Estimation of Local Receptor Density, B′max, and Other Parameters via Multiple-Injection Positron Emission Tomography Experiments

2004 ◽  
pp. 184-213 ◽  
Author(s):  
Evan D. Morris ◽  
Bradley T. Christian ◽  
Karmen K. Yoder ◽  
Raymond F. Muzic
Keyword(s):  
Positron Emission Tomography ◽  
Emission Tomography ◽  
Receptor Density ◽  
Multiple Injection ◽  
Positron Emission

scholarly journals Positron Emission Tomography in Cancer Research and Treatment

2002 ◽  
Vol 1 (6) ◽  
pp. 423-439 ◽  
Author(s):  
Mark Mandelkern ◽  
Jonathan Raines
Keyword(s):  
Positron Emission Tomography ◽  
Fdg Pet ◽  
Cellular Proliferation ◽  
Emission Tomography ◽  
Receptor Density ◽  
High Quality ◽  
Cancer Management ◽  
Abnormal Glucose Metabolism ◽  
Positron Emission ◽  
Near Term

Positron emission tomography (PET), the imaging of pharmaceuticals labeled with positronemitting radionuclides, is a rapidly growing modality for the diagnosis and management of cancer. PET yields high-quality images characterizing substrate metabolism, cellular proliferation, receptor density, and other parameters that can be used to identify cancer and evaluate its response to therapies. The technique mainly utilized in cancer management is FDG-PET, which exploits the abnormal glucose metabolism of cancer cells first characterized by Warburg. We discuss the principles of PET, the currently available instrumentation and radiopharmaceuticals, the efficacy of FDG-PET in the management of cancer, and the prospects for near-term advances in cancer using PET.

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.

Central D2 receptor blockade and antipsychotic effects of neuroleptics. Preliminary study with positron emission tomography

1990 ◽  
Vol 5 (4) ◽  
pp. 231-240 ◽  
Author(s):  
JL Martinot ◽  
ML Paillère-Martinot ◽  
C Loc'h ◽  
P Péron Magnan ◽  
B Mazoyer ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Dopamine Receptor ◽  
Negative Symptoms ◽  
Receptor Occupancy ◽  
Emission Tomography ◽  
Receptor Blockade ◽  
Low Doses ◽  
Receptor Density ◽  
Positron Emission ◽  
Significant Difference

SummaryThe striatal D2 receptor density/affinity index was assessed using positron emission tomography and 76Br-Bromolisuride in 15 schizophrenics, first untreated, and afterwards receiving neuroleptics, and in 14 control subjects. The patients received low or conventional doses of neuroleptics. The schizophrenics receiving low doses (n = 6) had preponderant negative symptoms. Mean D2 receptor occupancy was 24 ± 20%. Despite this weak central D2 receptor blockade, a significant decrease in negative symptoms was observed, a result consistent with the hypothesis of a disinhibitory action of some neuroleptics administered in low doses. The patients treated with conventional doses (n = 9) had mixed positive and negative symptoms, and the mean D2 receptor occupancy was 54 ± 13%. Significant decreases in positive symptoms, but also in negative symptoms, were obtained with this treatment. Before treatment, there was no significant difference in the striatal D2 receptor density/affinity index between: 1) patients and controls, 2) negative and mixed schizophrenics, and 3) the subsequent responder and non-responder patients. In addition, the D2 dopamine receptor occupancy by neuroleptics did not significantly differ in responder or nonresponder patients, suggesting that the central D2 dopamine receptor blockade is a necessary, but insufficient condition to account for the antipsychotic effect of neuroleptics.

scholarly journals In vivo evaluation of [11C]preladenant positron emission tomography for quantification of adenosine A2A receptors in the rat brain

2016 ◽  
Vol 37 (2) ◽  
pp. 577-589 ◽  
Author(s):  
Xiaoyun Zhou ◽  
Shivashankar Khanapur ◽  
Johan R de Jong ◽  
Antoon TM Willemsen ◽  
Rudi AJO Dierckx ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Receptor Occupancy ◽  
Compartment Model ◽  
Emission Tomography ◽  
Rat Striatum ◽  
Receptor Density ◽  
Reference Tissue ◽  
Tissue Compartment ◽  
Positron Emission ◽  
The Brain

[11C]Preladenant was developed as a novel adenosine A2A receptor positron emission tomography radioligand. The present study aims to evaluate the suitability of [11C]preladenant positron emission tomography for the quantification of striatal A2A receptor density and the assessment of striatal A2A receptor occupancy by KW-6002. Sixty- or ninety-minute dynamic positron emission tomography imaging was performed on rats. Tracer kinetics was quantified by the two-tissue compartment model, Logan graphical analysis and several reference tissue-based models. Test–retest reproducibility was assessed by repeated imaging on two consecutive days. Two-tissue compartment model and Logan plot estimated comparable distribution volume ( VT) values of ∼10 in the A2A receptor-rich striatum and substantially lower values in all extra-striatal regions (∼1.5–2.5). The simplified reference tissue model with midbrain or occipital cortex as the reference region proved to be the best non-invasive model for quantification of A2A receptor, showing a striatal binding potential ( BPND) value of ∼5.5, and a test–retest variability of ∼5.5%. The brain metabolite analysis showed that at 60-min post injection, 17% of the radioactivity in the brain was due to radioactive metabolites. The ED50 of KW-6002 in rat striatum for i.p. injection was 0.044–0.062 mg/kg. The study demonstrates that [11C]preladenant is a suitable tracer to quantify striatal A2A receptor density and assess A2A receptor occupancy by A2A receptor-targeting molecules.

scholarly journals Insights into schizophrenia using positron emission tomography: building the evidence and refining the focus

2010 ◽  
Vol 197 (1) ◽  
pp. 3-4 ◽  
Author(s):  
Nora S. Vyas ◽  
Neva H. Patel ◽  
Kuldip S. Nijran ◽  
Adil Al-Nahhas ◽  
Basant K. Puri
Keyword(s):  
Positron Emission Tomography ◽  
Cognitive Impairments ◽  
Emission Tomography ◽  
Receptor Density ◽  
Future Directions ◽  
Dopaminergic Transmission ◽  
Positron Emission ◽  
Transmission Studies ◽  
The Brain ◽  
Positron Emissions Tomography

SummarySchizophrenia involves dysregulation in dopaminergic transmission. Studies show heightened presynaptic striatal dopaminergic function and elevated striatal D2/D3 receptor density in the brain. Cognitive impairments result from hypostimulation of D1 receptors and are associated with dysfunction in the prefrontal cortex. Here we discuss relevant positron emissions tomography (PET) studies and provide future directions.

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