title: Evidence for the existence of a specific g protein-coupled receptor activated by guanosine.
abstract: 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.
authors.affiliation: School of Pharmacy, Medicinal Chemistry Unit, University of Camerino via S. Agostino 1, 62032 Camerino, Italy.
authors.forename: Rosaria
authors.initials: R
authors.lastname: Volpini
authors.forename: Gabriella
authors.initials: G
authors.lastname: Marucci
authors.forename: Michela
authors.initials: M
authors.lastname: Buccioni
authors.forename: Diego
authors.initials: D
authors.lastname: Dal Ben
authors.forename: Catia
authors.initials: C
authors.lastname: Lambertucci
authors.forename: Carmen
authors.initials: C
authors.lastname: Lammi
authors.forename: Ram C
authors.initials: RC
authors.lastname: Mishra
authors.forename: Ajiroghene
authors.initials: A
authors.lastname: Thomas
authors.forename: Gloria
authors.initials: G
authors.lastname: Cristalli
mesh_terms: D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000378:metabolism; D002462:Cell Membrane / Q000378:metabolism; D006151:Guanosine / Q000031:analogs & derivatives* / Q000378:metabolism*; D006160:Guanosine Triphosphate / Q000378:metabolism; D011485:Protein Binding; D051381:Rats; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*
chemical_list: D043562:Receptors, G-Protein-Coupled; D006151:Guanosine; D006160:Guanosine Triphosphate