| Assay Method Information | |
| | calcium assay |
| Description: | Capsaicin (0.3 μM) caused an increase in [Ca2+] in the vast majority (95%) of dorsal root ganglia neurons, which were thereby identified as TRPV1 expressing neurons. All synthesized derivatives were tested and all were able to inhibit the calcium uptake and several compounds exhibited more than 80% inhibition, e.g. compounds of Examples 1, 3, 4, 5, 6, 10, 11, 12, 13, 16, 19, 23, 31, 32, 35, 36, 39, 41, 45, 46, 47, 48, 51, 53, 67, 68, 69, 70, 71, 74, 75, 78, 80, 81, 82, 86, 87 and 89. Among them, derivatives such as compounds of Examples 4, 5, 6, 13, 19, 31, 36, 39, 45, 46, 47, 48, 51, 52, 53, 67, 70, 71, 74, 75, 78, 80, 81, 86 and 87, appeared the most potent TRPV1 antagonists exhibiting a complete abolition of capsaicin response (around 100%) at 300 nM. |
| Affinity data for this assay | |
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