Table 4.
| |||||
---|---|---|---|---|---|
compd | R | MW | cLogP | Ki (CB2), nMa,b | Ki (CB1, nMa,c |
54 | H | 338.44 | 3.75 | 35970 | NT |
55 | CH3 | 352.47 | 4.19 | 18200 | NB |
1d,e | 2.1 | NT | |||
10d,f | NT | 10.6 |
Binding affinities of compounds for CB1 and CB2 receptor were evaluated using [3H]CP-55,940 radioligand competition binding assay
NB: no binding, Ki > 20000 nM.
NT: not tested.
The binding affinities of reference compounds were evaluated in parallel with compounds 9, 11–61 under the same conditions.
CB2 reference compound SR144528.
CB1 reference compound SR141716.