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Table 2 Effect of different TRPM8 antagonists on T b in rats. P value is for comparing compound administered rat T b with vehicle administered rat T b . End of the study plasma concentration is reported in μM. Asterisk indicates one-way ANOVA followed by Dunnett's MCT

From: Transient receptor potential melastatin 8 (TRPM8) channels are involved in body temperature regulation

Compound

Dose mg/kg (route)

Max T bdecrease (°C)

P value *

Time post dosing (min)

Plasma concentration

AMG0635

3 (p.o.)

0.47

p < 0.05

120

0.38 ± 0.04

AMG8788

30 (p.o.)

0.53

p < 0.05

40

1.5 ± 0.6

AMG9678

10 (p.o.)

0.72

p < 0.001

60

0.04 ± 0.006

AMG9678

30 (p.o.)

0.70

p < 0.01

60

0.34 ± 0.1

AMG9678

100 (p.o.)

0.83

P < 0.05

60

0.36 ± 0.12

AMG2850

100 (p.o.)

0.98

p < 0.0001

140

22 ± 0.8

Compound 496

30 (p.o.)

0.64

p < 0.01

100

14.9 ± 0.95