Effective permeability (Pe), percentage of transport and membrane retention after 4 h in the PAMPA of PLG 1 and its fluorinated analogues 2 and 3a.
| Entry | Compound | P e (× 106)b cm s−1 | Transport (%) (4 h)b | Membrane retentionb |
|---|---|---|---|---|
| 1 | 1 | ndc | ndc | ndc |
| 2 | (S,S)-2 | 2.68 ± 0.04 | 5.34 ± 0.08 | 50% |
| 3 | (R,S)-2 | 0.31 ± 0.03 | 0.65 ± 0.06 | 30% |
| 4 | (S,S,S)-3 | ndc | ndc | ndc |
| 5 | (R,S,S)-3 | ndc | ndc | ndc |
Data are expressed as the mean ± SD.
Parameters definitions and their calculations are provided in Experimental section.
Not determined.