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Penn researchers demonstrate a new model for drug discovery with a fluorescent anesthetic
Date:4/3/2009

PHILADELPHIA - A collaboration of University of Pennsylvania and University of Wisconsin chemists and anesthesiologists have identified a fluorescent anesthetic compound that will assist researchers in obtaining more precise information about how anesthetics work in the body and will provide a means to more rapidly test new anesthetic compounds in the search for safer and more effective drugs.

The study is published online in the Proceedings of the National Academy of Sciences.

Using the fluorescing compound 1-aminoanthracene, or 1-AMA, the team developed a high-throughput assay to test for new anesthetic compounds. The assay will allow researchers to search for new anesthetic drugs and new molecular targets for anesthetics while at the same time creating high-resolution images of the compounds in action, a missing component that has hindered anesthetic research.

Researchers confirmed the compound as anesthetic after testing it successfully in tadpoles. By using transparent, albino tadpoles in the study, researchers were able to follow the fluorophore tag and image it in the brain of the immobilized, living animal.

Because the compound is fluorescent, researchers are able to image the compound in vivo in order to study its physiological effects. Where and how an anesthetic compound travels in an organism when administered and to what cells and concentrations are unknown in anesthetic administration and a key to improving efficacy and to reducing side effects. Because anesthetics bind weakly to their chemical targets, which may play a role in some of the unintended side effects, searching for new targets in the central nervous system is difficult.

"We don't know much about how anesthetics work at a molecular level," said Roderic G. Eckenhoff, vice chair for research and the Austin Lamont Professor of Anesthesiology and Critical Care at Penn's School of Medicine. "Thus, the development of new anesthetics h
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Contact: Jordan Reese
jreese@upenn.edu
215-573-6604
University of Pennsylvania
Source:Eurekalert

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