Allosteric Modulators: The New Generation of Receptor Antagonist

Allosteric modulation of receptor responses to a series of agonists. Potency values [expressed here as pEC₅₀ values (i.e., the negative logarithm of the molar concentration producing the half-maximal response) of muscarinic agonists for M₂ receptors are indicated in the absence and presence of saturating concentrations of the allosteric modulator eburnamonine. Acetylcholine (Ach, filled triangles), pilocarpine (open squares), oxotremorine (filled squares), methylfurmethide (filled diamonds), arecaidine propargyl ester (APE, filled circles), arecoline (open circles) and carbachol (open triangles). Data from (3).