Table 3

Repression activities of A276575 and its four enantiomers on ConA-induced proliferation of nontransfected human PBMC

CompoundEC50(n)Dex Efficacy
nM %
A276575 23 ± 15(4)87 ± 2.7  (4)
(−)-Syn enantiomer15 (2)76 (2)
(+)-Syn enantiomer180 ± 69 (3)100 ± 4.6  (3)
(−)-Anti enantiomer 12 ± 3.6 (5)93 ± 1.7  (5)
(+)-Anti enantiomer450 ± 200 (3)88 ± 1.9  (3)
Dexamethasone  1.5 ± 0.19 (5)100  (5)

Values represent the average ± S.E.M. of the number of experiments in parentheses conducted in duplicate. The amount of [3H]thymidine was 10 to 91 and 3,750 to 11,000 dpm/well in the absence and presence of ConA, respectively. The range of test compounds was between 10 pM and 10 μM.