Article ; Online: Radiosynthesis of (R,S)-[
2019 Volume 14, Issue 9, Page(s) 982–993
Abstract: ... with a low-affinity binder/high-affinity binder (LAB/HAB) ratio similar (1.2 vs. 1.3) to that of (R)-[ ...
Abstract | Translocator protein (TSPO) is a biomarker of neuroinflammation, which is a hallmark of many neurodegenerative diseases and has been exploited as a positron emission tomography (PET) target. Carbon-11-labelled PK11195 remains the most applied agent for imaging TSPO, despite its short-lived isotope and low brain permeability. Second-generation radiotracers show variance in affinity amongst subjects (low-, mixed-, and high-affinity binders) caused by the genetic polymorphism (rs6971) of the TSPO gene. To overcome these limitations, a new structural scaffold was explored based on the TSPO pharmacophore, and the analogue with a low-affinity binder/high-affinity binder (LAB/HAB) ratio similar (1.2 vs. 1.3) to that of (R)-[ |
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MeSH term(s) | Animals ; Fluorine Radioisotopes/chemistry ; Humans ; Polymorphism, Genetic ; Positron-Emission Tomography ; Proof of Concept Study ; Protein Binding ; Radiopharmaceuticals/chemical synthesis ; Rats ; Receptors, GABA/chemistry ; Receptors, GABA/metabolism ; Stereoisomerism |
Chemical Substances | Fluorine Radioisotopes ; Radiopharmaceuticals ; Receptors, GABA ; TSPO protein, human |
Language | English |
Publishing date | 2019-04-08 |
Publishing country | Germany |
Document type | Journal Article ; Research Support, Non-U.S. Gov't |
ZDB-ID | 2218496-X |
ISSN | 1860-7187 ; 1860-7179 |
ISSN (online) | 1860-7187 |
ISSN | 1860-7179 |
DOI | 10.1002/cmdc.201900023 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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