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. Author manuscript; available in PMC: 2012 Aug 17.
Published in final edited form as: ACS Chem Neurosci. 2011 Aug 17;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 nihms-291053-t0003.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