TABLE 5

Estimated equilibrium parameters and predicted EC20 values in rats and free conc. Cu in human

t1/2,kout from Table 4 are included for convenience. Cu denotes clinical plasma conc. in humans. All conc. are unbound.

CompoundResponseEmax/ImaxEC50/IC50γEC20/IC20Cut1/2,kout
nMnMnMmin
IvabradineHR (I)30611000.40335.75.3–23a1.4
MAP (I)53400,0000.3366460
SildenafilHR (E)11608370.47846.110–47b1.4
MAP (I)1038370.47846.1
DofetilideQT (E)12.550.60.1560.00730.45–4.5c4.4
PimobendanHR (E)1381440.4898.500.95–1.9d1.4
MAP (I)12.41440.4898.50
  • E, excitatory response; I, inhibitory response; t1/2,kout, equivalent half-lives for kout.

  • a Deedwania (2013).

  • b VIAGRA, Pfizer summary.

  • c Allen et al. (2000).

  • d Chu et al. (1995).