Estimation of Baseline Dopamine D2 Receptor Occupancy in Striatum and Extrastriatal Regions in Humans with Positron Emission Tomography with [18F] Fallypride

2008 ◽  
Vol 63 (2) ◽  
pp. 241-244 ◽  
Author(s):  
Patrizia Riccardi ◽  
Ron Baldwin ◽  
Ronald Salomon ◽  
Sharlet Anderson ◽  
Mohammad S. Ansari ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Receptor Occupancy ◽  
Emission Tomography ◽  
Dopamine D2 ◽  
Dopamine D2 Receptor Occupancy ◽  
Positron Emission

A Double-Injection Technique for in vivo Measurement of Dopamine D2-Receptor Density in Monkeys with 3-(2'-[18F] Fluoroethyl)Spiperone and Dynamic Positron Emission Tomography

1989 ◽  
Vol 9 (6) ◽  
pp. 850-858 ◽  
Author(s):  
Sung-Cheng Huang ◽  
Mark M. Bahn ◽  
Jorge R. Barrio ◽  
John M. Hoffman ◽  
Nagichettiar Satyamurthy ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Receptor Binding ◽  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Emission Tomography ◽  
Injection Technique ◽  
Receptor Density ◽  
Dopamine D2 ◽  
Positron Emission ◽  
Kinetics Of

Dopamine D2-receptor density in striatum of monkey was measured with 3-(2'-[18F]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; ≃ 1 Ci/μmol) was injected i.v.; 90 min later, a second bolus of lower SA FESP (5 mCi; ≃ 0.04 Ci/μmol) 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.

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