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. 2010 Aug 23;1(12):788–795. doi: 10.1021/cn1000638

Table 2. Functional Activity of Representative mGluR2 PAMs 5, 4168a.

graphic file with name cn-2010-000638_0010.jpg

compound R2 mGlu2 EC50 (μM)a mGlu2 Emax (%)
5 Ph- 6.29 138
41 2-F-Ph- 1.00 44
42 3-F-Ph- 1.91 96
43 4-Cl-Ph- 1.41 189
44 4-OH-Ph- >10  
45 4-CF3O-Ph- 0.24 228
46 2,3-diF-Ph- 10 131
47 2,4-diF-Ph- 4.79 128
48 2,4,6-triF-Ph- 2.96 118
49 3-F-4-Cl-Ph- 0.48 180
50 2-F-4-CF3−Ph- 3.16 124
51 3-Py- >10  
52 3-(6-MeO)Py- 6.03 66
53 3-(6-CF3)Py- 6.76 144
54 4-(2-Me)-triazolyl- >10  
55 2-benzimidazolyl- >10  
56 2-benzothiazolyl- 5.62 79
57 PhCH2CH2- 3.71 117
58 PhOCH2- 3.98 87
59 3-Cl-PhOCH2- 3.16 124
60 4-Cl-PhOCH2- 1.91 115
61 n-propyl- 7.24 53
62 n-butyl- 9.28 122
63 i-butyl- 0.54 75
64 s-butyl- 12.88 97
65 CF3CH2CH2- 8.71 97
66 cyclopentyl- 9.33 122
67 cyclohexyl- 0.43 120
68 cyclohexylmethyl- 1.08 161
a

Values are means of three experiments.