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TRPV1 activities of the two chiral isomers of 54
 | |||||
|---|---|---|---|---|---|
| rTRPV1 | hTRPV1 | ||||
| Ki (nM) Binding Affinity |
Ki (nM) [CAP] Antagonism |
Ki (nM) Binding Affinity |
Ki (nM) (CAP) Antagonism |
Ki (nM) (pH) Antagonism |
|
| 54 | 46.2 (±3.0) | 7.6 (±1.6) | 89 (±17) | 5.1 (±1.2) | 12.7 (±3.6) |
| 54R | 750 (±200) | 186 (±29) | 2590 (±390) | 217 (±57) | 440 (±41) |
| 54S | 24.4 (±0.82) | 4.16 (±0.67) | 15.8 (±4.4) | 0.49 (±0.13) | 8.3 (±1.6) |
