Jamming brain receptor could make epilepsy drugs more effective

NEW YORK, N.C., Sept. 8 (UPI) -- A better understanding of how epilepsy drugs work may help researchers design drugs that are more effective for more people.

Researchers at Columbia University Medical Center found how the drug perampanel blocks AMPA receptors in the brain, which transmit electrical signals and play a role in the development of seizures, which they say will help in the development of more effective drugs.

While perampanel is effective at blocking AMPA receptors, and is the only drug approved by the U.S. Food and Drug Administration that does so, but carries significant side effects and is not widely used for treatment.

"Our data suggest that the inhibitors wedge themselves into the AMPA receptor, which prevents the opening of a channel within the receptor," Dr. Alexander Sobolevsky, a professor of biochemistry and molecular biophysics at Columbia University Medical Center, said in a press release.

For the study, published in the journal Neuron, researchers used crystallography to see how perampanel and two other inhibitors operate by observing how they interact with rat AMPA receptors, which are similar to those in humans.

"The problem is that AMPA receptors are heavily involved in the central nervous system, so if you inhibit their function, you cause an array of unwanted effects," Sobolevsky said. "If we hope to design better drugs for epilepsy, we need to learn more about the structure and function of these receptors."