Imaging Dopamine Receptors in the Human Brain by Positron Tomography

Wagner, H. N.; Burns, H. Donald; Dannals, R. F.; Wong, Dean F.; Långström, Bengt; Duelfer, Timothy; Frost, J. James; Ravert, Hayden T.; Links, Jonathan M.; Rosenbloom, Sarah; Lukas, Scott E.; Kramer, Alfred V.; Kuhar, Michael J.

doi:10.1097/00004728-198402000-00055

Cited by 85 publications

(107 citation statements)

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“…[14][15][16] Moreover, alternative positron-emitting ligands such as [11C]raclopride [27][28][29] and [11C]N-methylspiperone 30 should also be useful probes for PET detection of the D 2 R reporter gene, and [123I]iodobenzamine 31 should be useful for analyzing the D 2 R reporter gene by SPECT.…”

Section: U Of Ad-d 2 R Virus Two Days Later Mouse B Was Injected Imentioning

confidence: 99%

Repetitive, non-invasive imaging of the dopamine D2 receptor as a reporter gene in living animals

MacLaren¹,

Gambhir

Satyamurthy³

et al. 1999

Gene Ther

332

164

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Section: U Of Ad-d 2 R Virus Two Days Later Mouse B Was Injected Imentioning

confidence: 99%

Repetitive, non-invasive imaging of the dopamine D2 receptor as a reporter gene in living animals

MacLaren¹,

Gambhir

Satyamurthy³

et al. 1999

Gene Ther

332

164

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“…For example, when k4 = 0, the tissue kinetics on a normalized graphical will approach a straight line with a slope of klk3/(k2 + k3) and an intercept at the y-axis of klk2/(k2 + k3) 2 . Therefore, the normalized graphical plot is a very simple way to show whether k4 is negligible or not, and, if it is negli gible, to show the magnitude of klk3/(k2 + k3)' For example, the linearity of the striatum-to-cere bellum ratio for 3-N-[11C]methylspiperone first ob served by Wagner et al (1983) and Wong et al (1984) indicates that k4 is small for the tracer. The individual values of the transport rate constants kl and k2' however, are not directly provided by the normalized graphical plot.…”

Section: Dynamic Approachmentioning

confidence: 99%

Neuroreceptor Assay with Positron Emission Tomography: Equilibrium versus Dynamic Approaches

Huang

Barrio

Phelps

1986

J Cereb Blood Flow Metab

148

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Section: Proof-of-concept In Humansmentioning

confidence: 99%

“…For [224,225] . Since these early studies, the cerebellum has often been used as suitable reference region for the development of PET radiotracers for other dopamine receptors [226] , serotonin 5-HT 1A and 5-HT 2 receptors [227,228] , muscarinic and nicotinic ACh receptors [229][230][231] , histamine receptors [232] , and the serotonin transporter [188,233] .…”

Section: Proof Of Target-specifi C Binding In Animalsmentioning

confidence: 99%

“…For example, in the case of the α4β2 nAChR radiotracer (-)-[ 18 F]flubatine, the time between the first report on radiosynthesis [164] and the fi rst report on human use [16] years [210,272] , and for [ 18 F]FEOBV [126] , a radiotracer for the VAChT, it has been almost 20 years [273] . At the beginning of neuroreceptor imaging with PET this transition time was much shorter, in the range of 1-2 years as exemplifi ed by [ 11 C]raclopride [225,274] , 3-N-[ 11 C]methylspiperone [224] , and [ 11 C]fl umazenil [49,275] .However, even if a radiotracer is not further developed into a radiopharmaceutical for imaging in human subjects it may fi nd widespread use in preclinical studies with special animal PET devices [276] to investigate animal models of diseases [7] or new drugs [8,252] . The foremost importance of this approach is the diagnosis and therapeutic monitoring of brain diseases.…”

mentioning

confidence: 99%

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Development of 18F-labeled radiotracers for neuroreceptor imaging with positron emission tomography

2014

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Positron emission tomography (PET) is an in vivo molecular imaging tool which is widely used in nuclear medicine for early diagnosis and treatment follow-up of many brain diseases. PET uses biomolecules as probes which are labeled with radionuclides of short half-lives, synthesized prior to the imaging studies. These probes are called radiotracers. Fluorine-18 is a radionuclide routinely used in the radiolabeling of neuroreceptor ligands for PET because of its favorable half-life of 109.8 min. The delivery of such radiotracers into the brain provides images of transport, metabolic, and neurotransmission processes on the molecular level. After a short introduction into the principles of PET, this review mainly focuses on the strategy of radiotracer development bridging from basic science to biomedical application. Successful radiotracer design as described here provides molecular probes which not only are useful for imaging of human brain diseases, but also allow molecular neuroreceptor imaging studies in various small-animal models of disease, including geneticallyengineered animals. Furthermore, they provide a powerful tool for in vivo pharmacology during the process of pre-clinical drug development to identify new drug targets, to investigate pathophysiology, to discover potential drug candidates, and to evaluate the pharmacokinetics and pharmacodynamics of drugs in vivo.Keywords: Alzheimer's disease; autoradiography; blood-brain barrier; brain tumor; cholinergic system; kinetic modeling; metabolism; molecular imaging; neurodegeneration; positron emission tomography; precursor; psychiatric disorder; radiotracer; sigma receptor ·Review· IntroductionPositron emission tomography (PET) is an in vivo molecular imaging tool widely used in nuclear medicine for early diagnosis and treatment follow-up of many brain diseases. Positron-emitting radionuclide-labeled substances allow the visualization, characterization, and measurement of biological processes at the molecular and cellular levels in humans and other living systems by highly sensitive coincidence-detection [1] . This is based on 511 keV photons (gamma radiation) originating from positronelectron annihilation. PET differs in that aspect from other modalities such as single-photon emission computed tomography (SPECT), magnetic resonance imaging (MRI), optical imaging, and ultrasound. Because of their high sensitivity (~10 -9 to 10 -12 M) PET and SPECT offer advantages over the other methods. Therefore, in the past, they were the only modalities that allowed noninvasive imaging of biochemical receptor sites. Nowadays, the other imaging modalities compete in that aspect although precise absolute quantitation in terms of biochemical parameters has not been achieved yet. fusion accuracy, provides an advanced diagnostic tool and research platform [2,3] .PET and SPECT use biomolecules as probes, labeled with radionuclides of short half-lives, synthesized prior to the imaging studies. These probes are called radiotracers. According to the concept developed by George ...

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Imaging Dopamine Receptors in the Human Brain by Positron Tomography

Cited by 85 publications

References 0 publications

Repetitive, non-invasive imaging of the dopamine D2 receptor as a reporter gene in living animals

Repetitive, non-invasive imaging of the dopamine D2 receptor as a reporter gene in living animals

Neuroreceptor Assay with Positron Emission Tomography: Equilibrium versus Dynamic Approaches

Development of 18F-labeled radiotracers for neuroreceptor imaging with positron emission tomography

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