Validation of reference tissue model of PET ligand [¹¹C]+3-MPB for the muscarinic cholinergic receptor in the living brain of conscious monkey.

N-[¹¹C]methyl-3-piperidyl benzilate ([¹¹C]+3-MPB) was developed as a positron emission tomography (PET) ligand for muscarinic cholinergic receptor (mAChR). The aim of the present study was to validate a Logan reference tissue method as an analytical method for in vivo binding of [¹¹C]+3-MPB to mAChR. Seven monkeys (Macaca mulatta) underwent [¹¹C]+3-MPB PET scans with an arterial blood sampling. Logan plot with arterial input function (Logan arterial input method) was performed to determine the binding potential (BP(ND)). The BP(ND) was also determined by Logan plot with the cerebellum as the reference region (Logan reference tissue method). BP(ND) values determined by Logan arterial input method and Logan reference tissue method showed a significant linear relationship. The present study suggests that the cerebellum is a suitable reference region for quantification of mAChR in the living brain with [¹¹C]+3-MPB and PET.