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New piece to the puzzle of brain function
Date:8/19/2011

is interesting from an application perspective when the brain is activated via the new binding site, a stronger impulse is simply sent through the receptor's 'lock', and this leads to entirely new and exciting opportunities in future drug development."

The nicotinic acetylcholine receptors are structurally similar to the GABAA receptors, which also play an important role in pharmaceutical chemical brain research.

Benzodiazepines for insomnia and anxiety attacks constitute a class of well established drugs that act by modulating the GABAA system. The scientists believe that they have discovered the nicotine equivalent of a benzodiazepine binding site.

"It is likely that the discovery will form the basis for the development of better medicines for psychiatric disorders in the future because the combination of a mechanistic and a structural understanding of the receptor is a very good starting point for structure-based design of drugs that act via the new binding site," Harpse says.

The new research results were achieved in close collaboration with NeuroSearch a European-based biopharmaceutical company specializing in diseases of the central nervous system (CNS).

"All the experimental work is conducted at NeuroSearch with manager Philip Ahring acting as the head person. The laboratory work is inspired by structural models developed in our research group at the Faculty of Pharmaceutical Sciences. In order to fully understand the new binding site, we have performed numerous mutation studies and electrophysiological measurements, and in every way it has been a great working relationship with full openness and the opportunity for exchange of ideas - very rewarding for both parties," Balle says.


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Contact: Thomas Balle
tb@farma.ku.dk
453-533-6409
University of Copenhagen
Source:Eurekalert

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