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.
Read more about this topic: Inverse Agonist
Famous quotes containing the word examples:
“Histories are more full of examples of the fidelity of dogs than of friends.”
—Alexander Pope (1688–1744)
“There are many examples of women that have excelled in learning, and even in war, but this is no reason we should bring ‘em all up to Latin and Greek or else military discipline, instead of needle-work and housewifry.”
—Bernard Mandeville (1670–1733)
“It is hardly to be believed how spiritual reflections when mixed with a little physics can hold people’s attention and give them a livelier idea of God than do the often ill-applied examples of his wrath.”
—G.C. (Georg Christoph)