Table 3.
Radioligand Competition Binding Affinity (Ki) Data of PAM Derivatives
 | ||||||
|---|---|---|---|---|---|---|
| compd | Y | MW | cLogP |
Ki (CB2), nMa,b |
Ki (CB1), nMa,c |
SId |
| 51 | 401.50 | 4.80 | 688 | >20000 | >29 | |
| 52 | CH2CH2 | 457.61 | 5.64 | 213 | >20000 | >93 |
| 53 | CH=CH | 453.58 | 5.80 | 167 | >20000 | >119 |
| 1e,f | 2.1 | NT | ||||
| 10e,g | NT | 10.6 | ||||
a
Binding affinities of compounds for CB1 and CB2 receptor were evaluated using [3H]CP-55,940 radioligand competition binding assay.
b
NB: no binding, Ki > 20000 nM.
c
NT: not tested.
d
SI: selectivity index for CB2, calculated as Ki(CB1)/Ki(CB2) ratio.
e
The binding affinities of reference compounds were evaluated in parallel with compounds 9, 11–61 under the same conditions.
f
CB2 reference compound SR144528.
g
CB1 reference compound SR141716.