Evidence for the Existence of a Specific G Protein-Coupled Receptor Activated by Guanosine

Authors

  • Prof. Rosaria Volpini,

    1. School of Pharmacy, Medicinal Chemistry Unit, University of Camerino via S. Agostino 1, 62032 Camerino (MC) (Italy), Fax: (+39) 0737 402295
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    • These authors contributed equally to this work.

  • Prof. Gabriella Marucci,

    1. School of Pharmacy, Medicinal Chemistry Unit, University of Camerino via S. Agostino 1, 62032 Camerino (MC) (Italy), Fax: (+39) 0737 402295
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    • These authors contributed equally to this work.

  • Dr. Michela Buccioni,

    1. School of Pharmacy, Medicinal Chemistry Unit, University of Camerino via S. Agostino 1, 62032 Camerino (MC) (Italy), Fax: (+39) 0737 402295
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  • Dr. Diego Dal Ben,

    1. School of Pharmacy, Medicinal Chemistry Unit, University of Camerino via S. Agostino 1, 62032 Camerino (MC) (Italy), Fax: (+39) 0737 402295
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  • Dr. Catia Lambertucci,

    1. School of Pharmacy, Medicinal Chemistry Unit, University of Camerino via S. Agostino 1, 62032 Camerino (MC) (Italy), Fax: (+39) 0737 402295
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  • Dr. Carmen Lammi,

    1. School of Pharmacy, Medicinal Chemistry Unit, University of Camerino via S. Agostino 1, 62032 Camerino (MC) (Italy), Fax: (+39) 0737 402295
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  • Dr. Ram C. Mishra,

    1. Biology Department, Georgia State University, 100 Piedmont Avenue SE, Atlanta, GA 30303 (USA)
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  • Ajiroghene Thomas,

    1. School of Pharmacy, Medicinal Chemistry Unit, University of Camerino via S. Agostino 1, 62032 Camerino (MC) (Italy), Fax: (+39) 0737 402295
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  • Prof. Gloria Cristalli

    Corresponding author
    1. School of Pharmacy, Medicinal Chemistry Unit, University of Camerino via S. Agostino 1, 62032 Camerino (MC) (Italy), Fax: (+39) 0737 402295
    • School of Pharmacy, Medicinal Chemistry Unit, University of Camerino via S. Agostino 1, 62032 Camerino (MC) (Italy), Fax: (+39) 0737 402295
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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.

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