(3-N-[C-11]METHYL)SPIPERONE, A LIGAND-BINDING TO DOPAMINE-RECEPTORS - RADIOCHEMICAL SYNTHESIS AND BIODISTRIBUTION STUDIES IN MICE

  • 1 January 1984
    • journal article
    • research article
    • Vol. 25  (11) , 1222-1227
Abstract
11C-labeled 3-N-methylspiperone, a positron-emitting dopamine-receptor antagonist with potential for use in positron emission tomography studies of human neurotransmitter receptors, was synthesized from 11CO2 in 40 min, with a radiochemical yield of .apprx. 20-40%. The specific activity of the (3-N-[11C]methyl)spiperone was determined by UV spectroscopy to be .apprx. 270 mCi/.mu.mol at the end of synthesis. In in vitro binding experiments, the Ki for 3-N-methylspiperone was .apprx. 250 pM (against H-3 spiperone). The brain-to-blood ratios in normal ICR mice were 2.8 or greater at the times studied, and the striatum-to-cerebellum ratio at 60 min after injection was 20:1.