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Thursday, November 19, 2009
Sports Doping Drugs Available Online
Drugs not yet approved for medical use are easily accessible online to cheating athletes.
By Emily Singer
An experimental drug that mimics the effect
of steroids, such as testosterone, without many of the harmful side effects is
freely available online, according to new research. A group from the German
Sport University Cologne in Germany detected the compound in a product called
Andarine, available online for $100 and labeled as green tea extracts and face
moisturizer. The research appears in the current issue of the journal Drug
Testing and Analysis.
Known as selective androgen receptor
modulators, or SARMs, the drugs are being developed for diseases such as muscle-wasting and osteoporosis. The World
Anti-Doping Agency, an international, independent organization based in
Lausanne, Switzerland, that coordinates anti-doping regulations across sports,
banned the drugs last year, before any of them were approved
for medical use, in recognition of the molecules' potential allure to sports
dopers, and athletes' willingness to take even experimental compounds. Since then, the agency has quietly been working with scientists across the globe to develop new tests to detect illegal use of the compounds.
According to a previous TR article on sports doping,
These drugs represent "a whole new horizon for anabolic therapies, and the
potential for abuse will be exceedingly high," says William Evans, director of the Nutrition, Metabolism, and
Exercise Laboratory at the University of Arkansas for Medical Sciences.
SARMs work similarly to testosterone but in a more targeted
way. "They are effective by binding to the steroid receptor in only
specific tissue, like muscle," says Evans, who is also a scientific
advisor to GTx, a company
developing the drugs. "They are not steroid drugs, but they produce the
anabolic effect of the steroids." GTx, based in Memphis, TN, has shown in
a clinical trial that one compound being developed for muscle wasting and bone
loss can significantly boost lean muscle mass in older people.
According to a press release from the journal,
Mario Thevis, Ph.D., and colleagues, analyzed the advertised
substance using state-of-the-art mass spectrometric approaches with high
resolution/high accuracy (tandem) mass spectrometry. "One unit (30 mL) was
purchased online and delivered in a box labeled to contain face moisturizer and
green tea extract. The sealed bottle did not declare any content and no further
documents accompanied package," said Dr. Thevis. He went on to explain
that LC-MS(/MS) analysis of this solution revealed the presence of S-4 at
approximately 150 mg/mL with equal amounts in each container, yielding a total
of 4.5 g of the SARM. The active ingredient was identified and characterized by
a) its elemental composition (as determined by high resolution/high accuracy
mass spectrometry, b) comparison to synthesized reference material regarding
retention time and product ion mass spectrum, and c) elucidation of its mass
spectrometric behavior. Besides the detection of the active ingredient S-4, a
significant amount of byproduct was observed.
"Major
concerns result from these findings," explained Dr. Thevis. "This
product with considerable anabolic properties is readily available without
sufficient research on its undesirable effects; this is especially significant
where uncontrolled dosing is applied and drug impurities with unknown effects
are present in considerable amounts as observed in the studied material."
The
issue was recently addressed at the Conference of Parties to the International
Convention against Doping in Sport, held October 26-28, 2009 at the United
Nations Educational, Scientific and Cultural Organization's (UNESCO)
headquarters in Paris. WADA President John Fahey said that government agencies
will need to adopt laws and regulations to combat the trafficking and supply of
illegal substances in order to rid sport of doping.
The
ease of purchasing SARMs as a performance-enhancing drug supports the need to
make early implementation of screening for emerging therapeutic compounds a
routine part of sports drug testing. "Our study demonstrates once more
that the misuse of therapeutics without clinical approval by athletes cannot be
dismissed," Dr. Thevis concludes.
Tuesday, July 07, 2009
Doping Hormone Erythropoietin Also Boosts Brainpower
The red-blood-cell-boosting hormone is already used to treat anemia and by some athletes to boost endurance.
By Emily Singer
The red-blood-cell-boosting hormone erythropoietin (EPO), which is used
clinically to treat anemia and illegally by athletes to boost endurance, may
also improve brainpower. According to research published in the journal BMC
Biology, mice treated with the drug performed better in certain learning
and memory tests than did control animals.
EPO is popular among dopers because it increases blood oxygenation,
mimicking the effect of blood doping. But it also targets the nervous system,
improving survival of brain cells. The drug is currently in clinical trials for
traumatic brain injury and stroke. (A previous post describes
how EPO blocks brain swelling after trauma.)
The new research looks at how the drug affects a healthy brain. According to
a press
release issued by the journal,
[Hannelore] Ehrenreich [from the Max Planck Institute of Experimental
Medicine, in Göttingen, Germany] and her colleagues tested the effects of
erythropoietin on the ability of the mice to learn how to exploit an
experimental set-up to receive sugared water. Over a series of learning stages,
the mice were trained to get their treat by poking their noses into holes lit
by LEDs, rather than into unlit holes, within a time limit. The mice that had
been treated with recombinant human erythropoietin were significantly more
likely to master the task than those that had not. According to Ehrenreich, "Treated
mice showed superior performance in associative, operant and discriminant
learning as well as in the initial training phases. Moreover,
erythropoietin-treated mice demonstrated better task adaptation and higher
performance stability." The researchers conclude, "Further untangling of molecular mechanisms
of erythropoietin action on higher cognitive functions may ultimately open new
avenues for prevention strategies and therapeutic interventions in
neuropsychiatric diseases."
Thursday, January 08, 2009
Dope Test Before Drug Is Tested in Humans
Scientists are creating anti-doping tests earlier and earlier in drug development.
By Emily Singer
Some athletes and trainers are tuned in to the drug-development pipeline, looking for the next big doping agent: experimental drugs
that can boost strength and endurance but are new enough to slip under the
screening radar. One scientist I spoke to for a previous piece on doping said that he still gets flooded with calls from athletes years after publishing details of a promising
advance in drug development for muscular dystrophy.
In an effort to combat the abuse of new compounds before it
starts, anti-doping agencies have begun working with drug companies to develop screening tests
before drugs are even on the market. In last year's Tour de France, the
World Anti-Doping Agency caught several cyclists using a longer-lasting form of
the endurance booster EPO (erythropoietin), called CERA. Soon after the
athletes were caught, it was revealed that the agency had been working with
Swiss drugmaker Roche to develop a test to detect CERA while the drug was still
being tested by the U.S. pharmaceutical company Amgen.
Now German scientists announce that they have developed a test
for a class of compounds called benzothiazepines,
which are being developed for
the treatment of heart abnormalities and have been shown to boost endurance in
mice. According to a press release from Drug
Testing and Analysis, the journal
publishing the research,
These
compounds stabilize protein channels that would otherwise "leak"
calcium from muscle cells during strenuous exercise. Calcium is needed for
muscle contraction and this "leaking" effect weakens the contractions
and is a causal factor in muscle fatigue.
While the drugs have not yet been
tested in humans, researchers say that they carry a high potential for abuse because
they are easy to make.
"As soon as these drugs enter
human clinical trials, there is a huge potential for them to be misused in
sports. This preventive research lets us prepare before these compounds are
officially launched," says Mario Thevis, Director of the Center for
Preventive Doping Research at the German Sport University of Cologne, Germany,
who led the research. The study characterises the compounds according to their
weight and molecular structure. This gives the researchers a molecular
"fingerprint" by which to identify the compounds. Thevis and
colleagues show that, using high resolution mass spectrometry, JTV-519 and
S-107 can be detected in spiked urine at concentrations as low as 0.1 nanograms
per millilitre.
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