Table 1. Pharmacological Data of Fragments 1a, 2a, and 3aa.
1a | 2a | 3a | ||
---|---|---|---|---|
Ki (μM) | α4β2 | ∼300 | 3.4 (5.46 ± 0.07) | ∼30 |
α4β4 | >300 | ∼100 | >300 | |
α3β4 | >300 | ∼300 | >300 | |
IC50 (μM) | α4β2 | >300 | ∼30 | ∼100 |
α3β4 | >300 | >300 | >300 |
The Ki values obtained for the compounds in the [3H]epibatidine binding assays are given in μM (with pKi ± S.E.M. value in the bracket). The IC50 values obtained for the compounds at α4β2 and α3β4 in the FMP assay are given in μM. The data are the means of 3–4 individual experiments.