Development and characterization of immobilized cannabinoid receptor (CB1/CB2) open tubular column for on-line screening

作者：Moaddel R^*; Rosenberg A; Spelman K; Frazier J; Frazier C; Nocerino S; Brizzi A; Mugnaini C; Wainer I W

来源：Analytical Biochemistry, 2011, 412(1): 85-91.

DOI：10.1016/j.ab.2010.12.034

• Biochromatography
• Basophils
• Zanthoxylum
• Cannabinoids
• KU-812

Cannabinoid receptors, CB1 and CB2, are therapeutic targets in the treatment of anxiety, obesity, movement disorders, glaucoma, and pain. We have developed an on-line screening method for CB1 and CB2 ligands, where cellular membrane fragments of a chronic myelogenous leukemia cell line, KU-812, were immobilized onto the surface of an open tubular (OT) capillary to create a CB1/CB2-OT column. The binding activities of the immobilized CB1/CB2 receptors were established using frontal affinity chromatographic techniques. This is the first report that confirms the presence of functional CB1 and CB2 receptors on KU-812 cells. The data from this study confirm that the CB1/CB2-OT column can be used to determine the binding affinities (K(i) values) for a single compound and to screen individual compounds or 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-affinity phytocannabinoid. Published by Elsevier Inc.

• 出版日期2011-5-1