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Evidence for the Existence of a Specific G Protein‐Coupled Receptor Activated by Guanosine
Author(s) -
Volpini Rosaria,
Marucci Gabriella,
Buccioni Michela,
Dal Ben Diego,
Lambertucci Catia,
Lammi Carmen,
Mishra Ram C.,
Thomas Ajiroghene,
Cristalli Gloria
Publication year - 2011
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201100100
Subject(s) - guanosine , chemistry , biochemistry , neuroprotection , receptor , g protein coupled receptor , adenosine , g protein , adenosine receptor , purine , microbiology and biotechnology , biology , pharmacology , agonist , enzyme
Guanosine, released extracellularly from neurons and glial cells, plays important roles in the central nervous system, including neuroprotection. The innovative DELFIA Eu‐GTP binding assay was optimized for characterization of the putative guanosine receptor binding site at rat brain membranes by using a series of novel and known guanosine derivatives. These nucleosides were prepared by modifying the purine and sugar moieties of guanosine at the 6‐ and 5′‐positions, respectively. Results of these experiments prove that guanosine, 6‐thioguanosine, and their derivatives activate a G protein‐coupled receptor that is different from the well‐characterized adenosine receptors.