Table 3. mGlu5 Potency and Rat Brain Penetration SAR in Sulfide Bridged Analogues.
entry | series | A | R1 | mGlu5 IC50 (nM) | rat B/P ratio |
---|---|---|---|---|---|
34 | I | CH | H | 19 | <0.01 |
35 | I | CH | Me | 87 | 0.10 |
36 | I | N | H | 18 | <0.01 |
37 | II | CH | H | 24 | 0.09 |
38 | II | CH | Me | 30 | 0.16 |
39 | II | N | H | 41 | 0.04 |
40 | III | CH | H | 146 | <0.01 |
41 | III | CH | Me | 380 | 0.02 |
42 | III | N | H | 19 | 0.26 |