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|Title:||Development and characterization of immobilized cannabinoid receptor (CB1/CB2) open tubular column for on-line screening.||Authors:||Moaddel, R
Wainer, I. W.
|Issue Date:||2011||Project:||None||Journal:||ANALYTICAL BIOCHEMISTRY||Abstract:||
Cannabinoid receptors, CB1 and CB2, are therapeutic targets in the treatment of anxiety, obesity, movementdisorders, glaucoma, and pain. We have developed an on-line screening method for CB1 and CB2ligands, where cellular membrane fragments of a chronic myelogenous leukemia cell line, KU-812, wereimmobilized onto the surface of an open tubular (OT) capillary to create a CB1/CB2–OT column. The bindingactivities of the immobilized CB1/CB2 receptors were established using frontal affinity chromatographictechniques. This is the first report that confirms the presence of functional CB1 and CB2receptors on KU-812 cells. The data from this study confirm that the CB1/CB2–OT column can be usedto determine the binding affinities (Ki values) for a single compound and to screen individual compoundsor a mixture of multiple compounds. The CB1/CB2–OT column was also used to screen a botanical matrix,Zanthoxylum clava-herculis, where preliminary results suggest the presence of a high-affinityphytocannabinoid.
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