Physicochemical properties of the CYP2D6 substrates and inhibitors
| Compound | pKa1/pKa2 | Ionization Factor | Designation |
|---|---|---|---|
| Bufuralol | 8.97a | 2.472 | Substrate |
| Dextromethorphan | 8.3a | 2.343 | Substrate |
| Quinidine | 4.2/8.8a | 2.456 | Reversible inhibitor |
| Amiodarone | 8.47b | 2.393 | Reversible inhibitor |
| Desethylamiodarone | 9.4b | 2.497 | Reversible inhibitor; time-dependent inhibitor |
| Clozapine | 7.75a | 2.045 | Reversible inhibitor |
| Paroxetine | 9.66a | 2.504 | Reversible inhibitor; time-dependent inhibitor |
| Metoclopramide | 0.6/9.3c | 2.493 | Reversible inhibitor; time-dependent inhibitor |
↵a Source: Simcyp.
↵b Source: The Human Metabolome Database (http://www.hmdb.ca).
↵c Foye et al. (2013).