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

Journal Article · Fri Dec 01 04:00:00 EST 1989 · Journal of Cerebral Blood Flow and Metabolism; (USA)

DOI:https://doi.org/10.1038/jcbfm.1989.119· OSTI ID:7165130

Huang, S C; Bahn, M M; Barrio, J R; Hoffman, J M; Satyamurthy, N; Hawkins, R A; Mazziotta, J C; Phelps, M E ^[1]

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1. UCLA School of Medicine (USA)

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.

• OSTI ID: 7165130
• Journal Information: Journal of Cerebral Blood Flow and Metabolism; (USA), Journal Name: Journal of Cerebral Blood Flow and Metabolism; (USA) Vol. 9:6; ISSN 0271-678X; ISSN JCBMD
• Country of Publication: United States
• Language: English

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AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
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KINETICS
LIGANDS
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MATHEMATICAL MODELS
MEMBRANE PROTEINS
NERVOUS SYSTEM
NEUROREGULATORS
NUCLEI
ODD-ODD NUCLEI
ORGANIC COMPOUNDS
ORGANS
PHENOLS
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RECEPTORS
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