TABLE 3

Papp in PAMPA and Papp, A>B values in MDCK assays for 32 CNS-active drugs Data are presented as mean ± S.D.


Compound

PAMPA Retention Factor (Rf)

PAMPA Papp

A > B Papp in MDCK
× 10-6 cm/s × 10-6 cm/s
Buspirone 0.5 ± 0.04 27.1 ± 19.95 23.3 ± 3.91
Caffeine N.D. N.D. 30.6 ± 2.47
Carbamazepine 0.2 ± 0.05 17.3 ± 2.38 29.4 ± 2.46
Carisoprodol 0.2 ± 0.06 16.2 ± 2.57 25.6 ± 2.86
Chlorpromazine 0.9 ± 0.03 6.1 ± 1.64 4.1 ± 0.44
Citalopram 0.5 ± 0.04 14.5 ± 3.74 18.3 ± 3.76
Cyclobenzaprine 0.8 ± 0.04 13.0 ± 2.49 12.2 ± 0.34
Diazepam 0.5 ± 0.03 17.4 ± 3.18 27.7 ± 2.45
Ethosuximide 0.1 ± 0.12 10.0 ± 1.24 26.8 ± 2.59
Fluoxetine 0.3 ± 0.08 0.1 ± 0.03 6.3 ± 0.61
Fluvoxamine 0.8 ± 0.06 10.0 ± 0.35 13.0 ± 2.69
Haloperidol 0.8 ± 0.04 8.6 ± 1.30 12.3 ± 3.31
Hydrocodone 0.2 ± 0.08 11.9 ± 0.25 20.0 ± 1.77
Hydroxyzine 0.6 ± 0.01 12.5 ± 0.56 16.1 ± 3.25
Lamotrigine N.D. N.D. 22.9 ± 0.97
Methylphenidate 0.3 ± 0.04 23.2 ± 6.53 24.7 ± 2.03
Metoclopramide 0.4 ± 0.05 11.0 ± 1.27 17.7 ± 2.61
Midazolam 0.5 ± 0.02 13.1 ± 1.28 22.5 ± 2.08
Morphine 0.2 ± 0.05 4.8 ± 0.78 1.8 ± 0.07
Nortriptyline 0.8 ± 0.06 10.1 ± 2.51 9.1 ± 0.16
Paroxetine 0.9 ± 0.01 5.7 ± 1.08 6.1 ± 0.29
Phenytoin 0.3 ± 0.03 15.2 ± 0.63 24.0 ± 1.80
Propoxyphene 0.6 ± 0.04 13.1 ± 1.08 21.9 ± 4.65
Risperidone 0.5 ± 0.05 13.8 ± 0.50 19.8 ± 3.24
9-Hydroxyrisperidone N.D. N.D. 16.8 ± 1.04
Selegiline 0.6 ± 0.04 26.1 ± 11.91 23.2 ± 1.46
Sertraline 0.9 ± 0.02 2.8 ± 0.50 1.9 ± 0.37
Sulpiride 0.01 ± 0.01 0.03 ± 0.03 0.9 ± 0.47
Thiopental 0.5 ± 0.02 21.1 ± 6.39 25.2 ± 1.15
Trazodone 0.5 ± 0.03 13.6 ± 1.07 19.7 ± 0.64
Venlafaxine N.D. N.D. 22.1 ± 0.77
Zolpidem
0.4 ± 0.03
15.7 ± 1.45
23.4 ± 0.76
  • N.D., no data were generated.