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- W1969866442 abstract "Adenosine A3 receptors are reported to couple negatively to adenylyl cyclase (AC) but their mediation of anti-inflammatory effects in human eosinophils prompted us to investigate their coupling to AC. The A3-selective agonists IB-MECA and Cl-IB-MECA evoked a concentration-dependent generation of cAMP (EC50, 3.2 and 1.8 μM, respectively) and were more potent than the A2A agonist CGS 21680 (EC50=15.4μM) and adenosine (EC50=19.2μM). The cAMP response was additive to that produced by forskolin (10 μM). The effect of IB-MECA was insensitive to A1 and A2A receptor antagonists, but was antagonized by the A3-selective antagonist MRS 1220 (0.1–2.5 μM) in a competitive manner. The estimated KB of 190 nM was, however, atypical. The cyclo-oxygenase inhibitor, indomethacin, had no effect on the cAMP response. A general inverse relationship between cAMP generation and inhibition of degranulation was seen. We conclude that in human eosinophils, an atypical form of A3 receptors positively coupled to AC may exist. The resulting cAMP generation may underlie the anti-inflammatory actions of A3 agonists in eosinophils." @default.
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- W1969866442 date "2003-01-01" @default.
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- W1969866442 title "Positive coupling of atypical adenosine A3 receptors on human eosinophils to adenylyl cyclase" @default.
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- W1969866442 doi "https://doi.org/10.1016/s0006-291x(02)02910-8" @default.
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