The effect of various inhibitors of 5-HT2Areceptor-mediated PLC and PLA2 activation
| Inhibitor | Concentration | PLA2-AA Release | PLC-IP Accumulation |
|---|---|---|---|
| μM | % max over basal | ||
| Control | 100 | 100 | |
| Mepacrine | 30 | 43 (8.4)1-150 | 120 (3.8) |
| ET-18 | 10 | 100 (8.2) | 28 (5.3)*** |
| RHC-80267 | 10 | 92 (9.9) | 81 (8.1) |
| Staurosporine | 0.1 | 95 (11) | 110 (7.1) |
The effect of PLA2 inhibition (mepacrine), PLC inhibition (ET-18), DAG lipase inhibition (RHC-80267), and PKC inhibition (staurosporine) on PLA2-AA release and PLC-IP accumulation. NIH3T3–5HT2A cells were preincubated with vehicle (control) or inhibitor for 15 min prior to the addition of 5-HT (10 μM) for 30 min. The data represent the mean (S.E.M.) of at least three independent experiments.
↵1-150 P < 0.05, ***P < 0.001 compared with a hypothetical value of 100 (one-sample ttest).