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31 July 2014 - Just published: regulation of 5-HT1A receptors in Alzheimer disease brain

Alzheimer disease is associated with profound changes in neurotransmitter regulation in the brain. The hippocampus is one brain region that regulates memory and serotonin 5-HT1A receptors are highly expressed therein. The present study examined post-mortem hippocampus from Alzheimer disease patients and found that the density of 5-HT1A receptors in an active state (detected with the biased agonist radiotracer [18F]F15599), decreased from early stages of the disease. These changes were not detected when using the antagonist radiotracer [18F]MPPF which recognises all 5-HT1A receptors, regardless of their activation state. These results suggest that it may be possible to identify early changes in activity in a brain region that is important for cognitive function. New strategies for detecting and treating Alzheimer disease are urgently needed in view of the rapidly ageing demographic profile of many developed countries.

Adrian Newman-Tancredi has extensive experience of drug discovery of serotonergic agents. For more information, Contact.

 

A Postmortem Study to Compare Agonist and Antagonist 5-HT1A Receptor-binding Sites in Alzheimer's Disease.
Becker G, Streichenberger N, Billard T, Newman-Tancredi A, Zimmer L.
CNS Neurosci Ther. 2014 Jul 9. doi: 10.1111/cns.12306. [Epub ahead of print]