| Assay Method Information | |
| | Competition Binding Assay and Inhibition of Ca2+ Uptake Assay |
| Description: | Binding assay mixtures were set up and contained [3H] RTX, various concentrations of competing ligands, and rVR1-transfected CHO cells. Nonspecific binding was determined in the presence of 100 nM nonradioactive RTX. After the binding reaction, membrane-bound RTX was separated from the free by centrifugation, and the radioactivity was determined by scintillation counting. Equilibrium binding parameters (Ki, Bmax, and cooperativity) were determined by fitting the Hill equation to the measured values with the aid of the program Origin 6.0. EC/IC50 is the functional potencies of TRPV1 antagonists against 50 nM capsaicin at the CHO/rVR1 cells, as determined in a Ca2+ uptake assay. |
| Affinity data for this assay | |
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