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. Author manuscript; available in PMC: 2013 Oct 19.
Published in final edited form as: Bioorg Med Chem Lett. 2012 Apr 13;22(11):3656–3660. doi: 10.1016/j.bmcl.2012.04.034

Table 1. Potencies of vanilloid ligands for binding to rat TRPV1 and for inducing calcium influx in CHO/TRPV1 cells.

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Y Z R1 R2 Ki (nM)a Binding Affinity Agonism b (%) Ki (nM)c Antagonism (%)
1 1 1 H 3,4-Me2 29.3 ±7.6 (15%) 67 ±25
2 1 1 H 4-t-Bu 64 ±21 (40%) 86 ±17
3 1 1 F 3,4-Me2 54 ±28 NE 7.8±3.0
4 1 1 F 4-t-Bu 22.6 ±2.7 (5%) 52 ±17
5 0 1 H 3,4-Me2 580 (±130 (19%) (48%)
6 0 1 H 4-t-Bu 416 ±44 (8%) (31%)
10 0 1 F 3,4-Me2 233 ±18 NE 650 ±210
11 0 1 F 4-t-Bu 115 ±2.7 NE 179 ±20
32 1 0 H 4-t-Bu 143 ±43 NE 91 ±25
33 1 0 F 4-t-Bu 69 ±18 NE 116 ±40
18 0 2 H 3,4-Me2 390 ±100 (5%) 33.7 ±2
19 0 2 H 4-t-Bu 366 ±8.1 NE 286 ±48
20 0 2 F 3,4-Me2 120 ±4.6 NE 111 ±43
21 0 2 F 4-t-Bu 190 ±38 NE 152 ±46
26 0 0 H 4-t-Bu 197 ±56 (46%) 940±420(46%
27 0 0 F 4-t-Bu 244 ±46 (35%) 213±18 (72%)

NE: not effective, WE: weakly effective at 30 μM

a

mean ± SEM of at least three experiments

b

if any agonism was detected, value in parentheses indicates fractional calcium uptake compared to that by 30 μM capsaicin

c

mean ± SEM of at least three experiments for measuring Ki. Value in parenthesis indicates measured extent of partial antagonism if observed