Potency and efficacy of leukotrienes at CysLT2 receptors
EC50 values are presented as mean ± S.E.M.
| Mouse CysLT2 Receptor Aequorin Assay | Human CysLT2 Receptor | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Aequorin Assay | β-Arrestin Assay | ||||||||
| Potency EC50 (n = 3) | Pctg of Max Efficacy (Avg, n = 3) | Fold Diff EC50 Agonist/EC50 LTC4 | Potency EC50 (n = 3) | Pctg of Max Efficacy (Avg, n = 3) | Fold Diff EC50 Agonist/EC50 LTC4 | Potency EC50 (n = 6–8) | Pctg of Max Efficacy (Avg, n = 6–8) | Fold Diff EC50 Agonist/EC50 LTC4 | |
| nM | % @ μM | nM | % @ μM | nM | % @ μM | ||||
| LTC4 | 38.6 ± 6.1 | 100 @ 1.5 | 1 | 94.6 ± 19.9 | 100 @ 1 | 1 | 54.4 ± 9.6 | 100 @ 0.8 | 1 |
| NMLTC4 | 46.1 ± 8.7 | 89 @ 1.5 | 1.2 | 122.3 ± 27.1 | 98 @ 3 | 1.3 | 8.7 ± 4.5 | 90 @ 0.8 | 0.16 |
| LTD4 | 49.2 ± 12.6 | 85 @ 1.5 | 1.3 | 144.9 ± 66.1 | 89 @ 3 | 1.5 | 34.7 ± 5.7 | 90 @ 0.9 | 0.64 |
| LTE4a | 146 ± 16.7 | 29 @ 1.5 | 3.8 | 1208 ± 554.2 | 45 @ 10 | 12.8 | |||
Pctg, percentage; Max, maximal; Diff, difference; Avg, average.
↵a Partial agonist.