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- W1970780150 abstract "Agonist-induced desensitization has been described for the A1, A2A, and A3 adenosine receptor subtypes of the G protein-coupled receptor superfamily. Desensitization of the fourth adenosine receptor subtype, the A2B adenosine receptor (A2BR), has not been studied extensively. We sought to determine whether the A2BR is subject to agonist-induced desensitization. COS 7 cells, which exhibit endogenous expression of the A2BR, and transfected CHO cells, which stably express a modified rat A2BR bearing a 5′ FLAG epitope tag, were studied. Cyclic AMP (cAMP) responsiveness to an acute challenge was measured after pretreating (desensitizing) cells with the adenosine receptor agonist 5′-N-ethylcarboxamidoadenosine (NECA). Incubation with NECA resulted in hyporesponsiveness to acute agonist challenge in both COS 7 and transfected CHO cells. Desensitized cells exhibited restoration of cAMP responses after recovery for 24 hr in growth medium. Choleratoxin-induced cAMP responses were preserved in desensitized cells, and high concentrations of NECA were unable to overcome the desensitization. Membrane levels of the epitope-tagged A2BR were assessed by western blot in transiently transfected COS 7 cells. The expression of epitope-tagged A2BRs was not different between control and desensitized cells. In northern blot analysis, levels of endogenous A2BR mRNA were similar in control and desensitized COS 7 cells. We conclude that the A2BR is subject to agonist-induced desensitization with preserved expression of A2BR mRNA and protein. Uncoupling of the A2B adenosine receptor from the G protein complex may contribute to the mechanism of desensitization." @default.
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- W1970780150 date "1998-03-01" @default.
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- W1970780150 title "Agonist-Induced Desensitization of A2B Adenosine Receptors" @default.
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- W1970780150 doi "https://doi.org/10.1016/s0006-2952(97)00560-1" @default.
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