Rates of glucuronidation of propranolol enantiomers and their dependence on the presence (racemic mixture) or absence of the other enantiomer
Formation of S-propranolol glucuronide (S-pg) and R-propranolol glucuronide (R-pg) was determined by incubations in the presence of 0.5 mM concentration of the tested enantiomer (in both the presence and absence of the other enantiomer). Values are ±S.D.
Racemic Mixture Reaction Velocity | Individual Enantiomers Reaction Velocity | |||||
|---|---|---|---|---|---|---|
| S-pg | R-pg | S-pg | R-pg | |||
| pmol/mg/min | pmol/mg/min | |||||
| UGT1A1 | 0.7 ± 0.0 | detectable | 0.6 ± 0.1 | 0.3 ± 0.0 | ||
| UGT1A9 | 8.3 ± 0.3 | 1.1 ± 0.1 | 21.6 ± 0.6 | 2.0 ± 0.4 | ||
| UGT1A10 | 5.5 ± 0.8 | 26.8 ± 4.2 | 8.7 ± 1.3 | 36.7 ± 1.7 | ||
| UGT2B4 | 4.9 ± 0.2 | 2.8 ± 0.1 | 5.8 ± 0.1 | 4.1 ± 0.5 | ||
| UGT2B7 | 19.5 ± 0.5 | 25.2 ± 0.6 | 32.9 ± 3.3 | 41.3 ± 2.0 | ||
| UGT2B17 | 1.1 ± 0.2 | detectable | 1.4 ± 0.3 | 0.4 ± 0.0 | ||
| HLM | 70.7 ± 4.9 | 50.4 ± 3.2 | 74.2 ± 8.9 | 47 ± 1.8 | ||
| HIM | 7.3 ± 0.7 | 13.1 ± 1.2 | 10.0 ± 2.8 | 21.8 ± 1.8 | ||