(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 journalArticle

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.

LanguageEnglish (US)
Pages1222-1227
Number of pages6
JournalJournal of Nuclear Medicine
Volume25
Issue number11
StatePublished - 1984

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Spiperone
Dopamine Receptors
Ligands
Inbred ICR Mouse
Neurotransmitter Receptor
Dopamine Antagonists
Carbon Monoxide
Positron-Emission Tomography
Cerebellum
Spectrum Analysis
Carbon
Electrons
Injections
Brain
3-N-methylspiperone
In Vitro Techniques

ASJC Scopus subject areas

  • Radiological and Ultrasound Technology

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(3-N-[11C]methyl)spiperone, a ligand binding to dopamine receptors : Radiochemical synthesis and biodistribution studies in mice. / Burns, H. D.; Dannals, R. F.; Langstrom, B.

In: Journal of Nuclear Medicine, Vol. 25, No. 11, 1984, p. 1222-1227.

Research output: Contribution to journalArticle

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