The Exercise Pill

By | December 10, 2008

The drug … changed the physical composition of muscle, essentially transforming the tissue from sugar-burning fast-twitch fibers to fat-burning slow-twitch ones – the same change that occurs in distance runners and cyclists through training. – co

The ability to buy exercise in a pill form is near — relatively speaking. Despite short notice, Olympics’ no-doping committees are preparing to test athletes for AICAR, a chemical shown to increase muscle endurance, even without exercise. Published in the July 31 online issue of Cell, researchers at the Salk Institute for Biological Studies found that AICAR, administered daily for four weeks, increased the endurance of sedentary mice by 44 percent. While it may be several years before average consumers can buy AICAR commercially, non-FDA approved access is expected.

Study co-author and developmental biologist Ronald Evans tells Scientific American that AICAR is “tricking the muscle into ‘believing’ it’s been exercised daily,” and that the study “proves you can have a pharmacologic equivalent to exercise.”

How is exercise in a pill form possible?

In summary, endurance training produces metabolic and structural changes in the muscles. This study shows that AICAR can produce muscle reformation –a state influenced by gene expression (or activation), increased cellular energy and muscle fiber composition.

Two types of muscle exist: Type 1 (slow-twitch) and Type 2 (fast-twitch). Type 1 burns more fat (oxidizes fatty acids), is more resistant to fatigue — due to an abundance of mitrochondria producing cellular energy — and increases with endurance training.

Type 2 muscle fibers contain fewer mitrochondria, fatigues more easily, burns glucose and is commonly found in obese and sedentary individuals.

Science Daily, among other sources provided, provides a digestible in-depth explanation of the way AICAR further works at the cellular and metabolic level to achieve increased muscle endurance.

How much will the exercise pill cost?

The so-called “exercise pill” will, at least initially, be out-of-reach for most exercise-challenged individuals. – ac

The compound, which is naturally produced in tiny amounts in human muscle cells and has been studied for decades, is readily available through Web sites that cater to researchers. One site was offering it for $120 a gram. – co

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AICA ribonucleotide or AICAR (aminoimidazole carboxamide ribonucleotide) is an intermediate in the generation of inosine monophosphate, which acts as an AMP-activated protein kinase agonist.[1] It stimulates glucose uptake and increases the activity of p38 mitogen-activated protein kinases α and β in skeletal muscle tissue,[2] as well as suppressing apoptosis by reducing production of reactive oxygen compounds inside the cell.[3]

In 2008, researchers at the Salk Institute discovered that AICAR given to experimental mice significantly improves their performance in endurance-type exercise, apparently by converting fast-twitch muscle fibers to the more energy-efficient, fat-burning, slow-twitch type. They also looked at the administration of GW 501516 (also called GW1516) in combination with AICAR. Given to mice that did not exercise, this combination activated 40% of the genes that were turned on when mice were given GW1516 and made to exercise. This suggests it may be possible to obtain some of the benefits of exercising without actually exercising.[4] Because of the enhanced endurance effects, this could potentially be used by athletes to enhance their performance. One of the lead researchers from this study has developed a urine test to detect it and has made the test available to the International Olympic Committee,[5] and the World Anti-Doping Agency has added AICAR to the prohibited list from 2009 onwards.[6]wiki

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