Table 3.
Effect of photoactivatable allosteric modulators on stimulation of [35S]GTPγS binding to HEK293 cell membranes expressing the CB1 wild-type receptor.
Concentration of photoactivatable allosteric modulators |
||||||
---|---|---|---|---|---|---|
Compd | 0 µM | 3.2 µM | 10 µM | |||
Emax (fmol/mg)a |
EC50 (nM) a |
Emax (fmol/mg) a |
EC50 (nM) a |
Emax (fmol/mg) a |
EC50 (nM) a |
|
26 | 68.9 ± 1.7 | 4.7 (2.7–8.0) | 41.3 ± 1.1 | 2.7 (0.9–4.6) | ND | ND |
27 | 68.9 ± 1.7 | 4.7 (2.7–8.0) | 27.0 ± 1.3 | 7.9 (2.8–22.0) | ND | ND |
28 | 68.9 ± 1.7 | 4.7 (2.7–8.0) | 34.1 ± 1.1 | 2.1 (0.5–8.3) | ND | ND |
36b | 68.9 ± 1.7 | 4.7 (2.7–8.0) | 31.1±0.9 | 1.2 (0.5–3.8) | ND | ND |
Emax and EC50 values were determined from the CP55,940 dose-response curves. The level of GTPγS binding of mock-transfected cell membrane (30.1 ± 1.6 fmol/mg) was subtracted from each Emax value. ND, no detectable specific [35S]GTPγS binding.