TABLE 1

Ligand potencies at the wild type and mutant ghrelin receptors

Data represent the mean ± S.E.M. from at least four independent experiments using a luciferase reporter gene assay; each experiment was performed in triplicate.

Ligand Wild Type I134T V160M A204E F279L
EC50a pEC50 ± S.E.M. EC50a pEC50 ± S.E.M. EC50a pEC50 ± S.E.M. EC50a pEC50 ± S.E.M. EC50a pEC50 ± S.E.M.
Ghrelin 75.2 7.12 ± 0.3 No stimulation 3.8 8.42 ± 0.29b 92.3 7.04 ± 0.13 34.9 7.36 ± 0.29
SP analog 41.8 7.38 ± 0.16 203.0 6.69 ± 0.41b 12.1 7.92 ± 0.51 No inhibition 30.4 7.52 ± 0.60
  • a Half-maximal effective concentration (nanomolar).

  • b p < 0.05 versus wild-type value.