Table 4.
Compound | at pH 7.4 |
Human liver microsome t1/2 min |
|
---|---|---|---|
Water Solubility (μg/mL) |
Log P | ||
4f | 0.81 ± 0.01 | 4.02 ± 0.11 | ND c |
4i | 0.16 ± 0.03 | 4.33 ± 0.12 | ND |
5f | 0.26 ± 0.05 | 4.75 ± 0.09 | ND |
6b | 3.21 ± 0.60 | 3.98 ± 0.02 | 7.89 |
6c | 7.67 ± 0.40 | 3.65 ± 0.03 | 25.19 |
6d | 0.45 ± 0.06 | 4.13 ± 0.05 | 10.59 |
6e | 7.21 ± 0.06 | 1.07 ± 0.21 | 25.97 |
| |||
Propranolola | 40.82 | ||
| |||
Terfenadineb | 21.14 |
Data presented as mean from three separate experiments with or without ± standard deviation (SD).
Propranolol has moderate metabolic stability with t1/2 of 3–5 h in vivo;
Terfenadine has fast metabolic stability with t1/2 of < 3 h in vivo.
Not determined.