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Alzheimer's disease (AD) involves selective loss of muscarinic m2, but not m1, subtype neuroreceptors in cortical and hippocampal regions of the human brain. Emission tomographic study of the loss of m2 receptors in AD is limited by the fact that there is currently no available m2-selective radioligand which can penetrate the blood–brain barrier. We now demonstrate thein vivom2 selectivity of a fluorine...
A series of 5-[[[(dialkylamino)alkyl]-1-phenyl]acetyl]-10,11-dihydro-5H-dibenzo[b,e][1,4 ]diazepin-11-ones 1 were prepared as potential m 2 -selective ligands. The binding affinities and selectivities of these compounds for the muscarinic cholinergic receptor subtypes were determined. The best m 2 -selective antimuscarinic agent studied was 5-[[4-[4-(diisobutylamino)butyl]-1-phenyl]acetyl]-10,11-dihydro-5H-dibenzo[b...
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