Compound, mode of action, doses, study period, molecular weight, and unbound fraction in rats
Unbound fractions from in-house data and FDA approval documentation (www.pharmapendium.com).
| Compound | Mode of Action | Doses | Study Period | Molecular Weight | fu |
|---|---|---|---|---|---|
| mg kg-1 | h | g mol−1 | |||
| Ivabradine | Blocks If and HCN channels in SAN | 0, 3, 10, 30 | 24 | 468.6 | 0.25 |
| Sildenafil | PDE5-inhibitor | 0, 3, 10, 30 | 7 | 474.6 | 0.05 |
| Dofetilide | IKr-channel blocker | 0, 1, 3, 10 | 7 | 441.6 | 0.2 |
| Pimobendan | Ca2+ sensitizer, PDE3-inhibitor | 0, 1, 3, 10 | 24 | 334.4 | 0.05 |
fu, unbound fraction of test compounds in rats; HCN, hyperpolarization-activated cyclic nucleotide–gated channels; If, funny current; SAN, sinoatrial node.