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. 2017 Jul 19;8(8):1697–1705. doi: 10.1039/c7md00296c

Table 1. CB1 and CB2 receptor affinity of 1,3,4- and 1,2,4-oxadiazole regioisomers 1a–c and 9a–c.

Inline graphic
Compd R X Y K i (hCB2) ± SEM a [nM] Displacement (hCB1) b
1a graphic file with name c7md00296c-u2.jpg Br F 2.9 ± 0.41 d –13% c
1b F Br 6.7 ± 1.0 d –5%
1c CN F 270 ± 32 d –8%
9a graphic file with name c7md00296c-u3.jpg Br F 25 ± 4.1 22% c
9b F Br 318 ± 55 –8%
9c CN F 219 ± 16 –1%
CP 55940 8.44 ± 0.18 9.26 ± 0.12
WIN 55212-2 8.57 ± 0.16 8.72 ± 0.24
HU 210 9.78 ± 0.04 9.55 ± 0.06

aThe reported Ki-values are mean values of three independent experiments (n = 3).

bDue to the low hCB1 affinity, only the radioligand displacement at a test compound concentration of 1 μM is given as mean value of two independent experiments (n = 2).

cMean value of four experiments (n = 4).

dThe CB2 affinity of lead compounds 1a–c has been recorded previously in another laboratory.11