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Synthesis and Precl...
Synthesis and Preclinical Evaluation of 6-[18F]Fluorine-α-methyl-l-tryptophan, a Novel PET Tracer for Measuring Tryptophan Uptake
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Krasikova, Raisa (author)
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- Kondrashov, Mikhail (author)
- Karolinska Institutet
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Avagliano, Camilla (author)
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Petukhov, Mikhail (author)
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Vazquez-Romero, Ana (author)
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Revunov, Evgeny (author)
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Johnström, Peter (author)
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Tari, Lenke (author)
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- Tóth, Miklós (author)
- Karolinska Institutet
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Häggkvist, Jenny (author)
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- Erhardt, Sophie (author)
- Karolinska Institutet
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- Cervenka, Simon (author)
- Karolinska Institutet
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- Schou, Magnus (author)
- Karolinska Institutet
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(creator_code:org_t)
- 2020-04-28
- 2020
- English.
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In: ACS Chemical Neuroscience. - : American Chemical Society (ACS). - 1948-7193. ; 11:12, s. 1756-1761
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- The positron emission tomography (PET) radioligand α-[11C]methyl-l-tryptophan ([11C]AMT) has been used to assess tryptophan metabolism in cancer, epilepsy, migraine, and autism. Despite its extensive application, the utility of this tracer is currently hampered by the short half-life of the radionuclide used for its labeling (11C, t1/2 = 20.4 min). We herein report the design, synthesis, radiolabeling, and initial in vivo evaluation of a fluorine-18 (18F, t 1/2 = 109.7 min) labeled analogue that is fluorinated in the 6-position of the aromatic ring ([18F]6-F-AMTr). In a head-to-head comparison between [18F]6-F-AMTr and [11C]AMT in mice using PET, peak brain radioactivity, regional brain distribution, and kinetic profiles were similar between the two tracers. [18F]6-F-AMTr was however not a substrate for IDO1 or TPH as determined in in vitro enzymatic assays. The brain uptake of the tracer is thus more likely related to LAT1 transport over the blood-brain barrier than metabolism along the serotonin or kynurenine pathways.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Neurovetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Neurosciences (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Radiologi och bildbehandling (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Radiology, Nuclear Medicine and Medical Imaging (hsv//eng)
Keyword
- Brain
- Fluorine-18
- Kynurenine
- LAT1
- PET
- Tryptophan
Publication and Content Type
- ref (subject category)
- art (subject category)
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- By the author/editor
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Krasikova, Raisa
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Kondrashov, Mikh ...
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Avagliano, Camil ...
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Petukhov, Mikhai ...
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Vazquez-Romero, ...
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Revunov, Evgeny
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show more...
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Johnström, Peter
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Tari, Lenke
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Tóth, Miklós
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Häggkvist, Jenny
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Erhardt, Sophie
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Cervenka, Simon
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Schou, Magnus
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show less...
- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Neurosciences
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Clinical Medicin ...
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and Radiology Nuclea ...
- Articles in the publication
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ACS Chemical Neu ...
- By the university
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Uppsala University
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Karolinska Institutet