TABLE 1

IC50 values for AM211 in the in vitro assays

All IC50 values are the mean ± S.D. with n values indicated in parentheses.

ReceptorIC50
nM
[3H]PGD2 radioligand membrane binding
    Human DP24.9 ± 1.3 (6)
    Mouse DP27.8 ± 2.2 (4)
    Guinea pig DP24.9 ± 1.9 (4)
    Rat DP210.4 ± 2.8 (3)
    Human DP2 + human SAa12.2 ± 3.4 (6)
    Mouse DP2 + mouse SAa20.1 ± 8.8 (5)
    Guinea pig DP2 + guinea pig SAa22.9 ± 6.0 (4)
    Rat DP2 + rat SAa34.2 ± 13.8 (3)
Human DP2 [35S]GTPγS binding13.3 ± 3.7 (6)
In vitro functional assays
    Human whole blood ESC2.7 ± 0.9 (7)
    Guinea pig whole blood ESC21.5 (2)b
    Human basophil CD203c2.5 (2)b
  • a Potency determined in the presence of 0.2% species-specific serum albumin (SA).

  • b S.D. not calculated for studies involving n values of <3.