Table 3.
IC50 | ||||
---|---|---|---|---|
NAM | mGlu5 HEK | striatal | hippocampal | cortical |
MPEP | 42.4 ± 7.5 nM | 1.13 ± 0.36 μM | 41.7 ± 4.7 nM | 119 ± 34.1 nM |
Fenobam | 178 ± 40 nM | 2.93 ± 0.48 μM | 442 ± 150 nM | 807 ± 53.5 nM |
AFQ056 | 37.6 ± 8.9 nM | 9.44 ± 3.78 μM | 257 ± 27.4 nM | 270 ± 73.0 nM |
RG7090 | 1.76 ± 0.88 nM | 62.0 ± 17.5 nM | 8.97 ± 3.40 nM | 80.2 ± 16.8 nM |
AZD2066 | 27.2 ± 9.1 nM | 3.56 ± 0.52 μM | 96.2 ± 17.8 nM | 380 ± 78.0 nM |
The IC50 values of various mGlu5 NAMs were determined from the inhibition curves in Figure 4 using GraphPad Prism.