Assessment of α7 nicotinic acetylcholine receptor availability in juvenile pig brain with [18F]NS10743

Deuther‐Conrad, Winnie; Fischer, Steffen; Hiller, Achim; Becker, Georg; Cumming, Paul; Xiong, Guoming; Funke, Uta; Sabri, Osama; Peters, Dan; Brust, Peter

doi:10.1007/s00259-011-1808-y

Cited by 36 publications

(24 citation statements)

References 34 publications

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“…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] . An example of ex vivo autoradiography of SERT distribution in rat brain where the radiotracer striatum, and substantia nigra [187,234] clearly showed the highest radiotracer accumulation, providing evidence for radiotracer selectivity [188] .…”

Section: Proof Of Target-specifi C Binding In Animalsmentioning

confidence: 99%

“…For the two-tissue compartmental model, the slope of the regression line in the Logan plot represents the total distribution volume V T , defi ned by K 1 /k 2 (1+k 3 /k 4 ) + fbv (fbv = fractional blood volume in the target region, k 3 /k 4 = BP [267] ). juvenile pig [230] . Newer developments include proposals to obtain parametric images even in cases without either an arterial input function or a reference region [268] , direct reconstruction algorithms of linear and nonlinear parametric images, and joint estimation of parametric images and input function [263] .…”

Section: Estimation Of Receptor-binding Parameters In Animalsmentioning

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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Section: Proof Of Target-specifi C Binding In Animalsmentioning

confidence: 99%

Section: Estimation Of Receptor-binding Parameters In Animalsmentioning

confidence: 99%

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

2014

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“…As illustrated by the data in Tab. 2, the general suitability of these derivatives for imaging of 7 nAChR is supported by preclinical PET studies in pigs (Deuther-Conrad et al, 2011;Lehel et al, 2009) and nonhuman primates (Hashimoto et al, 2008) as well as a first clinical study (Toyohara et al, 2009). However, substantial enhancement in the affinity of the 7 nAChR PET ligands is required to improve image analysis, modelling, and eventually quantification of 7 nAChR in brain diseases.…”

Section: Fig 2 Lead Structures For Development Of Radioligands For mentioning

confidence: 99%

Molecular Imaging of 7 Nicotinic Acetylcholine Receptors In Vivo: Current Status and Perspectives

Brust¹,

Deuther‐Conrad²

2012

Neuroimaging - Clinical Applications

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“…As illustrated by the data in Tab. 2, the general suitability of these derivatives for imaging of α7 nAChR is supported by preclinical PET studies in pigs (Deuther-Conrad et al, 2011;Lehel et al, 2009) and nonhuman primates (Hashimoto et al, 2008) as well as a first clinical study (Toyohara et al, 2009). However, substantial enhancement in the affinity of the α7 nAChR PET ligands is required to improve image analysis, modelling, and eventually quantification of α7 nAChR in brain diseases.…”

Section: Noninvasive Imaging Of 7 Receptors In Normal and Diseased Bmentioning

confidence: 99%

Neuroimaging - Clinical Applications

Bright¹

2012

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Assessment of α7 nicotinic acetylcholine receptor availability in juvenile pig brain with [18F]NS10743

Abstract: This study confirms the potential of [(18)F]NS10743 as a target-specific radiotracer for the molecular imaging of central α7 nAChRs by PET.

Cited by 36 publications

References 34 publications

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

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

Molecular Imaging of 7 Nicotinic Acetylcholine Receptors In Vivo: Current Status and Perspectives

Neuroimaging - Clinical Applications

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