Table 1.
L-α-amino acid | EC50 (μM) | pEC50±s.e.m. | N | Concentration of L-α-amino acid (mean±s.d.) in mouse plasmaa (μM) |
---|---|---|---|---|
L-Orn | 63.6 | 4.20±0.001 | 3 | 86±20 |
L-Lys | 135 | 3.97±0.18 | 4 | 366±55 |
L-Arg | 284 | 3.58±0.08b | 6 | 137±22 |
L-Cys | 356c | 3.46±0.09b | 3 | Not determined |
L-Ala | 486 | 3.41±0.18b,d | 4 | 431±85 |
Gly | 538e | 3.30±0.09b,f | 4 | 340±54 |
L-Ser | 1160g | 2.94±0.03b,d,f | 3 | 181±25 |
The IP turnover assay was used to determine the EC50 values of various amino acids at mGPRC6A. The pEC50 values of all the listed amino acids were compared to determine statistically significant differences (P<0.05; ANOVA followed by Tukey's test).
Taken from Komarov and Reddy (1998).
Significantly different from L-Orn.
L-Cys displayed a small but significant effect on mock-transfected cells at high concentrations (⩾1 mM). The EC50 value might thus be overestimated.
Significantly different from L-Lys.
Gly displayed partial agonism with a maximal response of 49±9% (mean±s.e.m.) relative to the maximal activation of mGPRC6A obtained by stimulation with 10 mM L-Arg.
Significantly different from L-Arg.
Owing to low potency, L-Ser was tested at concentrations eliciting sub-maximal effect. Assuming full agonism, concentration–response curves for this compound were fitted using the maximal response to L-Arg (10 mM), which was always included as control.