Distinct structure activity relations for VR binding and subsequent calcium uptake
| Ligand | Binding | Ca Uptake | Relative Potency |
|---|---|---|---|
| Ki, nM | EC50, nM | binding vs. Ca uptake | |
| Resiniferanoids (1–4) | |||
| Orthobenzoyl-RTX | 0.17 | 7.6 | 44.00 |
| RTX | 0.04 | 0.9 | 22.00 |
| ROPA-20-dimethoxyphenylacetate | 1.00 | 15.0 | 15.00 |
| 3β-Hydroxy-RTX | 4.40 | 57.5 | 13.00 |
| Tinyatoxin | 0.17 | 1.5 | 9.00 |
| ROPA-20-[4-aminoethoxy-3methoxyphenylacetate] | 4.30 | 13.0 | 3.00 |
| RTX-thiourea | 69.00 | 150.0 | 2.00 |
| ROPA-20-phenylacetate | 8.30 | 10.2 | 1.20 |
| RTX-amide | 26.00 | 26.5 | 1.00 |
| Capsaicinoids (2, 5) | |||
| Capsaicin | 4,900 | 340 | 0.07 |
| Vanillyl-octylthiourea | 8,500 | 150 | 0.02 |
| Olvanil | 340 | 180 | 0.02 |
| Phorboid vanilloids (6, 7) | |||
| PPAHV | 3,100 | 1,800 | 0.60 |
| PDDHV | >10,000 | 60 | <0.002 |
| Terpenoid 1,4-unsaturated dialdehydes (8) | |||
| Isovelleral | 5,200 | 95 | 0.02 |
References indicated in parentheses: (1) Ács et al., 1995; (2) Ács et al., 1996b; (3) Lee et al., 1995; (4) Walpole et al., 1996; (5) Winter et al., 1993; (6) Szallasi et al., 1996b; (7) Szallasi et al., 1998c; (8) Szallasi et al., 1996a.