General Principles of cAMP Assays Identifying Active Compounds

For Gas-coupled receptors, an agonist will stimulate production of cAMP, while an antagonist will inhibit agonist-induced cAMP production. For Gai-coupled receptors, the effect of an agonist whose binding results in the inhibition of AC cannot easily be measured because the basal cAMP is too low. Cells are first stimulated to produce cAMP with forskolin. An agonist will inhibit forskolin-induced cAMP production and this is measurable. Gai-coupled receptor antagonist: cells are stimulated to produce cAMP with forskolin. The antagonist will block the effect of an agonist acting on the receptor and therefore forskolin-induced cAMP formation is re-established.

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