Special Problems Associated with the Synthesis of High Specific Activity Carbon-11 Labeled Radiotracers

Dannals, Robert F.; Ravert, Hayden T.; Wilson, Alan A.; Wagner, Henry N.

doi:10.1007/978-1-4899-0626-7_5

Cited by 4 publications

(2 citation statements)

References 11 publications

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“…Methods for improving the specific radioactivity in the preparation of 11 C-radiotracers are well documented [151,152]. However, although many PET facilities produce 18 F- radiotracers with high SA, the details of such production have not been discussed.…”

Section: B Production Of 18 F-radiotracers With Very High Sa For Imamentioning

confidence: 99%

The Quest for Eldorado: Development of Radioligands for In Vivo Imaging of Nicotinic Acetylcholine Receptors in Human Brain

Horti¹,

Villemagne²

2006

CPD

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Neuronal nicotinic acetylcholine receptors (nAChRs), ubiquitously distributed in the human brain, are implicated in various neurophysiological processes and in the pathophysiology and/or treatment strategies of Alzheimer's and Parkinson's diseases, Tourette's syndrome, epilepsy, schizophrenia, depression, and anxiety, as well as being particularly affected in tobacco dependence/withdrawal. In the past two decades, researchers have developed an extensive series of radioligands for the assessment of nAChRs in vivo through emission tomography, PET and SPECT. Several radioligands, derivatives of A-85380: 2-[(18)F]FA, 6-[(18)F]FA and 5-[(123)I]IA, are now being employed for the evaluation of nAChR in humans with PET and SPECT. Displaying better imaging properties than (11)C-nicotine and a better toxicity profile than epibatidine analogs, they have allowed quantification of thalamic nAChR in the human brain. Nevertheless, A-85380 derivatives still exhibit slow brain kinetics and a moderate signal-to-noise ratio. Current research efforts on the part of PET/SPECT radiochemists, therefore, have focused on development of new, highly specific and highly selective nAChR radioligands with improved brain kinetics that are able to localize high-affinity nAChRs in vivo. Key examples of new PET/SPECT ligands that are derived from several different structural classes are discussed along with a review of their chemical as well as their in vitro and/or in vivo properties. In particular, new PET nAChR radioligands will be examined that either present faster brain kinetics allowing simple and reliable quantification approaches or higher binding potentials suitable for the evaluation of extrathalamic nAChR.

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Section: B Production Of 18 F-radiotracers With Very High Sa For Imamentioning

confidence: 99%

The Quest for Eldorado: Development of Radioligands for In Vivo Imaging of Nicotinic Acetylcholine Receptors in Human Brain

Horti¹,

Villemagne²

2006

CPD

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“…The high specific radioactivity of PET radiotracers for neuroreceptors is a general requirement because of the concerns about the binding competition between the [ 18 F] radiotracer and its natural non-radioactive [ 19 F] isotopomer (carrier), which is always present in the radiolabeled product [63]. For reliable quantification analysis and also due to the safety concerns, a dose of PET radiotracer should occupy less than 5% of the available binding sites.…”

Section: Development Of [18f]asem[48 59]mentioning

confidence: 99%

Development of [ 18 F]ASEM, a specific radiotracer for quantification of the α7-nAChR with positron-emission tomography

Horti¹

2015

Biochemical Pharmacology

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The alpha-7 subtype of the nicotinic acetylcholine receptor (α7-nAChR) is fundamental to physiology; it mediates various brain functions and represents an important target for drug discovery. Exploration of the brain nicotinic acetylcholine receptors (nAChRs) using positron-emission tomography (PET) will make it possible to better understand the important role of this receptor and to study its involvement in schizophrenia, bipolar disorder, Alzheimer's and Parkinson's diseases, drug dependence, inflammation and many other disorders and simplify the development of nicotinic drugs for treatment of these disorders. Until recently, PET imaging of α7-nAChRs has been impeded by the absence of good radiotracers. This review describes various endeavors to develop α7-nAChR PET tracers by several research groups including the author’s group. Most initial PET tracers for imaging α7-nAChRs did not exhibit suitable imaging properties due to their low specific binding. Recently discovered [18F]ASEM is the first highly specific α7-nAChR radioligand and it was recently translated to human PET imaging.

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Mild synthesis of [N-methyl-11C]-isovaleroyl-(l)-carnitine. The usefulness of a tritium approach

Angelini¹,

Carnevaletti²,

Margonelli³

et al. 1999

Applied Radiation and Isotopes

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Special Problems Associated with the Synthesis of High Specific Activity Carbon-11 Labeled Radiotracers

Cited by 4 publications

References 11 publications

The Quest for Eldorado: Development of Radioligands for In Vivo Imaging of Nicotinic Acetylcholine Receptors in Human Brain

The Quest for Eldorado: Development of Radioligands for In Vivo Imaging of Nicotinic Acetylcholine Receptors in Human Brain

Development of [ 18 F]ASEM, a specific radiotracer for quantification of the α7-nAChR with positron-emission tomography

Mild synthesis of [N-methyl-11C]-isovaleroyl-(l)-carnitine. The usefulness of a tritium approach

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