EC50 and IC50 values of recombinant and chimeric 5-HT3 receptors for various agonists and antagonists
| 5-HT3receptor | 5-HT | 2-Me-5-HT | PBG | mCPBG | Metoclopramide | Tropisetron |
|---|---|---|---|---|---|---|
| μm | nm | |||||
| H | 2.3 ± 0.2 | 2.8 ± 0.5 | 41.2 ± 4 | 1.9 ± 0.2 | 0.29 ± 0.01 | 0.59 ± 0.07 |
| M1 | 2.9 ± 0.2 | 2.3 ± 0.2 | 12.5 ± 1.1 | 0.55 ± 0.18 | 0.11 ± 0.01 | 0.19 ± 0.003 |
| GP1 | 2.9 ± 0.1 | 2.7 ± 0.1 | >1000 | 13.3 ± 0.1 | 3.4 ± 0.3 | 9.2 ± 0.4 |
| GP2 | 3.8 ± 0.3 | 2.5 ± 0.1 | >1000 | 15.1 ± 0.3 | 5.6 ± 0.5 | 9.3 ± 0.5 |
| C1 | 1.3 ± 0.08 | 21.8 ± 1.4 | ||||
| E4 | 1.28 ± 0.06 | 19.3 ± 7.2 | ||||
Antagonists were tested in the presence of 10 μm 5-HT. Transfected HEK 293 cells were recorded at a holding potential of −50 mV. The data were obtained from 4 to 11 independent experiments. Values are presented as mean ± standard error.