V. Pike, I. A. Cliffe, A. Fletcher
1995
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Abstract
N-(2-(1-(4-(2-Methoxyphenyl)-1 -piperazinyl)ethyl))-N-(2-pyridyl)cyclohexanecarboxamide (WAY-100635) has properties that favour its development as the first radioligand for studies of 5-HT1A receptors in vivo with positron emission tomography (PET). These include high potency, high selectivity, pure antagonist action and amenability to labelling with the positron-emitter, carbon-11 (t 1/2 = 20.4 min). Here the status of our preclinical development of [11 C] WAY-100635 as a PET radioligand is summarised. On the basis of studies in rats and human volunteers, it is concluded that [11C]WAY-100635 is a promising radioligand for the study of central 5-HT 1A receptors with potential for application to the study of neuropsychiatric disorders and to the human pharmacology of psychoactive drugs.