Article
Inverse agonism and the regulation of receptor number.
Trends in pharmacological sciences - 1 Dec 1997
Milligan G, Bond R A
Abstract excerpt
Inverse agonists are ligands that preferentially stabilize inactive conformations of G protein-coupled receptors. In a range of systems, sustained treatment with inverse agonists can produce substantially greater upregulation of receptor levels than antagonists. The use of constitutively active mutant receptors can exaggerate this effect but may also allow agonists and antagonists to mimic the effect by...
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