Table 1.

TRPV1 antagonists: their potencies to block the activation of the rat TRPV1 channel in different modes

Name, companyIUPAC nameStructureIC50 (nm) for activation modesReference
CAP (500 nm)pH (5.0)Heat (45°C)
AMG0347,Amgen(2E)-N-(7-Hydroxy-5,6,7,8-tetrahydro-1-naphthalenyl)-3-(2-(1-piperidinyl)-6-(trifluoro-methyl)-3-pyridinyl)-2-propenamideEmbedded Image0.7 ± 0.10.8 ± 0.30.2 ± 0.1Steiner et al. (2007)
AMG517,AmgenN-(4-((6-(4-(Trifluoro-methyl)phenyl)-4-pyrimidinyl)oxy)-1,3-benzothiazol-2-yl)-acetamideEmbedded Image1.0 ± 0.70.5 ± 0.21.5 ± 0.7Gavva et al. (2007b)
AMG8163,Amgentert-Butyl (2-(6-((2-(acetylamino)-1,3-benzothiazol-4-yl)oxy)-4-pyrimidinyl)-5-(trifluoromethyl)phenyl)-carbamateEmbedded Image0.6 ± 0.30.6 ± 0.30.2 ± 0.1Gavva et al. (2007a);Lehto et al. (2008)
A-425619,Abbott1-(5-Isoquinolinyl)-3-(4-(trifluoromethyl)- benzyl)-ureaEmbedded Image10 ± 213 ± 2a58 ± 4Gavva et al. (2007a)
AMG9810,Amgen(2E)-3-(4-tert-Butyl-phenyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-propenamideEmbedded Image79 ± 9349 ± 669 ± 1Gavva et al. (2007a)
JYL1421,Schwarz PharmaN-(4-((((4-tert-Butyl-benzyl)carbamothioyl)-amino)methyl)-2-fluoro-phenyl)methanesulfon-amideEmbedded Image8>4000>4000Gavva et al. (2007a)
SB-366791,GlaxoSK(2E)-3-(4-Chlorophenyl)-N-(3-methoxyphenyl)-acrylamideEmbedded Image547 ± 231>40000>40000Gavva et al. (2005)
CPZ,SandozN-(2-(4-Chlorophenyl)ethyl)-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2- benzazepine-2-carbothioamideEmbedded Image887 ± 340>400006.0 ± 2.9Gavva et al. (2005)
(324 ± 41)(355 ± 25)(<1000)Savidge et al. (2002)b
  • aThis value was measured at a pH of 5.5 (no inhibition occurred at 5.0).

  • bFor comparison, the IC50 values for guinea pig TRPV1 are shown in parentheses (measured at a CAP concentration of 100 nm, pH of 5.5, and temperature of 50°C).