Structure–activity relationships of inverse agonists for G‐protein‐coupled receptors

Abstract

It has been recently established that G-protein-coupled receptors (GPCRs) can be constitutively active, i.e., they can be active in the absence of an agonist. This activity can be inhibited by so-called inverse agonists. For a number of GPCRs, such inverse agonists have been developed and studied, now enabling for the first time a study into their structure-activity relationships.

Review of 5-HT4R Ligands: State of Art and Clinical Applications

“…Indeed, 5-HT 4 R ligands can be full agonists, partial agonists, antagonists or inverse agonists (see [193], for a general review) depending on the preparation studied. For example, tegaserod (79) and cisapride (3) have been reported as being full or partial agonists.…”

Partial Agonism, Neutral Antagonism, and Inverse Agonism at the Human Wild-Type and Constitutively Active Cholecystokinin-2 Receptors

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