Table 1.
Comparison of binding affinities and EC50 values of p-tyr and EPPTB at human and rodent TAAR1
| Compound | Parameter, assay, preparation | Mouse | Rat | Human |
|---|---|---|---|---|
| p-tyr | Ki, binding, HEK293* | 404 ± 129 | 70 ± 12 | nd |
| EC50, cAMP, HEK293† | 545 ± 179 | 125 ± 36 | 1664 ± 135 | |
| EC50, GIRK, Xenopus oocytes‡§ | 167 ± 24 | nd | nd | |
| EC50, patch-clamp, VTA slices§ | 305 ± 11 | nd | nd | |
| EPPTB | Ki, binding, HEK293* | 0.9 ± 0.1 | 942 ± 133 | nd |
*Radioligand [3H]-rac-2-(1,2,3,4-tetrahydro-1-naphthyl)-2-imidazoline (12).
†Biotrak Enzyme Immunoassay for cAMP.
‡Current mediated by Kir3.1 and Kir3.2 co-expressed with TAAR1.
§Current at −50 mV holding potential; nd, not determined. Values are given as nM (mean ± SEM). The results were obtained from at least four independent experiments.