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. Author manuscript; available in PMC: 2014 Mar 27.
Published in final edited form as: J Med Chem. 2012 Oct 31;55(22):9973–9987. doi: 10.1021/jm301212u

Table 4.

Radioligand Competition Binding Affinity (Ki) Data of PAM Derivatives

graphic file with name nihms562666t4.jpg
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
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

The binding affinities of reference compounds were evaluated in parallel with compounds 9, 11–61 under the same conditions.

e

CB2 reference compound SR144528.

f

CB1 reference compound SR141716.