TABLE 1

Summary of antagonistic activity, selectivity, and lipophilicity (log D7.4) of 4-(1-aryltriazol-4-yl)-tetrahydropyridine derivatives IC50 values (nanomolar) of compounds toward human mGluR1a and human mGluR5 are shown as mean ± S.E.M. from more than three individual experiments




mGluR1a

mGluR5

Log D7.4


Compound 1 9.8 ± 0.88 820 ± 170 >4.0 Embedded Image
Compound 2 7.0 ± 1.2 170 ± 17 2.9 Embedded Image
FTIDC
5.8 ± 0.49
6200 ± 520
2.1
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