A double-injection technique for in vivo measurement of dopamine D2-receptor density in monkeys with 3-(2'-( sup 18 F)fluoroethyl)spiperone and dynamic positron emission tomography

• Published in: Journal of cerebral blood flow and metabolism 1989-12, Vol.9:6
• Main Authors: Huang, S.C., Bahn, M.M., Barrio, J.R., Hoffman, J.M., Satyamurthy, N., Hawkins, R.A., Mazziotta, J.C., Phelps, M.E.
• Format: Article
• Language: English
• Subjects: 550601 - Medicine- Unsealed Radionuclides in Diagnostics; AMINES; AROMATICS; AUTONOMIC NERVOUS SYSTEM AGENTS; BETA DECAY RADIOISOTOPES; BETA-PLUS DECAY RADIOISOTOPES; BIOCHEMICAL REACTION KINETICS; BODY; BRAIN; CARDIOTONICS; CARDIOVASCULAR AGENTS; CENTRAL NERVOUS SYSTEM; COMPUTERIZED TOMOGRAPHY; DIAGNOSTIC TECHNIQUES; DOPAMINE; DRUGS; EMISSION COMPUTED TOMOGRAPHY; FLUORINE 18; FLUORINE ISOTOPES; HOURS LIVING RADIOISOTOPES; HYDROXY COMPOUNDS; INJECTION; INTAKE; INTRAVENOUS INJECTION; ISOMERIC TRANSITION ISOTOPES; ISOTOPES; KINETICS; LIGANDS; LIGHT NUCLEI; MATHEMATICAL MODELS; MEMBRANE PROTEINS; NERVOUS SYSTEM; NEUROREGULATORS; NUCLEI; ODD-ODD NUCLEI; ORGANIC COMPOUNDS; ORGANS; PHENOLS; POLYPHENOLS; POSITRON COMPUTED TOMOGRAPHY; PROTEINS; RADIOISOTOPES; RADIOLOGY AND NUCLEAR MEDICINE; REACTION KINETICS; RECEPTORS; SYMPATHOMIMETICS; TOMOGRAPHY
• ISSN: 0271-678X; 1559-7016
• DOI: 10.1038/jcbfm.1989.119

Dopamine D2-receptor density in striatum of monkey was measured with 3-(2'-({sup 18}F)fluoroethyl)spiperone (FESP) and dynamic positron emission tomography (PET), using a double-injection technique. A first bolus of high specific activity (SA) FESP (5 mCi; approximately equal to 1 Ci/mumol) was injected i.v.; 90 min later, a second bolus of lower SA FESP (5 mCi; approximately equal to 0.04 Ci/mumol) was injected. A dynamic PET study was performed to measure the kinetics of FESP in striatum over 180 min, and the metabolite-corrected concentration of FESP in plasma as a function of time was obtained from arterial blood samples. A nonlinear compartmental model that took into account the saturability of the receptor binding was used to describe the kinetics of FESP in striatum. Model parameters were estimated by regression with a constraint based on information about the equilibrium dissociation constant of the ligand-receptor binding. Dopamine D2-receptor density in striatum was estimated to be 25.9 +/- 12.7 pmol/g in seven Macaca nemestrina monkeys. The method does not require the use of cerebellum as a reference tissue region and an estimate of dopamine D2-receptor density can be obtained from a single study.