain it here if I did (since this article is already far too technical).

So this is the question.  We know that Ethylene Dienone is hydrolyzed by chemical means (acid does this readily).  But will it hydrolyze in a similar manner in the body?  I looked into this and I did find research on other steroid ethylene ketals.   This research indicated that  indeed ketals do readily hydrolyze in the body back to ketones (perhaps via enzymes).  The second question is whether or not the double bond isomerization back to 4,9 will occur with in-vivo hydrolysis.  This I am not entirely sure about.  It may not.  Acid may be required to catalyze this double bond shift and it is possible that in-vivo hydrolysis lacks this acid component.  In that case you would be left with the double bonds in the 5(10),9(11) configuration – which is a configuration that I doubt is associated with much physiological activity.

What do we have here?

What we have here is (possibly) a “tren” pro-drug – a chemical derivative of “tren” that might convert to “tren” in the body.  But didn’t they ban all chemical pro-drug derivatives with the latest update to the anabolic steroid control act back in 2010?  Actually they didn’t.  And although I didn’t say anything about it at the time I had to shake my head in disbelief when I read the provision in that law where they thought they were covering their assess by making all hydrolyzable chemical derivatives of AAS illegal.  I shook my head because they only covered derivatives of alcohol groups – specifically esters and ethers.  They completely neglected the whole slew of ketone derivative possibilities.  I always thought in the back of my mind that someday someone would figure this out and make a ketal or hydrazine or whatever of a controlled steroid.  Finally it appears someone has done just that (although I doubt IronMagLabs did this intentionally – rather I think they just stumbled into this).

Bottom line then is that this is the first ketone derivative of a controlled anabolic steroid to hit the market.  Whether it fully converts into its original compound via double bond isomerization in-vivo is still up for debate.  But this whole situation is much larger than “super dmz” because now that this has been done, and I have shined a big search light on it, we may expect to see nandrolone 3-oxime, or dihydrotestosterone-3,3-dimethyl acetal, or trenbolone-3-semicarbazone – all easily synthesized derivatives of controlled anabolic steroids that can slip through yet another loophole due to an inexplicable oversight by legislators.

When will this silliness end?



New steroid sold as a supplement – Does it work? Is it a controlled substance? (Part I)

By Patrick Arnold

The bodybuilder message boards have been going crazy with folks who are curious about a new grey market supplement product called “Super DMZ”, sold by a company called IronMagLabs.  This product contains two synthetic steroid products with structures (not to mention marketing claims) suggesting they are in the class of anabolic / androgens.

One of the ingredients is already known by many under the name of dimethazine.  Dimethazine is a steroid that was sold at one time overseas and consists of two molecules of methasterone (aka superdrol) linked together by an azine group at the 3 positions.  This azine group is hydrolyzable in the body so basically dimethazine is a methasterone prodrug.  As such it delivers many of the same anabolic effects as methasterone, along as presenting similar toxic risks.

The second ingredient in Super DMZ is the interesting ingredient and the one surrounded by all the mystery.  Much of the mystery arises from the fact that IronMagLabs is being deliberately evasive about the true nature of the compound.  They have changed the name of the compound once already, and the names they have utilized had faulty syntax and spelling.

The first name they used, even though they screwed it up, was descriptive enough that myself and a couple of other people were able to decipher its identity.  IronMagLabs then oddly changed the name, perhaps due to fear that the first name was too descriptive and not secret enough.  Forget the fact that it is illegal to not disclose ingredients on a label (this is the bizarro world of grey market supplements).  Anyway, the first name they used was 3-ethylenedioxy-stem-5(10),9(11)-dien-17-one.  Although they bastardized this name it is pretty clear that what they are referring to is 3,3-ethylenedioxy-estra-5(10),9(11)-17-one.  Now before I explain what this compound is (i.e. what its used for, and  what probably happens to it in the body) I will tell you what IronMagLabs is claiming

To be honest it’s really hard to figure out what IronMagLabs is claiming, but I will tell you what comments they made when pressed on the Anabolic Minds message board.  The first comment was “A Mifepristone intermediate; antiprogestational antiglucocorticoid antagonist steroidal spirooxazole.”   Now this is true, in fact it was taken right off the website of a chinese company which supplies this compound.  However, if IronMagLabs is suggesting that it has pharmacological activity similar to mifepristone (also known as RU-486 or the abortion pill) they are gravely mistaken.  It is simply a chemical intermediate (and quite a distant one from the final drug target).  The next comment IronMagLabs made was even stranger.  It was simply a link to the Wikipedia entry for the endometriosis drug gestrinone.  Like mifepristone, gestrinone has anti-progestational activity but unlike mifepristone there is no connection whatsoever (not even a nebulous one regarding chemical synthesis processes) between gestrinone and their mystery steroid ingredient.

So putting aside all the confusing banter put out by IronMagLabs , let’s look at what this ingredient really is.

End of Part I



Arnold Classic 2012

By Patrick Arnold

Last weekend I attended the Arnold Classic Fitness Expo – just like I have every year for the last 15 years.  Boy has that show changed.  The first several years the expo was primarily a bodybuilding event and it was more or less a freak show with ripped bodybuilders everywhere and tons and tons of scantily clad women.  Now it’s become more of a family event, with regular people of all ages walking around.  Of course that’s in large part because it’s become way more than bodybuilding.  In addition to the fitness expo there is the Arnold Sports Festival going on, which includes competitions in over 30 sports.  Many of these sports are quite far removed from bodybuilding, and there are many sporting events that include children as competitors.   As a result, the whole feel of the show has been changed towards a more “wholesome” atmosphere.

Most of the years I have gone to the Arnold it has been as a supplement company vendor with a booth.  This year I worked the booth of my primary nutritional supplement company Epharm.  Working the Epharm booth is a lot of fun because we sample our energy shot Clearshot Concentrate.  Clearshot Concentrate is a wicked hot spicy shot that hits you almost instantly, so it’s a blast to see unsuspecting people shoot one down and then react.  Reactions include crying tears, yelps, contorted faces, looks of shock, and the occasional person who feigns the stoic face but is actually peeing their pants.  Often – after the burn goes away and they get their senses back, – they realize how awesome they feel and they proceed to buy a bottle.  We sold a ton last weekend.

The Arnold expo floor is very crowded for most of the hours it is open, so those who work the booths are essentially trapped.  The Epharm booth however was on the far edge of the show and right behind the curtains was the emergency row.  The emergency row is blocked off and empty, so we were able to sneak in and out of our booth with relative ease.  Still, to walk the actual expo floor is pretty much impossible except for late on Sunday, so that’s when I hit the floor to see what was going on.

There wasn’t a whole lot of new stuff to see.  I got to meet up with some of my friends from other companies and chit chat.  One of these guys is a person named Markel Boulis, who owns 2:1 protein bar company.  He won the GNC protein bar of the year award again (I

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think this is like his third award in five years).  His bars are remarkable, almost too good to be true.  Anyway what makes Markel’s story interesting is that I met him in prison back in 2006-2007.  We were in the same unit and hung out a lot.  Markel was a chiropractor and had nothing to do with the supplement business.   After prison I never talked to him but then at the Mr. Olympia expo I ran into him at his bar booth.  It was quite a shock to see that this guy got out of prison and started a company and within two years had won the best protein bar in GNC.

I also talked to John Perrotta who was promoting an interesting product called the spider bottle.  The spider bottle is a shaker bottle with a built in wire spring that serves to open and close when the bottle is shaken.  This spring oscillates and acts sort of like a whisk to break up lumps and ensure complete even mixing.  It’s a neat little invention and John is a good salesman and a nice guy.

On Saturday I hung out quite a bit with Vince Andrich, an industry vet who is working with Dr. Scott Connelly on introducing a new protein powder called Myotropics.   The protein powder should be on the shelves any day now and is some sort of high grade whole milk protein.  I am looking forward to trying it.   Vince always is fun to talk to because he has been through it all in this industry.

Last but not least I wanna give a call out to my dear friends Rick Collins, Mike Dimaggio, Marc Gann, and Alan Feldstein.   Yes, these guys have been my attorneys for years but our relationship goes far beyond a professional one.   They have to be the most clever and hilarious people I know, and they truly care about me and my business partner Lakhan – not just on the attorney/client level but on a personal level as well.

I am sure I skipped over a lot of other interesting things that happened that weekend.  No, I did not attend the bodybuilding show.  I am not a huge fan of competitive bodybuilding and with so much other stuff going on it’s just not worth it to spend a few hours watching posing and flexing.

If you have never attended the expo you should make an effort to get there at least once in your life.  Next year is the 25th anniversary so it should be an interesting spectacle.   If you attend and run into me please say Hi (just look for the name badge around my neck)




One man can make a difference

By Patrick Arnold

I have good news to tell everyone! Considering how our nutritional supplement industry has been under unprecedented assault here in the states with the FDA’s intolerant and strong handed stance on issues, issues that intend to dismantle what our whole industry is based upon ( a law called DSHEA), I find this recent small development something worthy of recognition. Something to remind us all that we CAN make a difference.

In this blog, on January 4th, I told you all about an issue regarding 7-keto DHEA (and derivatives thereof). This issue involved the government of the United Kingdom (UK) and some unfortunate knee jerk legislation motivated by a desire to make everything “peachy keen” for the upcoming 2012 London Summer Olympic Games. We can all completely understand why they (the UK government officials involved) would want to make their olympic games as clean and controversy free as possible. Problem is these folks are not qualified to make certain decisions. So these folks rely upon organizations such as the World Anti Doping Agency (WADA) for guidance.

WADA’s job is to make sure athletes don’t resort to artificial means to enhance their performance. That is a pretty hefty load to carry, considering how our modern world kind of exists upon artificial means to help pretty much everything. Anyway, WADA does their job as they feel it needs to be done. Which means ban everything that even can remotely be imagined to help performance. That’s cool, let them do that. Unfortunately the problem occurs when their athletic organization laws carry over into policy of state government. Then it gets weird.

And it got weird in the UK. Basically what happened was some government bureaucrats had good intentions gone stupid. These folks thought that it would look good to the rest of the world if on the eve of the summer games they banned some of these nasty performance enhancing drugs (in this case stuff classified under the category of steroids – a tragically misinterpreted chemical term….).

By banned I mean banned officially by the UK government. These bureaucrats figured that their guide would be the WADA list of banned substances. Hell, they didn’t know any better.

Problem is, WADA does some strange things. For all intents and purpose they kind of do whatever they want. And whatever they want often makes little sense – as in classifying compounds as anabolic steroids that are not anabolic steroids. Which is exactly what happened with 7-keto DHEA. WADA decided (arbitrarily, capriciously, and with no effort insofar as to background research) to add 7-keto DHEA to the list of anabolic steroids

So taking the baton from their WADA masters these UK bureaucrats thought they would do a wonderful thing by banning 7-keto so that no UK citizen can touch the stuff without being a serious criminal – all because they trusted that what is on the WADA list must certainly be verified “bad”. Bad not just for helping an athltete perform better but bad for society in general. The assumption was it must be a dangerous substance of abuse. This is no exaggeration

The real sad thing is all this would have happened without protest – that is if it weren’t for my eagle eyed friend Andy.

Andy, a UK citizen, somehow got wind of this pending legislation and he informed me of it. How he knew about it I don’t know. This issue is not something that is front page news so Andy had to have made an effort to catch this. Andy apparently took to time to read the news that falls through the cracks. I was quite taken aback by all this when Andy emailed me and told me.

It’s kind of a big deal to me – 7-keto DHEA and its derivatives such as beta-AET are supplements I often tout as being one of very few products that really, really do something and have scientific support. And I know they are not anabolic steroids. Not even close. I am quite familiar with pharmacology as it relates to these substances.

So this is what I did. I told Andy to contact Humanetics Corporation. I know the people there, I have visited them and done business with them. They own the patent on 7-keto DHEA. They actually originally intended to sell the product as a drug, and then decided to market it as a supplement. These guys have worked closely with the United States FDA and they have very impressive documentation on the safety and efficacy of 7-keto. But not just the safety – more importantly they went out of their way to prove that it is NOT an anabolic steroid – as per the classical pharmacogolical definition.

Recall that 7-keto dhea has a steroid structure – but that does not mean it is an anabolic steroid. Anabolic steroids are a class of drugs associated with well documented ethical and toxicological concerns. A square is a rectangle but not all rectangles are squares. U follow me? i hope someone does….

Anyway, Andy contacted Humanetics, and as I anticipated they were quite taken aback. Humanetics proceeded to get in touch with the relevant characters in the UK and they provided them with their abundant archives of scientific and US government agency related documenations that convincingly showed that 7-keto (and its derivatives)

1) are not anabolic steroids

2) have undergone extensive safety and efficacy studies published in highly regarded peer reviewed journals

3) is (7-keto dhea specifically) explicitly recognized by the US FDA as a legitimate dietary supplement ingredient

So kudos to Andy and how he stayed on this issue till it was resolved. One person can make a difference sometimes

the UK reversed their decision. Document below

12-02-07 Further advice ACMD (2)