TABLE 2

pEC50/pIC50 values derived from curve fitting of TRPV1 agonists/antagonists dose-response measured using YFP-TRPV1-Luc intramolecular BRET probe, TRPV1-Luc/YFP-CaM intermolecular BRET probe, ACA, and APC

BRET assays were measured both in 96-well plate and 384 well plate’s formats. Values represent the mean ± S.E. of 3–9 independent experiments performed in duplicate. Values found in the literature are also indicated along with the method used, cellular model, and reference.

CompoundIntramolecular
BRET Probe		Intermolecular
BRET Probe		ACAAPCPotency Found in the LiteratureMethodCellular
Model		Reference
96
wells		384
wells		96
wells		384
wells
AgonistsCapsaicin6.96 ± 0.076.83 ± 0.056.73 ± 0.107.11 ± 0.218.05 ± 0.087.45 ± 0.037.1 - 7.3Ca2+(Fluo3/4)HEK293(Ralevic et al., 2001; Bianchi et al., 2006)
Olvanil5.89 ± 0.106.95 ± 0.056.42 ± 0.118.42 ± 0.167.93 ± 0.137.59 ± 0.046.36 - 7.73Ca2+(Fluo3/4)HEK293(Ralevic et al., 2001; Bianchi et al., 2006)
OLDA6.96 ± 0.744.94 ± 0.114.90 ± 0.315.99 ± 0.306.20 ± 0.105.64 ± 0.055.49 ± 0.06Ca2+(Fluo4)HEK293(Bianchi et al., 2006)
RTX8.02 ± 0.088.34 ± 0.067.59 ± 0.088.12 ± 0.188.19 ± 0.088.24 ± 0.047.92 – 8.6945Ca uptake
Ca2+(Fluo4)		HEK293
neurons		(Winter et al., 1990; Bianchi et al., 2006)
AntagonistsAMG 5177.12 ± 0.107.95 ± 0.146.97 ± 0.077.87 ± 0.058.12 ± 0.098.40 ± 0,059.19 ± 0,2545Ca uptakeCHO(Gavva et al., 2007b)
JNJ172032126.12 ± 0.116.91 ± 0.076.34 ± 0.066.47 ± 0.096.96 ± 0.028.24 ± 0,067.20 ± 0.11Ca2+(Fluo3)HEK293(Swanson et al., 2005)
BCTC8.05 ± 0.147.55 ± 0.057.54 ± 0.107.30 ± 0.028.02 ± 0.019.06 ± 0.028.77 ± 0.01Calcium4CHO-Trex(Papakosta et al., 2011)
SB 3667916.15 ± 0.356.47 ± 0.145.83 ± 0.216.45 ± 0.205.58 ± 0.087.84 ± 0.066.89 ± 0.2245Ca uptakeCHO(Gunthorpe et al., 2004; Gavva et al., 2005)
AMG 98106.12 ± 0.106.51 ± 0.326.55 ± 0.066.45 ± 0.096.31 ± 0.058.12 ± 0.047.72 ± 0.3345Ca uptakeCHO(Gavva et al., 2005)
AMG 216297.8 ± 0.188.64 ± 0.067.84 ± 0.098.35 ± 0.068.42 ± 0.048.64 ± 0.089.28 ± 0.2345Ca uptakeCHO(Gavva et al., 2007a)
Capsazepine6.31 ± 0.08n.d.6.19 ± 0.14n.d.6.32 ± 0.048.40 ± 0.067.90 – 8.2745Ca uptake
Ca2+(Fluo4)		CHO
HEK		(Gavva et al., 2005; Bianchi et al., 2006)