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. 2011 Apr 15;2(8):411–432. doi: 10.1021/cn2000266

Table 3. mGlu5 Potency and Rat Brain Penetration SAR in Sulfide Bridged Analogues.

graphic file with name cn-2011-000266_0008.jpg

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