Table 1.
[Ca2+]i measurements |
||||||
---|---|---|---|---|---|---|
R-CO-Leu-Ile-Gly-Arg-Leu-NH2a | % response 100 μM |
% response 10 μM |
% response 2.5 μM |
EC50 (μM) | xRTCAb EC50 (nM) |
|
2-furoyl-Leu-Ile-Gly-Arg-Leu-Orn(Aloc)-NH2 | 100 ± 0 | 97.8 ± 1.0 | 93.6 ± 3.3 | 0.84 ± 0.08 | 138 ± 13 | |
1 | 2-aminothiazol-4-yl | 100 ± 0 | 96.2 ± 1.4 | 67.5 ± 7.5 | 1.77 ± 0.24 | 142 ± 18 |
2 | 6-aminonicotinyl | 100 ± 0 | 93 ± 2.0 | 55 ± 11.6 | 2.60 ± 0.32 | 311 ± 26 |
3 | 6-aminopyridin-2-yl | 99.3 ± 0.7 | 94.4 ± 2.6 | 27.1 ± 6.9 | 3.50 ± 0.36 | ND |
4 | 4-aminophenyl | 93.0 ± 0.3 | 86.9 ± 4.1 | 16.5 ± 5.3 | 6.59 ± 1.7 | ND |
The structures do not contain C-terminal Orn as 2-furoyl-Leu-Ile-Gly-Arg-Leu-Orn(Aloc)-NH2.
EC50 = concentration of compound that was able to generate 50% maximal intracellular activity. Values are expressed ± SEM (N ≥ 2 for 100 μM; N ≥ 4 for all others in Ca2+ assay; data are expressed % response ± SEM; N ≥ 8 in the RTCA assay). ND = not determined.