Figure 6.
Agonist desensitization rates. (a) Desensitization rates of fully efficacious agonists varied greatly. Desensitization rates were determined as previously described in ‘Methods.' Using a one-way ANOVA nonparametric test, statistical analysis of the desensitization rates of the highly efficacious agonists (all at 1 μM) were compared to 1 μM WIN55,212-2 (P<0.001 (**), P<0.05 (*)). (b) Less efficacious agonists desensitized more slowly than WIN55,212-2. To evaluate whether or not desensitization rates correlate with agonist efficacy, the desensitization rates of agonists and WIN55,212-2 at equally efficacious concentrations were determined. The desensitization rate of 100 nM WIN55,212-2 was not quite statistically different from 1 μM WIN 55,212-2 with P>0.08 (^). 10 μM Δ9-THC, 10 μM AM356, and 1 μM AM411 all desensitized at significantly slower rates compared to 100 nM WIN55,212-2 (P<0.001(**)), however, the desensitization rate of 10 μM 2-AG ether was not statistically different from 100 nM WIN55,212-2 (P>0.17).