Localization of serotonin 5‐HT2 receptors in living human brain by positron emission tomography using N1‐([11C]‐methyl)‐2‐BR‐LSD
Synapse January 1, 1987 Dean F. Wong, John R. Lever, Paul Hartig et al. 93 citations
A new radioligand, [11C]-MBL, selectively binds to serotonin 5-HT2 receptors in the brain, as shown by in vitro assays (Ki = 0.5 nM) and PET imaging in baboons and seven healthy human volunteers. In humans, highest binding occurred in frontal, temporal, and parietal cortex, with lower levels in caudate and putamen. Blocking with ketanserin confirmed specificity. Frontal cortex-to-cerebellum ratios ranged from 1.7 to 2.7, with older volunteers showing lower ratios, suggesting age-related decline in 5-HT2 receptor density. [11C]-MBL enables in vivo monitoring of these receptors in most human brain regions.