Radiolabeled HOCPCA as a highly useful tool in drug discovery and pharmacology
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F21%3A00541447" target="_blank" >RIV/61388963:_____/21:00541447 - isvavai.cz</a>
Result on the web
<a href="https://doi.org/10.1002/jlcr.3870" target="_blank" >https://doi.org/10.1002/jlcr.3870</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1002/jlcr.3870" target="_blank" >10.1002/jlcr.3870</a>
Alternative languages
Result language
angličtina
Original language name
Radiolabeled HOCPCA as a highly useful tool in drug discovery and pharmacology
Original language description
GHB (γ‐hydroxybutyrate) is not only an endogenously present small molecule but also a clinically prescribed drug for the symptomatic treatment of narcolepsy. However, GHB's mechanism of action remains to be uncovered. Within the CNS, GHB targets both GABAB receptors and a pharmacologically distinct population of high‐affinity binding sites with unknown molecular identity. HOCPCA (3‐hydroxycyclopent‐1‐enecarboxylic acid) is a structural analog of GHB selectively targeting GHB high‐affinity binding sites. Here, we discuss the usefulness of 3H‐ and 11C‐labeled HOCPCA as radioligands for selectively probing GHB high‐affinity binding sites and their application in drug discovery. As such, [3H]HOCPCA's exceptional affinity and selectivity makes it an indispensable tool in drug discovery, and its utility has been demonstrated in, for example, homogenate binding studies, in vitro as well as ex vivo autoradiography. Moreover, the successful synthesis of [11C]HOCPCA is a starting point for further ligand development for future in vivo investigations of GHB high‐affinity binding sites.
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
2021
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
64
Issue of the periodical within the volume
2
Country of publishing house
GB - UNITED KINGDOM
Number of pages
5
Pages from-to
77-81
UT code for WoS article
000551481700001
EID of the result in the Scopus database
2-s2.0-85088402815