Table 2.

Functional activity at hTAAR1 receptor and cytotoxicity against Vero-76 of compounds 1–16.

Compound	hTAAR1 Activity a	hTAAR1 b EC50, nM	Vero-76 Cells c CC50, µM
1	71%	370	84 ± 5
2	100%	30	80 ± 5
3	90%	160	> 100
4	35%	>2000	90 ± 3
5	inactive	-	95 ± 3
6	64%	93	83 ± 5
7	32%	244	87 ± 4
8	inactive	-	88 ± 2
9	80%	64	>100
10	30%	>2000	74 ± 5
11	inactive	-	64 ± 2
12	inactive	-	78 ± 2
13	inactive	-	87 ± 5
14	inactive	-	94 ± 6
15	81%	20	82 ± 5
16	49%	71	89 ± 4
TYR	100%	66	-

^a As compared with 1 µM TYR (full agonism); ^b Data are representative of four independent experiments and are expressed as means (errors on EC₅₀ are within 10%). ^c Compound concentration (µM) required to reduce the viability of Vero-76 cells by 50% as determined by the MTT method. The results are expressed as CC₅₀±SEM of three separate experiments performed in duplicate.