TABLE 3

Agonist profile of ABT-107 at nAChRs assayed by FLIPR Ca2+ imaging

Receptor, Assay TypeEC50 (nM); Maximal Effecta vs. 100 μM (−)-Nicotinen
α4β2, Human, HEK-293>100,000; 4 ± 1%14
α3β4*, Human, IMR-32>100,000; 6 ± 1%14
α4β4, Human, HEK-2932700 (2000–3400); 12 ± 1%9
α7, Rat cortical cultures, with A-86774410.9 (6.8–17.3)5
α7, Human, IMR-32
    with A-86774412.6 (10.8–14.7)4
    with PNU-1205960.7 (0.5–0.9)5
    with PNU-120596 + MLA10.4 (8.1–13.2)5
  • a Values are expressed as means with 95% CIa or mean ± S.E.M.