Table 2

Transport and calcein-AM results for CNS-indicated drugs

NameTherapeutic Indication2-aMean Papp A→BbS.D.MeanPapp B→AS.D.B→A/A→B RatioMeanPapp+ GF120918S.D.B→A/A→B RatioPgp SubstrateCalcein-AM ResultCalcein-AM Interaction
(nm/s) (nm/s) (nm/s) (% max)
Amantadineantiviral antiparkinsonian4277.924056.400.953301.630.76N2.10c N
Biperidenantiparkinsonian5151.2249166.80.9547414.40.89N4.97N
Carbamazepineanticonvulsant6024.7759284.80.9856720.71.13N1.22N
Flumazenilbenzodiazepine antagonist59794.855243.80.9248454.70.88N3.89N
Imipramineantidepressant39388.641438.21.054848.421.04N5.37N
Ketamineanesthetic7488.316951270.9372823.20.93N1.23N
Meprobamateanxiolytic34449.933424.20.9725439.90.95N2.24N
Naloxonenarcotic antagonist49516.86382321.2942123.20.87N0.73N
Naltrexonenarcotic antagonist40249.541849.31.0447118.91.03N2.03N
Nitrazepamanticonvulsant38989.945693.11.1752668.00.95N3.66N
Nordazepamanxiolytic64767.760217.10.936853.701.01N5.17N
Scopolamineantiemetic17141.11941.661.141659.681.05N0.54N
Selegilineantiparkinsonian70313653548.60.7668347.71.23N3.02N
Sumatriptananti-migraine3.990.165.880.601.485.000.111.32N0.76N
Tacrinecognitive stimulant43898.040934.50.934423.270.79N4.76
Zimeldineantidepressant67630.568531.91.0166243.51.04N7.40N
Amitriptyllineantidepressant47434.963622.21.346034.761.44N25.5Y
Bromocriptineantiparkinsonian194d 5.062456.191.26182e 4.891.04N61.6Y
Buspironeanxiolytic54710.35175.800.956391.340.91N24.1Y
Chlorpromazineantipsychotic303e 67.738517.31.2742421.01.23N46.9Y
Chlorprothixeneantipsychotic260e 12.532860.91.2645523.81.52N57.5Y
Clomipramineantidepressant369e 63.55261211.425721.651.10N48.2Y
Desipramineantidepressant55131.556824.21.0344135.00.94N12.8Y
Doxepinantidepressant5423.8262277.31.158472641.31N15.3Y
Fluoxetineantidepressant52145.16179.191.1851121.40.93N23.5Y
Flurazepamanxiolytic70549.762123.40.8861632.00.83N22.6Y
Fluvoxamineantidepressant317e 22.938033.41.204881391.18N20.8Y
Haloperidolantipsychotic55630.057919.21.045906.850.94N37.2Y
Maprotilineantidepressant45592.948082.81.0552461.11.17N36.7Y
Metergolineanalgesic antipyretic179d 52.0216e 19.41.21216e 32.41.19N84.4Y
Midazolamanesthetic60911461350.81.0161341.11.05N74.9c Y
Nortriptyleneantidepressant337e 56.446880.31.394266.321.05N13.7c Y
Noscapineantitussive64271.066198.21.0348310.60.97N35.5Y
Perphenazineantipsychotic305e 6.0144927.51.4740631.71.36N65.4Y
Procyclidineantiparkinsonian7036.0366515.70.9562686.11.02N16.2Y
Progabideanticonvulsant68450.96017.690.8866220.10.95N14.1Y
Promazineantipsychotic336e 23.438828.51.1542167.91.17N16.3Y
Toxindoleantidepressant51918.359846.01.155439.631.00N32.7Y
Trazodoneantidepressant7472.2669867.50.946104.330.84N21.1Y
Trimipramineantidepressant40531.737264.80.9247018.41.16N22.8Y
Zolpidemsedative6941047885.191.1466920.00.83N17.3Y
Eletriptanantimigraine14.80.4966349.044.742916.71.09Y2.60N
Methysergideantimigraine1749.587535.274.3339417.20.97Y3.83N
Nalbuphineanalgesic1407.693037.952.171560.131.01Y−0.07N
Zolmitriptanantimigraine2.520.016.250.012.482.170.501.24Y−1.01N
Levomeprazineantipsychotic347e 17.953566.71.5447810.71.26Y25.6Y
Protriptyleneantidepressant25910.861379.22.3734614.31.01Y15.0Y
Ripseridoneantipsychotic38960.362723.81.6153614.10.97Y52.6Y
  • Drugs in the table are grouped by response (Y = Yes and N = No) in the Pgp efflux and calcein-AM assays as described underMaterials and Methods.

  • 2-a Therapeutic Indication was taken from The Merck Index, 2001; b mass balance for drugs was > 70% except where noted; c data taken from Polli et al. (2001b); d mass balance for this drug was 40 to 50%;e mass balance for this drug was 50 to 70%.