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Effects of protein kinase C activation on the sensitivity of pre‐ and postsynaptic adenosine receptors
Author(s) -
Dunwiddie Thomas V.,
Diao Lihong
Publication year - 1998
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/(sici)1098-2299(199811/12)45:3/4<329::aid-ddr32>3.0.co;2-u
Subject(s) - postsynaptic potential , adenosine , receptor , protein kinase c , adenosine receptor , adenosine a1 receptor , chemistry , endocrinology , medicine , pharmacology , biology , kinase , biochemistry , agonist
Prolonged incubation of hippocampal brain slices at reduced temperature immediately after preparation (“cold shock” treatment) has been shown to lead to an extremely persistent activation of protein kinase C (PKC). Because of the numerous suggestions that adenosine receptor sensitivity can be modulated by PKC, we have characterized the changes in both pre‐ and postsynaptic adenosine A 1 receptor sensitivity following such treatment. The maximal effect of activation of postsynaptic A 1 receptors was significantly reduced, although there was no change in the EC 50 value. On the other hand, the sensitivity of presynaptic adenosine receptors was slightly although significantly increased (the EC 50 value was reduced), with no apparent change in the maximal effect. Finally, the effect of dipyridamole was reduced in these slices, suggesting that its ability to inhibit adenosine transport was reduced. These results suggest that the cold shock treatment does not affect PKC activity in all cellular compartments and that, in particular, PKC‐dependent changes in nerve terminal and somatic A 1 receptors are markedly different. Drug Dev. Res. 45:329–335, 1998. Published 1998 Wiley‐Liss, Inc. †