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Minerva Biotecnologica 2004 June;16(2):101-8

Copyright © 2004 EDIZIONI MINERVA MEDICA

language: English

Binding and functional characterization of A3 adenosine receptors in human neutrophils exposed to electromagnetic fields

Varani K. 1, Gessi S. 1, Merighi S. 1, Iannotta V. 1, Cattabriga E. 1, Pancaldi C. 1, Cadossi R. 2, Borea P. A. 1

1 Pharmacology Unit, Department of Clinical and Experimental Medicine, University of Ferrara, Ferrara, Italy; 2 Laboratory of Biophysics, IGEA, Carpi, Italy


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Adenosine medi­ates a num­ber of phys­io­log­i­cal func­tions ­through the inter­ac­tion ­with 4 ­cell sur­face sub­types clas­si­fied as A1, A2A, A2B and A3 recep­tors ­which are cou­pled to G pro­teins. Recently we ­have dem­on­strat­ed ­that ­anti-inflam­ma­to­ry ­actions of aden­o­sine are pro­duced by the involve­ment of A2A and A3 aden­o­sine recep­tor sub­types. In ­human neu­troph­ils A3 recep­tors ­exert ­their ­anti-inflam­ma­to­ry prop­er­ties by inhib­it­ing degran­u­la­tion, chem­o­tax­is and super­ox­ide ­anion pro­duc­tion. Several ­works ­have inves­ti­gat­ed the depen­dence of pro­longed expo­sure to puls­ing elec­tro­mag­net­ic ­fields (PEMFs) on pro­life­ra­tive ­effects and on ­cell den­sity. The ­present ­paper ­describes a sig­nif­i­cant alter­a­tion of A3 aden­o­sine recep­tor den­sity and func­tion­al­ity in ­human neu­troph­ils ­exposed to PEMFs. Saturation bind­ing experi­ments ­were per­formed ­using a ­high affin­ity radio­lig­and antag­o­nist, [3H]-MRE 3008F20, and ­revealed a sig­nif­i­cant ­increase of A3 aden­o­sine recep­tor den­sity in ­PEMF-treat­ed ­human neu­troph­ils. A ther­mo­dy­nam­ic anal­y­sis of [3H]-MRE 3008F20 bind­ing was per­formed ­with the aim of obtain­ing new ­insights ­into the ­effect of PEMFs on the forc­es driv­ing ­drug-recep­tor ­coupling. Competition of radio­lig­and bind­ing by the ­high affin­ity A3 recep­tor ago­nists Cl-IB-­MECA and IB-­MECA in the ­absence and in the pres­ence of PEMFs has ­been per­formed. In func­tion­al ­assays the ­effects of Cl-IB-­MECA and IB-­MECA in the aden­y­lyl ­cyclase activ­ity, in the super­ox­ide ­anion pro­duc­tion and in cal­cium ­release ­have ­been eval­u­at­ed.

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