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Inverse agonism at adenosine A 1 receptors was studied in a variety of experimental set-ups. As a read-out, the binding of [ 35 S]GTPγS to membranes of either CHO or COS-7 cells expressing human adenosine A 1 receptors was used. When wild-type receptors were studied, inverse agonism could only be detected at higher levels of receptor expression. However, receptors fused...
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