Table 3.
Antagonist activity of enantiopure β-lactam derivatives at rTRPM8 channels (Ca2+ microfluorimetry assays). Activation is induced by 100 µM menthol.
![]() | |||||
Compound | XR1 | R2 | R3 | IC50 (µM) | 95% Confidence Intervals |
---|---|---|---|---|---|
1 | OtBu |
![]() |
Bn | 1.06 ± 1.21 | 0.72 to 1.55 |
34 | NHiBu |
![]() |
Bn | 0.30 ± 1.26 | 0.19 to 0.50 |
35 | NHBn |
![]() |
Bn | 0.49 ± 1.27 | 0.30 to 0.79 |
36 | NHCH2(2-Pic) |
![]() |
Bn | 0.84 ± 1.32 | 0.48 to 1.49 |
37 | OtBu |
![]() |
H | 3.06 ± 1.25 | 2.67 to 3.51 |
40 | OtBu |
![]() |
H | 6.36 ± 1.41 | 3.08 to 13.17 |
41 | OtBu |
![]() |
H | 9.26 ± 1.41 | 4.44 to 19.35 |
42 | NHiBu |
![]() |
H | 2.19 ± 1.36 | 1.15 to 4.17 |
43 | NHiBu |
![]() |
H | 4.03 ± 1.35 | 2.14 to 7.60 |
44 | NHiBu |
![]() |
H | 3.27 ± 1.31 | 1.86 to 5.75 |
45 | NHiBu |
![]() |
H | 3.56 ± 1.40 | 1.74 to 7.31 |
AMTB | 7.3 ± 1.50 | 6.82 to 7.85 |