Table 1: Parameters of GRABeCB2.0 activation and antagonism.
Live cell images of GRABeCB2.0-expressing HEK293 cells treated with 2-AG (1 μM), AEA (10 μM), or CP (1 μM), followed by SR1 (2 μM) on agonist-stimulated increase in GRABeCB2.0 fluorescent signal. Calculation of the activation onset (i.e., the slope of the fluorescent signal increase within the first 20 sec after start of agonist treatment), the magnitude of the response (i.e., peak response and area under the curve), and the decay following SR1 treatment (i.e., τ value following treatment). Analysis of data presented in Figure 1, n= 42–66 cells from 3–5 independent experiments.
| CB1R agonists | ||||
|---|---|---|---|---|
| PD parameter | Units | 2-AG | CP | AEA |
| Initial response: slope | (× 10−2 DF/F0/sec) | 6.6 | 4.5 | 10.9 |
| Maximal response: peak | (DF/F0) | 2.5 | 1.7 | 2.7 |
| Overall response | (area under the curve) | 649 | 453 | 760 |
| Antagonism response: t | (sec) | 42.7 | 24.3 | 36.8 |