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Online ISSN: 1860-7187
April 19, 2011
VIP: Evidence for the Existence of a Specific G-Protein-Coupled Receptor Activated by Guanosine
Rosaria Volpini, Gabriella Marucci, Michela Buccioni, Diego Dal Ben, Catia Lambertucci, Carmen Lammi, Ram C. Mishra, Ajiroghene Thomas, and Gloria Cristalli*
Guanosine, released extracellularly from neurons and glial cells, plays important roles in the central nervous system, including neuroprotection. A binding site for guanosine, different from the well-known adenosine receptors, was detected on rat brain membranes, and it could be the target for innovative treatment of neurodegeneration. In this work, Gloria Cristalli and co-workers at the School of Pharmacy of the University of Camerino (Italy) optimized an innovative assay and synthesized a series of guanosine analogues for the characterization of this putative guanosine binding site at rat brain membranes.
Results of their experiments demonstrate that guanosine derivatives (but not adenosine analogues) activate this receptor with varying potency and, in some cases, at very low concentrations. Hence, these compounds could be useful tools for further characterization of the putative guanosine receptor and for an improved understanding of its role in ischemic and neurodegenerative pathways. Moreover, they could represent lead compounds for the development of new drugs for the treatment of neurodegenerative diseases.
Received February 17, 2011; published online April 15, 2011, DOI: 10.1002/cmdc.201100100.