Preclinical and the first clinical studies on [11C]CHIBA-1001 for mapping α7 nicotinic receptors by positron emission tomography

摘要

Objective 4-[11C]methylphenyl 2,5-diazabicyclo[3.2.2]nonane-2-carboxylate ([11C]CHIBA-1001), a 4-methyl-substituted derivative of the selective α7 nicotinic acetylcholine receptor (α7 nAChR) partial agonist 4-bromophenyl 1,4 diazabicyclo[3.2.2]nonane-4-carboxylate (SSR180711), is a potential radioligand for mapping α7 nAChRs in the brain by positron emission tomography (PET). In this study, we performed preclinical and first clinical PET studies using [11C]CHIBA-1001 for imaging α7 nAChRs in the human brain.