Synthesis of [3H]muscimol
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F25%3A00638328" target="_blank" >RIV/61388963:_____/25:00638328 - isvavai.cz</a>
Result on the web
<a href="https://doi.org/10.1002/jlcr.4159" target="_blank" >https://doi.org/10.1002/jlcr.4159</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1002/jlcr.4159" target="_blank" >10.1002/jlcr.4159</a>
Alternative languages
Result language
angličtina
Original language name
Synthesis of [3H]muscimol
Original language description
Muscimol, a potent GABAA receptor agonist and psychoactive alkaloid found in Amanita mushrooms, is widely used as a tool compound in neurochemical research. Despite its importance, synthetic access to [3H]muscimol of high specific activity has remained limited due to the challenges associated with conventional labeling strategies. Herein, we report a novel synthetic approach for the preparation of [3H]muscimol based on the reduction of a suitably protected amide precursor using in situ generated tritioborane (BT3·THF). The precursor was synthesized in four steps from dimethyl acetylenedicarboxylate, and subsequent electrophilic reduction afforded [3H]benzyl-protected muscimol in a radiochemical yield of 44 mCi (1.63 GBq) and a molar activity of 48.3 Ci/mmol (1.79 TBq/mmol). Final deprotection with HBr in acetic acid yielded [3H]muscimol·HBr in > 95% radiochemical purity. The method avoids the use of bulk tritiated water employed in established synthetic protocols and enables safe, reliable, and efficient access to this valuable radioligand for applications in GABA receptor studies.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10406 - Analytical chemistry
Result continuities
Project
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2025
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Journal of Labelled Compounds and Radiopharmaceuticals
ISSN
0362-4803
e-ISSN
1099-1344
Volume of the periodical
68
Issue of the periodical within the volume
9/10
Country of publishing house
US - UNITED STATES
Number of pages
8
Pages from-to
e4159
UT code for WoS article
001555222200009
EID of the result in the Scopus database
2-s2.0-105012930714