TABLE 5

Region 4 SAR studies

Embedded ImageXHα4β2 nAChRsHα3β4 nAChRs
IC50 Value (μM)anHIC50 Value (μM)anH
KAB-18Embedded Image13.5 (9.7–18.5)−0.7NAc
DDR-5Embedded Image19.8 (8.3–47.1)−0.8NAc
DDR-3Embedded Image16.6 (9.7–28.6)−0.914.5 (4.9–43.1)−0.7
JHB-9Embedded Image17.6 (11.6–26.8)−0.910.2 (3.4–30.5)−0.9
APB-21Embedded Image12.6 (3.0–53.8)−0.815.5 (8.4–29.0)−0.9
DDR-14Embedded Image6.4 (4.1–10.4)−1.12.7 (0.4–17.9)−1.2
  • nH, Hill coefficient; NA, no activity at concentrations up to 100 μM.

  • a Values represent geometric means (confidence limits), n = 4–8.