TABLE 1

Radioligand binding properties of wild-type and mutant cell lines

The Kd and Bmax values were determined from saturation binding experiments using [3H]SR141716A on HEK293 cell membrane preparations stably transfected with the wild-type or mutant hCB1 receptor. Data represent the mean and corresponding S.E.M. of at least three independent experiments performed in triplicate. No statistically significant difference was observed between the wild-type and mutant binding properties as determined by a two-tailed Student’s t test.

RadioligandCell LineKd (nM)95% CLBmax95% CL
pmol/mg
[3H]SR141716AWT hCB12.2(0.4–3.9)2.4(1.9–2.9)
D2.63176A4.2(0.1–9.8)2.3(1.0–3.5)
K373A1.7(0.2–3.5)1.8(0.1–3.7)
D2.63176A-K373A4.4(0.1–9.1)2.7(1.7–3.7)
D2.63176K-K373D3.5(0.1–24)0.7(0.1–2.4)