Table 2. In vitro binding affinity.
Compound | Ki(nM) for TSPOa | Ki(nM) for CBRa |
---|---|---|
CB251 | 0.27 ± 0.09 | >105 |
PK 11195 | 1.38 ± 0.42; 1.4 ± 0.4c | >105 |
PBR28 | 6.1 ± 6.4c | – |
flunitrazepamb | – | 5.11 ± 0.87 |
aAffinity of compounds determined by displacement of [3H]PK 11195 and [3H]flunitrazepam from rat cerebrocortical samples. The data are expressed as the mean values of three separate experiments performed in duplicate, which differed by less than 10%.
bFlunitrazepam, a selective ligand for CBR, was used for comparison.
cAccording to Ref. 25.