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Treatment for Alzheimer’s disease has to date involved inhibiting the breakdown of the neurotransmitter, acetylcholine. This, however, has not been very selective and has therefore had limited effect.
Further research has shown that the M1-muscarinic acetylcholine (M1) receptor is an effective target for potential drug candidates; however, progress in this area has been hampered by adverse drug effects on gastrointestinal and cardiovascular systems.
In order to overcome these side-effects and be suitable for consumption by elderly patients, Sosei Heptares and Eli Lilly have joined forces to investigate an alternative therapy. This therapy promises to be more selective (activating receptors involved in learning and memory) and offers the potential for the relevant dosage to be applied without any major side effects.
Using Macromolecular Crystallography (MX) at Diamond, they were able to identify and study a selective M1-receptor orthosteric partial agonist (HTL9936) with the desired effects.
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