Inverse Agonist - Examples

Examples

An example of a receptor that possesses basal activity and for which inverse agonists have been identified is the GABAA receptor. Agonists for the GABAA receptor (such as the benzodiazepines alprazolam and diazepam) elicit a sedative effect while inverse agonists have anxiogenic (for example, Ro15-4513) or even convulsive effects (certain beta-carbolines).

Two known endogenous inverse agonists are the agouti related peptide (AgRP) and its associated peptide Agouti signaling peptide (ASIP) both are expressed in humans and each bind melanocortin receptors 4 and 1 (Mc4R and Mc1R) respectively with nanomolar affinities.

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