Abstract
The G protein–coupled receptor allosteric modulator SCH-202676 (N-(2,3-diphenyl-1,2,4-thiadiazol-5-(2H)-ylidene)methanamine), which affects a wide range of structurally unrelated G protein–coupled receptors, has highly divergent effects on purine receptors. SCH-202676 inhibited radioligand binding to human adenosine A 1, A 2A, and A 3 receptors (IC 50 = 0.5–0.8 μM) and affected dissociation kinetics, but at the human P2Y 1 nucleotide receptor it had no effect. SCH-202676 (10 μM) selectively accelerated agonist dissociation at adenosine A 3 receptors and either slowed (adenosine A 1 receptors) or accelerated (adenosine A 2A receptors) antagonist dissociation. Thus, SCH-202676 differentially modulated A 1, A 2A, and A 3 receptors as well as agonist- and antagonist-occupied receptors.
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