Table 1.
Comparison of half-maximal concentrations for binding at and functional activation of human MCH-1R and MCH-2R by MCH, Phe13Tyr19-MCH, and salmon MCH
| Ligand | Binding IC50, nM ± SEM (n)
|
Function EC50, nM ± SEM (n)
|
||
|---|---|---|---|---|
| MCH-1R | MCH-2R | MCH-1R | MCH-2R | |
| MCH | 0.3 ± 0.1 (10) | 1.5 ± 0.9 (8) | 3.9 ± 1.2 (3) | 0.1 ± 0.1 (3) |
| Phe13Tyr19-MCH | 0.3 ± 0.1 (3) | 0.8 ± 0.1 (3) | 8.5 ± 0.9 (3) | 0.2 ± 0.1 (3) |
| Salmon MCH | 0.2 ± 0.1 (5) | 436.7 ± 143.8 (3) | 35.0 ± 14.8 (3) | 0.8 ± 0.1 (3) |
Membrane binding was assessed by competition of [125I]Phe13Tyr19-MCH in a scintillation proximity assay. Functional activation was measured by mobilization of intracellular calcium detected in a fluorometric imaging plate reader assay. Values shown are nanomolar concentrations and averaged from at least three independent experiments.