(3-N-[11C]methyl)spiperone, a ligand binding to dopamine receptors: Radiochemical synthesis and biodistribution studies in mice

H. D. Burns, R. F. Dannals, B. Langstrom

Research output: Contribution to journalArticlepeer-review

Abstract

Carbon-11-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 ~20-40%. The specific activity of the (3-N-[11C]methyl)-spiperone was determined by ultraviolet spectroscopy to be approximately 270 mCi/μmol at the end of synthesis. In in vitro binding experiments, the K(i) for 3-N-methylspiperone was found to be approximately 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.

Original languageEnglish (US)
Pages (from-to)1222-1227
Number of pages6
JournalJournal of Nuclear Medicine
Volume25
Issue number11
StatePublished - 1984

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

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