Scientists, seemingly moving forward with discovery at all costs, have developed two molecular manipulations of metabolism. The LA Times carries the story.
One is known as AICAR, and the other as GW1516, a drug increasing PPAR peroxisome proliferator-activated receptors. PPAR-d binds to regions of DNA.
Scientists have discovered what could be the ultimate workout for couch potatoes: exercise in a pill.
In experiments on mice that did no exercise, the chemical compound, known as AICAR, allowed them to run 44% farther on a treadmill than those that did not receive the drug."You're getting the benefits of exercise without having to do any work," said David Mangelsdorf, a pharmacologist at University of Texas Southwestern Medical Center in Dallas, who was not connected with the research.
Great, no exercise and all benefits. Welfare cardio.
His team started not with AICAR but with another compound known as GW1516, which drug maker GlaxoSmithKline is trying to develop to raise levels of HDL, or good cholesterol. The drug is known to stimulate the production of a protein known as PPARd, which in turn activates the genes that boost endurance in muscle cells.
In sedentary mice, the drug had no effect on endurance. Only when the drug was combined with exercise did it give the mice an advantage. After five weeks of training, mice that got the drug were able to run for an average of three hours and 24 minutes, a 68% improvement over mice that received only training.
When the researchers dissected the test mice, they found that the number of high-efficiency muscle fibers had increased 29%. "That's a huge increase," Evans said. "That's the kind of stuff that Lance Armstrong and endurance athletes aim for."
The lab turned attention to AICAR. 5-amino-4-imidazolecarboxamide ribonucleoside (AICAR) markedly activates cellular AMP-activated protein kinase (AMPK). The drug also enhances insulin action.
Evans decided to try AICAR because it closely resembles a nucleotide that prompts the production of an enzyme that activates the high-endurance genes.
To Evans' surprise, the experiment worked. When sedentary mice were fed the drug daily for four weeks, they were able to run an average of 1,795 feet on a treadmill, 44% farther than mice that had received a placebo.
It is nice the lab thought of doping...
In the meantime, Evans said, his team has developed detection protocols for both compounds and their breakdown products and turned them over to the World Anti-Doping Agency in Montreal.
He said it was unclear whether the tests would be in place for the Olympics.
Frederic Donze, a spokesman for the association, said in an e-mail that the organization "does not indicate when it implements new detection means or methods."
But, he added, it is not crucial for the tests to be in place now.
"A number of anti-doping organizations, including the International Olympic Committee, store doping control samples of their events for eight years for potential future retesting and detection as anti-doping science advances," Donze said.
Someday these drugs, probably meant for muscle wasting disease will be appropriated for illicit uses. And so it goes.