New Synthesis and Tritium Labeling of a Selective Ligand for Studying High-Affinity gamma-Hydroxybutyrate (GHB) Binding Sites
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F13%3A00421055" target="_blank" >RIV/61388963:_____/13:00421055 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1021/jm4011719" target="_blank" >http://dx.doi.org/10.1021/jm4011719</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1021/jm4011719" target="_blank" >10.1021/jm4011719</a>
Alternative languages
Result language
angličtina
Original language name
New Synthesis and Tritium Labeling of a Selective Ligand for Studying High-Affinity gamma-Hydroxybutyrate (GHB) Binding Sites
Original language description
3-Hydroxycyclopent-1-enecarboxylic acid (HOCPCA, 1) is a potent ligand for the high-affinity GHB binding sites in the CNS. An improved synthesis of 1 together with a very efficient synthesis of [H-3]-1 is described. The radiosynthesis employs in situ generated lithium trimethoxyborotritide. Screening of 1 against different CNS targets establishes a high selectivity, and we demonstrate in vivo brain penetration. In vitro characterization of [H-3]-1 binding shows high specificity to the high-affinity GHBbinding sites.
Czech name
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Czech description
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Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CC - Organic chemistry
OECD FORD branch
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Result continuities
Project
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2013
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 Medicinal Chemistry
ISSN
0022-2623
e-ISSN
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Volume of the periodical
56
Issue of the periodical within the volume
20
Country of publishing house
US - UNITED STATES
Number of pages
5
Pages from-to
8201-8205
UT code for WoS article
000326259900041
EID of the result in the Scopus database
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