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

Table 2. mGlu₅ Potency and Rat Brain Penetration SAR in Constrained Cyclic Amine 1,2,4-Triazole Analogues.

entry	series	R¹	R²	mGlu₅ IC₅₀ (nM)	rat B/P ratio
20	I	3-chlorophenyl	A (Z = CH; R³ = CO₂NH₂)	11	<0.01
21	I	3-chlorophenyl	A (Z = N; R³ = NH₂)	<3	0.085
22	I	3-chlorophenyl	A (Z = N; R³ = NMe₂)	39	0.285
23	I	5-chlorothiophen-3-yl	B (Z = N; R³ = H)	39	<0.01
24	II	5-chlorothiophen-3-yl	B (Z = N; R³ = H)	34	0.06
25	I	5-chlorothiophen-3-yl	B (Z = N; R³ = Me)	61	0.16
26	II	3-chlorophenyl	B (Z = N; R³ = H)	32	<0.01
27	II	3-chlorophenyl	B (Z = CH; R³ = Me)	39	<0.01
28	III	3-chlorophenyl	B (Z = N; R³ = H)	46	not reported

Table 2. mGlu5 Potency and Rat Brain Penetration SAR in Constrained Cyclic Amine 1,2,4-Triazole Analogues.