TABLE 1

Effect of Salvinorin A derivatives on KOR subtype binding and KOR-1-stimulated Ca2+ mobilization KOR-2 binding experiments were done as described under Materials and Methods. The salvinorin A derivatives were screened using a large panel of cloned human receptors, ion channels, and transporters (see Roth et al., 2002 for list) and were inactive (data not shown)

Drug
Ki at KOR-1
Ki at KOR-2A
Ki at KOR-2B
pEC50a
Emax a
nM ± S.E.M. nM ± S.D.
U69,593 0.7 ± 0.05b 121 ± 10c >10,000c 1.14 ± 0.02 100
U50,488H 0.2 ± 0.05b 55.6 ± 7.4c 20,400 ± 5160c 1.39 ± 0.14 102 ± 4
Salvinorin A 18.7 ± 3.4a >10,000 >10,000 0.84 ± 0.07 104 ± 7
Salvinorinyl-2-propionate 32.6 ± 15.7a ND ND 1.23 ± 0.18 102 ± 8
Salvinorin B
>10,000a
>10,000
>10,000
NA
NA

  • NA, no activity; ND, not done

  • ↵ a The results for KOR-1 binding and KOR-1-stimulated Ca2+ mobilization are taken from Chavkin et al. (2004)

  • ↵ b Data from Toll et al. (1998)

  • ↵ c Data from Rothman et al. (1990)