Abstract
The 5-HT 1A receptor antagonist, WAY-100635 [ N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)- N-(2-pyridyl) cyclohexanecarboxamide], was labelled in its carbonyl group with carbon-11 ( t 1 2 = 20.4 min ), injected intravenously into healthy male volunteers and studied with positron emission tomography (PET). The acquired data provide exquisite delineation of 5-HT 1A receptors in brain, with the ratio of radioactivity uptake in receptor-rich regions, such as medial temporal cortex, to that in receptor-devoid cerebellum reaching 25 by 60 min after radioligand injection. Application of biomathematical modelling to the data revealed high values (7.8) for binding potential, a measure of B max K D , in receptor-rich regions. Only very polar radioactive metabolites were present in plasma, a finding consistent with the low level of nonspecific binding seen in cerebellum. [ carbonyl- 11C]WAY-100635 is concluded to be far superior to the previously reported [ O-methyl- 11C]WAY-100635 as a radioligand for PET studies of 5-HT 1A receptors in human brain.
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