. Author manuscript; available in PMC: 2011 Apr 1.

Published in final edited form as: J Med Chem. 2011 Feb 4;54(5):1308–1313. doi: 10.1021/jm1013049

Table 1.

Ca²⁺ Mobilization and in Vitro Physiological (RTCA) Assays

		[Ca²⁺]_i measurements
	R-CO-Leu-Ile-Gly-Arg-Leu-NH₂^a	% response 100 μM	% response 10 μM	% response 2.5 μM	EC₅₀ (μM)	xRTCA^b 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.