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Propofol discovery may help lead to development of new anaesthetics
Date:9/22/2013

ed co-principal investigator Alex S Evers, MD, the Henry E. Mallinckrodt Professor and head of the Department of Anesthesiology at Washington University.

"We knew that intravenous anaesthetics, like propofol, act on an important receptor on brain cells called the GABAA receptor, but we didn't really know exactly where they bound to that receptor."

In an attempt to understand how propofol induces anaesthesia during surgery, scientists have tried to identify how and where it interacts with receptors in the brain called gamma-aminobutyric acid type A (GABAA) receptors. Activating these receptors with propofol for example stops a nerve cell communicating with its neighbours, leading to unconsciousness.

For this study, the scientists created a molecule that closely resembles and mimics propofol but has an added hook that grabs onto the GABAA receptor and won't let it go when it is activated by a bright light. They then extracted the receptor, cut it into pieces and identified the place on the protein that the propofol mimic had attached to.

Using the techniques they have developed, the scientists say they will now identify binding sites of other anaesthetics. They believe their approach also can be used to study other types of drugs, such as psychiatric agents and anti-seizure drugs.


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Contact: Simon Levey
s.levey@imperial.ac.uk
44-020-759-46702
Imperial College London
Source:Eurekalert

Page: 1 2

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