Table 5.

Four classes of rat TRPV1 antagonists with distinct pharmacological action profiles

Profile	Examples	Response to capsaicin (0.5 μmol L−1)	Response to pH 5	Response to heat (45 °C)	Effect on body temperature in rodents
A	A-425619, AMG0347, AMG517, AMG6880, AMG7472, AMG8163, AMG9810, BCTC, iodo-resiniferatoxin, SB-705498	Block	Block	Block	Hyperthermia
B	AMG0610, AMG8563, capsazepine; SB-366791	Block	Partial block	Block	Hyperthermia
C	AMG8562	Block	Potentiation	Block	No change
D	AMG7905	Block	Potentiation	Potentiation	Hypothermia

A-425619: 1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea; AMG0347: (E)-N-(7-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)-3-(2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)acrylamide; AMG517: N-(4-[6-(4-trifluoromethyl-phenyl)-pyrimidin-4-yloxy]-benzothiazol-2-yl)-acetamide I; AMG0610: (2E)-3-(6-tert-butyl-2-methylpyridin-3-yl)-N-(1H-indol-6-yl)acrylamide; AMG6880: (2E)-3-[2-piperidin-1-yl-6-(trifluoromethyl)pyridin-3-yl]-N-quinolin-7-ylacrylamide; AMG7472: 5-chloro-6-{(3R)-3-methyl-4-[6-(trifluoromethyl)-4-(3,4,5-trifluorophenyl)-1H-benzimidazol-2-yl]piperazin-1-yl}pyridin-3-yl)methanol; AMG7905: N-(6-(2-(cyclohexylmethylamino)-4-(trifluoromethyl)phenyl)pyrimidin-4-yl)benzo[d]thiazol-6-amine; AMG8163: tert-butyl-2-(6-([2-(acetylamino)-1,3-benzothiazol-4-yl]oxy)pyrimidin-4-yl)-5-(trifluoromethyl)phenylcarbamate; AMG8562: (R,E)-N-(2-hydroxy-2,3-dihydro-1H-inden-4-yl)-3-(2-(piperidin-1-yl)-4-(trifluoromethyl)phenyl)acrylamide; AMG8563: (S,E)-N-(2-hydroxy-2,3-dihydro-1H-inden-4-yl)-3-(2-(piperidin-1-yl)-4-(trifluoromethyl)phenyl)acrylamide; AMG9810: (E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)acrylamide; BCTC: N-(4-tertiarybutylphenyl)-4(3-cholorphyridin-2-yl)-tetrahydropyrazine-1(2H)-carboxamide; SB-366791: (2E)-3-(4-chlorophenyl)-N-(3-methoxyphenyl)acrylamide; SB-705498: N-(2-bromophenyl)-N'-[((R)-1-(5-trifluoromethyl-2-pyridyl)pyrrolidin-3-yl)]urea. Adapted from Lehto et al. (2008).