Derivatives of Drug Also Show Potential To Block Effects of Cocaine

ANAHEIM, Calif., March 22 -- A new more effective form of the drug Ritalin^™ (methylphenidate) that produces fewer side effects and has the potential to be used in anticocaine therapy could soon be available, according to research findings presented here today at the national meeting of the American Chemical Society, the world's largest scientific society.

Commonly prescribed to treat Attention Deficit/Hyperactivity Disorder (ADHD), especially in school-age children, Ritalin has an approximate $500 million annual market in the U.S. Estimates vary on the number of youngsters taking the drug, but published reports in the scientific literature indicate that possibly as many as three percent of the country's elementary and secondary students, about 1.5 million, are prescribed Ritalin.

Using a new synthesis developed in his lab, University of Pennsylvania chemist Jeffrey Winkler, Ph.D., and his research group were able to make analogues of Ritalin that he says "have never been prepared before." Additionally, he notes, "Some of those new compounds look like very interesting candidates as anticocaine therapies."

Being able to synthesize "chiral Ritalin" from inexpensive non-chiral starting materials is the key to the drug's improvement, says Winkler. Drug compounds generally have mirror images, known as being right and left handed, but often only one of the "hands" is biologically active, delivering the desired pharmacological agents. Drugs containing "both hands" are called racemic. If a drug can be made one-handed, or chiral, it generally means smaller doses are needed and it avoids any potential side effects that might be contributed from the other hand. Such is the case for Ritalin, says Winkler. "It means less side effects and also less drug would have to be taken," by only including the biologically active r
'"/>

Contact: Charmayne Marsh
y_marsh@acs.org
202-872-4445
American Chemical Society
23-Mar-1999