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| | Radioligand Binding Assay and Antagonist Ca2+ Influx Functional Assay |
| Description: | The hTRPV1-expressing CHO cell membranes were incubated with [3H]A-778317 and test compounds to establish equilibrium. After incubation was terminated, bound tritium radioactivity (dpm) was counted in a scintillation counter. The Ki values were determined by the application of the Cheng-Prusoff equation: Ki = (IC50 x Kd)/(Kd+[L]) where [L] is the concentration of [3H]A-778317 (2 nM ) and Kd is the dissociation constant of the [3H]A-778317 determined in the saturation analysis (Kd=6.2 nM for A-778317). EC/IC50 is the functional potencies of TRPV1 antagonists against 50 nM CAP at the hTRPV1 receptor, as determined in a Ca2+ influx assay. |
| Affinity data for this assay | |
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