Table 1.
Pharmacological selectivity of JNJ compounds
| JNJ-38893777 | JNJ-17203212 | |
|---|---|---|
| pIC50 (capsaicin) | 8.08 | 7.19 |
| pIC50 (low pH) | 8.13 | 7.8 |
| pK i (hTRPV1) | 8.0 | 7.3 |
| Activity against related TRP channelsa | no activity (pIC50 < 5) | weak activity against cTRPM8 (pIC50 < 6) |
| Activity against non-related channels or receptors | weak activity against: | no activity |
| human Cholecystokinin 1 receptor (pK i 6.1) | ||
| human Adenosine 3 receptor (pK i 6.2) | ||
| rat cerebral cortex sodium channel (pK i 6.1) |
pIC50 values were determined using the recombinant hTRPV1 in a Ca2+ influx in vitro assay (FLIPR) [58]. pK i values were determined by radioligand binding to a broad panel of receptors, channels and transporters at CEREP (Paris, France) [43]
aActivity was tested against the following related TRP channels: rTRPV2, hTRPV4, hTRPA1, cTRPM8