Experimental setup to determine the binding affinity of doxepin isomers to H1R (IMAGE)
Caption
Doxepin is an antihistaminic drug that has two geometric isomers, which bind to the H1R receptor (depicted in the top half of the image). To understand why the Z-isomer is more effective than the E-isomer, researchers developed an experimental protocol to accurately quantify the binding affinity of each isomer to H1R. This involved extracting intact H1R-doxepin complexes from yeast cultures, releasing the bound doxepin molecules, and determining which isomer they represent using high-performance liquid chromatography.
Credit
Mitsunori Shiroishi from Tokyo University of Science
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