App Note

Characterizing pharmacological compounds with complementary Upstream and Downstream GPCR readouts

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Case studies combining GTP binding and cAMP assays for greater insight

The GTP Gi binding assay and the cAMP Gi assay enable you to study the GPCR activation response at different levels of the signaling pathway. This application note describes two case studies highlighting the complementary and relevant use of these assays for characterizing a panel of reference compounds ( full agonists, partial agonists, and antagonists)  in two different receptor models.

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  • Compounds action on upstream and downstream readouts
  • Differences in compounds potencyies and efficacyies depending on biological GPCR biological activation mechanism and potential signal amplification
  • Concrete examples based on δ-opioid and D2 receptor models
  • Detailed experimental conditions and explanatory diagrams

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