Getting The "Exercise Effect" From A Pill

FOR RELEASE: (Print & Broadcast) Wed., April 16, 9:30 a.m., PDT ACS
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GETTING THE 'EXERCISE EFFECT' -- FROM A PILL

SAN FRANCISCO, April 16 -- "There are two ways to approach the treatment of obesity, a condition that affects approximately one in three Americans," according to Dr. Robert Dow, principal research investigator with Pfizer Inc, who is presenting a paper at the American Chemical Society national meeting here today. "Either you inhibit food intake, or you improve energy expenditure to get the 'exercise effect.'" Pfizer, based in Groton, Conn., has developed compounds that in animal trials boosted metabolic rates to mimic the exercise effect of increased calorie burning -- without exercise. The tests showed a 10 to 30 percent jump in metabolic rate. "If you have a 10 percent increase in energy expenditure, you're potentially looking at about a half pound a week drop in weight," Dow says. There are currently no drugs on the market that work this way.

Intriguingly, the compounds do not seem to bring about one other effect of an exercise-induced hike in metabolism. "If I go out and ski all day and I come in, I'm ravenous and I eat more," Dow says. "But that sort of compensation has not been seen in the animal tests with these compounds."

The compounds are hormone mimics that act on the beta-adrenergic system, which has three sub- types of receptors in cells in the body. These receptors are stimulated by the adrenaline released in the body's fight-or-flight response to danger. One of the receptor types is predominant in the heart, where it is involved in raising the heart rate. A second type is involved in dilation of blood vessels and a drop in blood pressure. The third type of receptor is found in fat tissue, and it's this one that the compounds stimulate, boosting metabolism. That means they leave the other two types of receptors alone, minimizing side effects.

Some previous similar compounds passed through animal trials with flying colors but failed in human clinical trials, Dow says. He explains this is because they were developed before the human beta-3 adrenergic receptor had been identified. The Pfizer compounds, on the other hand, work better at that receptor, so Dow expects them to perform better in the human trials than their predecessors. If human clinical trials are successful, the compounds could be available within five to ten years, Dow says.

MEDI 180 will be presented at 9:10 a.m., Wed., April 16, in Room 135, Exhibit Level, Moscone Center. The national meeting of the American Chemical Society will be held in San Francisco April 13-17. This paper is among the 7,700 presentations that will be made. # # # #

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The American Chemical Society, founded in 1876, is the world's largest scientific society, with more than 151,000 members.