TABLE 3

CB, FFA, and prostanoid receptor fluorescent ligands

ToolDataReference
CB1 Receptor and GPR55 Receptor Ligands
T1117hGPR55-mediated Ca2+ response in HEK293 cellsaDaly et al., 2010
mCB1 10% displacement of [3H]CP-55,940 with 1 µM T1117
hCB1 Kd = 460 ± 80 nMBruno et al., 2014
CB Receptor Ligands
2-AGE-biotin-3bbhCB1 Ki = 221 ± 8 nMMartin-Couce et al., 2011
hCB2 Ki = 450 ± 11 nM
NMP6hCB1 < 40% at 10 µMPetrov et al., 2011
hCB2 Ki = 387 nM
Biotin-HU210-1ahCB1 Ki = 2.4 ± 0.4 nMMartín-Couce et al., 2011
hCB2 Ki = 1.6 ± 0.4 nM
Biotin-HU308-3ahCB1 Ki > 5000 nMMartín-Couce et al., 2011
hCB2 Ki = 44 ± 4 nM
NIR-mbc94mCB2 Ki = 260 nMSexton et al., 2011
NIR760-mbc94mCB2 Kd = 26.9 ± 3.7 nMZhang et al., 2013
NIR760-QhCB2 Kd = 75.51 ± 27.97 nMWu et al., 2014b
ZW760-mbc94mCB2 Kd = 53.9 ± 13.0 nMWu et al., 2014a
NIR760-XLP6mCB1 Kd > 10,000 nMLing et al., 2015
mCB2 Kd = 169.1 ± 66.09 nM
IR700DX-mbc94mCB2 Kd = 42.0 ± 19.6 nMZhang et al., 2014
FFA Receptor Ligands
TUG-905-NBD-4hFFA1 Kd = 7.4 ± 1.3 nMChristiansen et al., 2016
F-TAK-875AhFFA1 Kd = 15.1 ± 3.2 nMRen et al., 2016
TAK-875-Alexa488-16hFFA1-mediated Ca2+ response equipotent to TAK-875Bertrand et al., 2016b
EP3 Receptor Ligands
Pyryllium-labeled cinnamon acid derivative 8hEP1 Ki = 68,625 ± 12,735 nMTomasch et al., 2012
hEP2 Ki = 2943 ± 279 nM
hEP3 Ki = 135 ± 23 nM
hEP4 Ki = 902 ± 226 nM
  • a HEK293 cells stably expressing GPR55.

  • b Biotin-tagged ligand (precursor for fluorescent tool) that conjugates with streptavidin-fluorophore in situ during the biologic experiment to provide corresponding fluorescent tool.