Table 1.
IC50 (nM) values of diverse TRPV1 antagonists
| 14 (Jerman et al., 2000) | Ruthenium Red (ammoniated ruthenium oxychloride) |
| 912 (Rigoni et al., 2003)a | Capsazepine (N-[2-(4-chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide) |
| 0.071 (Rigoni et al., 2003)a | Iodo-resiniferatoxin (6,7-deepoxy-6,7-didehydro-5-deoxy-21-dephenyl-21-(phenylmethyl)-daphnetoxin,20-(4-hydroxy-5-iodo-3-methoxybenzeneacetate) |
| 638.6 (Appendino et al., 2003) | 6-iodo-nordihydrocapsaicin (6-iodo-nordihy 8-methyl-N-vanillyl-trans-6-nonenamide) |
| 7.5 (Gunthorpe et al., 2003) | SB 366791 (N-(3-methoxyphenyl)-4-chlorocinnamide) |
| 100 (Himmel et al., 2002) | L-R4W2 (L-enantiomers of the arginine-rich hexapeptide) |
| 4.8–58 (Sun et al., 2003)b | 4-(2-pyridyl)piperazine-1-carboxamides |
| 7.8 (Lee et al., 2003)c | N-[2-(3,4-dimethylbenzyl)-3-pivaloyloxypropyl]-N′-[3-fluoro-4-(methylsulphonylamino)benzyl] thiourea |
| 9.2 (Wang et al., 2002)c | JYL1421 ([N-(4-tert-butylbenzyl)-N′-[3-fluoro-4-(methylsulphonylamino)benzyl]thiourea]) |
| 6–35 (Valenzano et al., 2003) | BCTC (N-(4-tertiarybutylphenyl)-4-(3-cholorphyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide) |
NB: IC50 values are referred to the inhibition of capsaicin-induced calcium uptake in: endogenous TRPV1 in rat DRG neurons.
a
Human TRPV1 HEK293 cell line.
b
Rat TRPV1 HEK293 cell line.
c
rVR1 CHO cells.