Potency and efficacy values for LPA and analogs using agonist-induced [35S]GTPγS binding mediated by the pertussis toxin-insensitive hEdg2 receptor-rGiα1 fusion protein
| Compound | pEC50 ± S.E. | Maximal LPA Response |
|---|---|---|
| % | ||
| LPA (oleoyl C18:1) | 6.7 ± 0.1 | 100 |
| LPG (oleoyl C18:1) | 5.0 ± 0.1 | 84 ± 3 |
| LPE (oleoyl C18:1) | 5.0 ± 0.2 | 29 ± 2 |
| LPC (oleoyl C18:1) | Inactive | |
| LPE (palmitoyl C16:0) | Inactive | |
| S-1-P | 5.7 ± 0.2 | 22 ± 1 |
Potency (pEC50) and efficacy values (E max) for LPA and related phospholipids in the agonist-induced [35S]GTPγS binding assay were carried out in membranes prepared from PTX treated (100 ng/ml for 20 h before harvesting) hEdg2 receptor-rGiα1 fusion protein transiently expressing HEK cells. Efficacy values are the maximal stimulation achieved and are presented as a percentage of the maximal LPA response. Results are arithmetic means ± S.E. of ≥3 experiments.