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Acetylcholinesterase and butyrylcholinesterase accumulate with brain β-amyloid (Aβ) plaques in Alzheimer disease (AD). The overall activity of acetylcholinesterase is found to decline in AD, whereas butyrylcholinesterase has been found to either increase or remain the same. Although some cognitively normal older adults also have Aβ plaques within the brain, cholinesterase-associated plaques are generally less abundant in such individuals. Thus, brain imaging of cholinesterase activity associated with Aβ plaques has the potential to distinguish AD from cognitively normal older adults, with or without Aβ accumulation, during life. Current Aβ imaging agents are not able to provide this distinction. To address this unmet need, synthesis and evaluation of a cholinesterase-binding ligand, phenyl 4-(123)I-iodophenylcarbamate ((123)I-PIP), is described.

the journal of nuclear medicine

Synthesis and Preliminary Evaluation of Phenyl 4-<sup>123</sup>I-Iodophenylcarbamate for Visualization of Cholinesterases Associated with Alzheimer Disease Pathology

Synthesis and Preliminary Evaluation of Phenyl 4-123I-Iodophenylcarbamate for Visualization of Cholinesterases Associated with Alzheimer Disease Pathology

Synthesis and Preliminary Evaluation of Phenyl 4-¹²³I-Iodophenylcarbamate for Visualization of Cholinesterases Associated with Alzheimer Disease Pathology