메뉴 건너뛰기




Volumn 11, Issue 4, 2011, Pages 450-466

Do we need to optimize plasma protein and tissue binding in drug discovery?

Author keywords

And tissue binding; Clearance; Drug design; Free unbound drug concentration; Plasma protein binding

Indexed keywords

DRUG BINDING PROTEIN; PLASMA PROTEIN;

EID: 79551662332     PISSN: 15680266     EISSN: None     Source Type: Journal    
DOI: 10.2174/156802611794480918     Document Type: Article
Times cited : (40)

References (60)
  • 1
    • 21444433359 scopus 로고    scopus 로고
    • Strategies to optimize brain penetration in drug discovery
    • Liu, X.; Chen, C. Strategies to optimize brain penetration in drug discovery. Curr. Opin. Drug Discov. Devel., 2005, 8, 505-512.
    • (2005) Curr. Opin. Drug Discov. Devel , vol.8 , pp. 505-512
    • Liu, X.1    Chen, C.2
  • 2
    • 34447503927 scopus 로고    scopus 로고
    • The importance of plasma protein binding in drug discovery
    • Trainor, G. The importance of plasma protein binding in drug discovery. Expert. Opin. Drug Discov., 2007, 2, 51-64.
    • (2007) Expert. Opin. Drug Discov , vol.2 , pp. 51-64
    • Trainor, G.1
  • 4
    • 38849136513 scopus 로고    scopus 로고
    • CSF as a surrogate for assessing CNS exposure: An industrial perspective
    • Lin, J. H. CSF as a surrogate for assessing CNS exposure: an industrial perspective. Curr. Drug Metab., 2008, 9, 46-59.
    • (2008) Curr. Drug Metab , vol.9 , pp. 46-59
    • Lin, J.H.1
  • 5
    • 76649085489 scopus 로고    scopus 로고
    • Significance of protein binding in pharmacokinetics and pharmacodynamics
    • Schmidt, S.; Gonzalez, D.; Derendorf, H. Significance of protein binding in pharmacokinetics and pharmacodynamics. J. Pharm. Sci., 2010, 99, 1107-1122.
    • (2010) J. Pharm. Sci , vol.99 , pp. 1107-1122
    • Schmidt, S.1    Gonzalez, D.2    Derendorf, H.3
  • 6
    • 42449100856 scopus 로고    scopus 로고
    • Progress in brain penetration evaluation in drug discovery and development
    • Liu, X.; Chen, C.; Smith, B. J. Progress in brain penetration evaluation in drug discovery and development. J. Pharmacol. Exp. Ther., 2008, 325, 349-356.
    • (2008) J. Pharmacol. Exp. Ther , vol.325 , pp. 349-356
    • Liu, X.1    Chen, C.2    Smith, B.J.3
  • 7
    • 0037407697 scopus 로고    scopus 로고
    • Development and validation of a 96-well equilibrium dialysis apparatus for measuring plasma protein binding
    • Banker, M. J.; Clark, T. H.; Williams, J. A. Development and validation of a 96-well equilibrium dialysis apparatus for measuring plasma protein binding. J. Pharm. Sci., 2003, 92, 967-974.
    • (2003) J. Pharm. Sci , vol.92 , pp. 967-974
    • Banker, M.J.1    Clark, T.H.2    Williams, J.A.3
  • 8
    • 0035038596 scopus 로고    scopus 로고
    • Development of a high throughput equilibrium dialysis method
    • Kariv, I.; Cao, H.; Oldenburg, K. R. Development of a high throughput equilibrium dialysis method. J. Pharm. Sci., 2001, 90, 580-587.
    • (2001) J. Pharm. Sci , vol.90 , pp. 580-587
    • Kariv, I.1    Cao, H.2    Oldenburg, K.R.3
  • 9
    • 0141537961 scopus 로고    scopus 로고
    • Semi-automatic highthroughput determination of plasma protein binding using a 96-well plate filtrate assembly and fast liquid chromatography-tandem mass spectrometry
    • Fung, E. N.; Chen, Y. H.; Lau, Y. Y. Semi-automatic highthroughput determination of plasma protein binding using a 96-well plate filtrate assembly and fast liquid chromatography-tandem mass spectrometry. J. Chromatogr. B Analyt. Technol. Biomed. Life. Sci., 2003, 795, 187-194.
    • (2003) J. Chromatogr. B Analyt. Technol. Biomed. Life. Sci , vol.795 , pp. 187-194
    • Fung, E.N.1    Chen, Y.H.2    Lau, Y.Y.3
  • 10
    • 29044432751 scopus 로고    scopus 로고
    • High-throughput screening of protein binding by equilibrium dialysis combined with liquid chromatography and mass spectrometry
    • Wan, H.; Rehngren, M. High-throughput screening of protein binding by equilibrium dialysis combined with liquid chromatography and mass spectrometry. J. Chromatogr. A, 2006, 1102, 125-134.
    • (2006) J. Chromatogr. A , vol.1102 , pp. 125-134
    • Wan, H.1    Rehngren, M.2
  • 11
    • 55749099657 scopus 로고    scopus 로고
    • Validation of a rapid equilibrium dialysis approach for the measurement of plasma protein binding
    • Waters, N. J.; Jones, R.; Williams, G.; Sohal, B. Validation of a rapid equilibrium dialysis approach for the measurement of plasma protein binding. J. Pharm. Sci., 2008, 97, 4586-4595.
    • (2008) J. Pharm. Sci , vol.97 , pp. 4586-4595
    • Waters, N.J.1    Jones, R.2    Williams, G.3    Sohal, B.4
  • 12
    • 17144395222 scopus 로고    scopus 로고
    • Predicting human serum albumin affinity of interleukin- 8 (CXCL8) inhibitors by 3D-QSPR approach
    • Aureli, L.; Cruciani, G.; Cesta, M. C.; Anacardio, R.; De Simone, L.; Moriconi, A. Predicting human serum albumin affinity of interleukin- 8 (CXCL8) inhibitors by 3D-QSPR approach. J. Med. Chem., 2005, 48, 2469-2479.
    • (2005) J. Med. Chem , vol.48 , pp. 2469-2479
    • Aureli, L.1    Cruciani, G.2    Cesta, M.C.3    Anacardio, R.4    de Simone, L.5    Moriconi, A.6
  • 13
    • 33846230530 scopus 로고    scopus 로고
    • Plasma protein binding affinity and its relationship to molecular structure: An in-silico analysis
    • Gleeson, M. P. Plasma protein binding affinity and its relationship to molecular structure: an in-silico analysis. J. Med. Chem., 2007, 50, 101-112.
    • (2007) J. Med. Chem , vol.50 , pp. 101-112
    • Gleeson, M.P.1
  • 14
    • 33845748281 scopus 로고    scopus 로고
    • Genetic algorithm-optimized QSPR models for bioavailability, protein binding, and urinary excretion
    • Wang, J.; Krudy, G.; Xie, X. Q.; Wu, C.; Holland, G. Genetic algorithm-optimized QSPR models for bioavailability, protein binding, and urinary excretion. J. Chem. Inf. Model, 2006, 46, 2674-2683.
    • (2006) J. Chem. Inf. Model , vol.46 , pp. 2674-2683
    • Wang, J.1    Krudy, G.2    Xie, X.Q.3    Wu, C.4    Holland, G.5
  • 15
    • 2642548329 scopus 로고    scopus 로고
    • Computational prediction of the plasma protein-binding percent of diverse pharmaceutical compounds
    • Yamazaki, K.; Kanaoka, M. Computational prediction of the plasma protein-binding percent of diverse pharmaceutical compounds. J. Pharm. Sci., 2004, 93, 1480-1494.
    • (2004) J. Pharm. Sci , vol.93 , pp. 1480-1494
    • Yamazaki, K.1    Kanaoka, M.2
  • 17
    • 0242290408 scopus 로고    scopus 로고
    • Fast gradient HPLC method to determine compounds binding to human serum albumin. Relationships with octanol/water and immobilized artificial membrane lipophilicity
    • Valko, K.; Nunhuck, S.; Bevan, C.; Abraham, M. H.; Reynolds, D. P. Fast gradient HPLC method to determine compounds binding to human serum albumin. Relationships with octanol/water and immobilized artificial membrane lipophilicity. J. Pharm. Sci., 2003, 92, 2236-2248.
    • (2003) J. Pharm. Sci , vol.92 , pp. 2236-2248
    • Valko, K.1    Nunhuck, S.2    Bevan, C.3    Abraham, M.H.4    Reynolds, D.P.5
  • 19
    • 46449114275 scopus 로고    scopus 로고
    • Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds
    • Obach, R. S.; Lombardo, F.; Waters, N. J. Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. Drug Metab. Dispos., 2008, 36, 1385-1405.
    • (2008) Drug Metab. Dispos , vol.36 , pp. 1385-1405
    • Obach, R.S.1    Lombardo, F.2    Waters, N.J.3
  • 20
    • 0018190444 scopus 로고
    • Hepatic elimination of flowing substrates: The distributed model
    • Bass, L.; Robinson, P.; Bracken, A. J. Hepatic elimination of flowing substrates: the distributed model. J. Theor. Biol., 1978, 72, 161-184.
    • (1978) J. Theor. Biol , vol.72 , pp. 161-184
    • Bass, L.1    Robinson, P.2    Bracken, A.J.3
  • 21
    • 0017603437 scopus 로고
    • Hepatic clearance of drugs. I. Theoretical considerations of a well-stirred model and a parallel tube model. Influence of hepatic blood flow, plasma and blood cell binding, and the hepatocellular enzymatic activity on hepatic drug clearance
    • Pang, K. S.; Rowland, M. Hepatic clearance of drugs. I. Theoretical considerations of a well-stirred model and a parallel tube model. Influence of hepatic blood flow, plasma and blood cell binding, and the hepatocellular enzymatic activity on hepatic drug clearance. J. Pharmacokinet. Biopharm., 1977, 5, 625-653.
    • (1977) J. Pharmacokinet. Biopharm , vol.5 , pp. 625-653
    • Pang, K.S.1    Rowland, M.2
  • 22
    • 0017603438 scopus 로고
    • Hepatic clearance of drugs. II. Experimental evidence for acceptance of the well-stirred model over the parallel tube model using lidocaine in the perfused rat liver in situ preparation
    • Pang, K. S.; Rowland, M. Hepatic clearance of drugs. II. Experimental evidence for acceptance of the well-stirred model over the parallel tube model using lidocaine in the perfused rat liver in situ preparation. J. Pharmacokinet. Biopharm., 1977, 5, 655-680.
    • (1977) J. Pharmacokinet. Biopharm , vol.5 , pp. 655-680
    • Pang, K.S.1    Rowland, M.2
  • 23
    • 0017565370 scopus 로고
    • Hepatic clearance of drugs. III. Additional experimental evidence supporting the well-stirred model, using metabolite (MEGX) generated from lidocaine under varying hepatic blood flow rates and linear conditions in the perfused rat liver in situ preparation
    • Pang, K. S.; Rowland, M. Hepatic clearance of drugs. III. Additional experimental evidence supporting the well-stirred model, using metabolite (MEGX) generated from lidocaine under varying hepatic blood flow rates and linear conditions in the perfused rat liver in situ preparation. J. Pharmacokinet. Biopharm., 1977, 5, 681-699.
    • (1977) J. Pharmacokinet. Biopharm , vol.5 , pp. 681-699
    • Pang, K.S.1    Rowland, M.2
  • 24
    • 0022549973 scopus 로고
    • A dispersion model of hepatic elimination: 1. Formulation of the model and bolus considerations
    • Roberts, M. S.; Rowland, M. A dispersion model of hepatic elimination: 1. Formulation of the model and bolus considerations. J. Pharmacokinet. Biopharm., 1986, 14, 227-260.
    • (1986) J. Pharmacokinet. Biopharm , vol.14 , pp. 227-260
    • Roberts, M.S.1    Rowland, M.2
  • 25
    • 0022552317 scopus 로고
    • A dispersion model of hepatic elimination: 2. Steady-state considerations--influence of hepatic blood flow, binding within blood, and hepatocellular enzyme activity
    • Roberts, M. S.; Rowland, M. A dispersion model of hepatic elimination: 2. Steady-state considerations--influence of hepatic blood flow, binding within blood, and hepatocellular enzyme activity. J. Pharmacokinet. Biopharm., 1986, 14, 261-288.
    • (1986) J. Pharmacokinet. Biopharm , vol.14 , pp. 261-288
    • Roberts, M.S.1    Rowland, M.2
  • 26
    • 0022922022 scopus 로고
    • A dispersion model of hepatic elimination: 3. Application to metabolite formation and elimination kinetics
    • Roberts, M. S.; Rowland, M. A dispersion model of hepatic elimination: 3. Application to metabolite formation and elimination kinetics. J. Pharmacokinet. Biopharm., 1986, 14, 289-308.
    • (1986) J. Pharmacokinet. Biopharm , vol.14 , pp. 289-308
    • Roberts, M.S.1    Rowland, M.2
  • 27
    • 0018163388 scopus 로고
    • Hepatic transport kinetics and plasma disappearance curves: Distributed modeling versus conventional approach
    • Forker, E. L.; Luxon, B. Hepatic transport kinetics and plasma disappearance curves: distributed modeling versus conventional approach. Am. J. Physiol., 1978, 235, E648-660.
    • (1978) Am. J. Physiol , vol.235
    • Forker, E.L.1    Luxon, B.2
  • 28
    • 77949821065 scopus 로고    scopus 로고
    • On the influence of protein binding on pharmacological activity of drugs
    • Berezhkovskiy, L. M. On the influence of protein binding on pharmacological activity of drugs. J. Pharm. Sci., 2010, 99, 2153-2165.
    • (2010) J. Pharm. Sci , vol.99 , pp. 2153-2165
    • Berezhkovskiy, L.M.1
  • 30
    • 0021361240 scopus 로고
    • Discrimination between the venous equilibrium and sinusoidal models of hepatic drug elimination in the isolated perfused rat liver by perturbation of propranolol protein binding
    • Jones, D. B.; Morgan, D. J.; Mihaly, G. W.; Webster, L. K.; Smallwood, R. A. Discrimination between the venous equilibrium and sinusoidal models of hepatic drug elimination in the isolated perfused rat liver by perturbation of propranolol protein binding. J. Pharmacol. Exp. Ther., 1984, 229, 522-526.
    • (1984) J. Pharmacol. Exp. Ther , vol.229 , pp. 522-526
    • Jones, D.B.1    Morgan, D.J.2    Mihaly, G.W.3    Webster, L.K.4    Smallwood, R.A.5
  • 31
    • 0023682627 scopus 로고
    • Effect of plasma protein binding on elimination of taurocholate by isolated perfused rat liver: Comparison of venous equilibrium, undistributed and distributed sinusoidal, and dispersion models
    • Smallwood, R. H.; Morgan, D. J.; Mihaly, G. W.; Jones, D. B.; Smallwood, R. A. Effect of plasma protein binding on elimination of taurocholate by isolated perfused rat liver: comparison of venous equilibrium, undistributed and distributed sinusoidal, and dispersion models. J. Pharmacokinet. Biopharm., 1988, 16, 377-396.
    • (1988) J. Pharmacokinet. Biopharm , vol.16 , pp. 377-396
    • Smallwood, R.H.1    Morgan, D.J.2    Mihaly, G.W.3    Jones, D.B.4    Smallwood, R.A.5
  • 32
    • 0026752823 scopus 로고
    • Application of the axial dispersion model of hepatic drug elimination to the kinetics of diazepam in the isolated perfused rat liver
    • Diaz-Garcia, J. M.; Evans, A. M.; Rowland, M. Application of the axial dispersion model of hepatic drug elimination to the kinetics of diazepam in the isolated perfused rat liver. J. Pharmacokinet. Biopharm., 1992, 20, 171-193.
    • (1992) J. Pharmacokinet. Biopharm , vol.20 , pp. 171-193
    • Diaz-Garcia, J.M.1    Evans, A.M.2    Rowland, M.3
  • 33
    • 0018750411 scopus 로고
    • Albumin-deficient ratmutant
    • Nagase, S.; Shimamune, K.; Shumiya, S. Albumin-deficient ratmutant. Science, 1979, 205, 590-591.
    • (1979) Science , vol.205 , pp. 590-591
    • Nagase, S.1    Shimamune, K.2    Shumiya, S.3
  • 34
    • 48849115495 scopus 로고    scopus 로고
    • Toxicokintic and toxicodynamic analysis of clofibrate based on free drug concentrations in nagase analbuminemia rats (NAR
    • Miida, H.; Arakawa, S.; Shibaya, Y.; Honda, K.; Kiyosawa, N.; Watanabe, K.; Manabe, S.; Takasaki, W.; Ueno, K. Toxicokintic and toxicodynamic analysis of clofibrate based on free drug concentrations in nagase analbuminemia rats (NAR). J. Toxicol. Sci., 2008, 33, 349-361.
    • (2008) J. Toxicol. Sci , vol.33 , pp. 349-361
    • Miida, H.1    Arakawa, S.2    Shibaya, Y.3    Honda, K.4    Kiyosawa, N.5    Watanabe, K.6    Manabe, S.7    Takasaki, W.8    Ueno, K.9
  • 35
    • 0036218554 scopus 로고    scopus 로고
    • Changes in plasma protein binding have little clinical relevance
    • Benet, L. Z.; Hoener, B. A. Changes in plasma protein binding have little clinical relevance. Clin. Pharmacol. Ther., 2002, 71, 115-121.
    • (2002) Clin. Pharmacol. Ther , vol.71 , pp. 115-121
    • Benet, L.Z.1    Hoener, B.A.2
  • 36
    • 0036799286 scopus 로고    scopus 로고
    • The pharmacokinetic- pharmacodynamic approach to a rational dosage regimen for antibiotics
    • Toutain, P. L.; del Castillo, J. R.; Bousquet-Melou, A. The pharmacokinetic- pharmacodynamic approach to a rational dosage regimen for antibiotics. Res. Vet. Sci., 2002, 73, 105-114.
    • (2002) Res. Vet. Sci , vol.73 , pp. 105-114
    • Toutain, P.L.1    del Castillo, J.R.2    Bousquet-Melou, A.3
  • 37
    • 0031442434 scopus 로고    scopus 로고
    • Quantitative structure-pharmacokinetics relationships: I. Development of a whole-body physiologically based model to characterize changes in pharmacokinetics across a homologous series of barbiturates in the rat
    • Blakey, G. E.; Nestorov, I. A.; Arundel, P. A.; Aarons, L. J.; Rowland, M. Quantitative structure-pharmacokinetics relationships: I. Development of a whole-body physiologically based model to characterize changes in pharmacokinetics across a homologous series of barbiturates in the rat. J. Pharmacokinet. Biopharm., 1997, 25, 277-312.
    • (1997) J. Pharmacokinet. Biopharm , vol.25 , pp. 277-312
    • Blakey, G.E.1    Nestorov, I.A.2    Arundel, P.A.3    Aarons, L.J.4    Rowland, M.5
  • 38
    • 0036874825 scopus 로고    scopus 로고
    • Influence of nonspecific brain and plasma binding on CNS exposure: Implications for rational drug discovery
    • Kalvass, J. C.; Maurer, T. S. Influence of nonspecific brain and plasma binding on CNS exposure: implications for rational drug discovery. Biopharm. Drug. Dispos., 2002, 23, 327-338.
    • (2002) Biopharm. Drug. Dispos , vol.23 , pp. 327-338
    • Kalvass, J.C.1    Maurer, T.S.2
  • 40
    • 0029160004 scopus 로고
    • Effective half-life in clinical pharmacology
    • Boxenbaum, H.; Battle, M. Effective half-life in clinical pharmacology. J. Clin. Pharmacol., 1995, 35, 763-766.
    • (1995) J. Clin. Pharmacol , vol.35 , pp. 763-766
    • Boxenbaum, H.1    Battle, M.2
  • 41
    • 0018668570 scopus 로고
    • Effect of altered plasma protein binding on apparent volume of distribution
    • Oie, S.; Tozer, T. N. Effect of altered plasma protein binding on apparent volume of distribution. J. Pharm. Sci., 1979, 68, 1203-1205.
    • (1979) J. Pharm. Sci , vol.68 , pp. 1203-1205
    • Oie, S.1    Tozer, T.N.2
  • 44
    • 1242273811 scopus 로고    scopus 로고
    • Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics
    • Lombardo, F.; Obach, R. S.; Shalaeva, M. Y.; Gao, F. Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. J. Med. Chem., 2004, 47, 1242-1250.
    • (2004) J. Med. Chem , vol.47 , pp. 1242-1250
    • Lombardo, F.1    Obach, R.S.2    Shalaeva, M.Y.3    Gao, F.4
  • 45
    • 0037142338 scopus 로고    scopus 로고
    • Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data
    • Lombardo, F.; Obach, R. S.; Shalaeva, M. Y.; Gao, F. Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. J. Med. Chem., 2002, 45, 2867-2876.
    • (2002) J. Med. Chem , vol.45 , pp. 2867-2876
    • Lombardo, F.1    Obach, R.S.2    Shalaeva, M.Y.3    Gao, F.4
  • 46
    • 0035913059 scopus 로고    scopus 로고
    • ElogD(oct): A tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds
    • Lombardo, F.; Shalaeva, M. Y.; Tupper, K. A.; Gao, F. ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds. J. Med. Chem., 2001, 44, 2490-2497.
    • (2001) J. Med. Chem , vol.44 , pp. 2490-2497
    • Lombardo, F.1    Shalaeva, M.Y.2    Tupper, K.A.3    Gao, F.4
  • 47
    • 0030898087 scopus 로고    scopus 로고
    • Drug equilibration across the blood-brain barrier--pharmacokinetic considerations based on the microdialysis method
    • Hammarlund-Udenaes, M.; Paalzow, L. K.; de Lange, E. C. Drug equilibration across the blood-brain barrier--pharmacokinetic considerations based on the microdialysis method. Pharm. Res., 1997, 14, 128-134.
    • (1997) Pharm. Res , vol.14 , pp. 128-134
    • Hammarlund-Udenaes, M.1    Paalzow, L.K.2    de Lange, E.C.3
  • 48
    • 11144290156 scopus 로고    scopus 로고
    • Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice
    • Maurer, T. S.; Debartolo, D. B.; Tess, D. A.; Scott, D. O. Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice. Drug Metab. Dispos., 2005, 33, 175-181
    • (2005) Drug Metab. Dispos , vol.33 , pp. 175-181
    • Maurer, T.S.1    Debartolo, D.B.2    Tess, D.A.3    Scott, D.O.4
  • 51
    • 33644756715 scopus 로고    scopus 로고
    • Improving the in vitro prediction of in vivo central nervous system penetration: Integrating permeability, P-glycoprotein efflux, and free fractions in blood and brain
    • Summerfield, S. G.; Stevens, A. J.; Cutler, L.; del Carmen Osuna, M.; Hammond, B.; Tang, S. P.; Hersey, A.; Spalding, D. J.; Jeffrey, P. Improving the in vitro prediction of in vivo central nervous system penetration: integrating permeability, P-glycoprotein efflux, and free fractions in blood and brain. J. Pharmacol. Exp. Ther., 2006, 316, 1282-1290.
    • (2006) J. Pharmacol. Exp. Ther , vol.316 , pp. 1282-1290
    • Summerfield, S.G.1    Stevens, A.J.2    Cutler, L.3    del Carmen, O.M.4    Hammond, B.5    Tang, S.P.6    Hersey, A.7    Spalding, D.J.8    Jeffrey, P.9
  • 52
    • 67649408864 scopus 로고    scopus 로고
    • Unbound brain concentration determines receptor occupancy: A correlation of drug concentration and brain serotonin and dopamine reuptake transporter occupancy for eighteen compounds in rats
    • Liu, X.; Vilenski, O.; Kwan, J.; Apparsundaram, S.; Weikert, R., Unbound brain concentration determines receptor occupancy: a correlation of drug concentration and brain serotonin and dopamine reuptake transporter occupancy for eighteen compounds in rats. Drug Metab. Dispos. 2009, 37, 1548-1556.
    • (2009) Drug Metab. Dispos , vol.37 , pp. 1548-1556
    • Liu, X.1    Vilenski, O.2    Kwan, J.3    Apparsundaram, S.4    Weikert, R.5
  • 53
    • 33645821904 scopus 로고    scopus 로고
    • Evaluation of the utility of brain slice methods to study brain penetration
    • Becker, S.; Liu, X. Evaluation of the utility of brain slice methods to study brain penetration. Drug Metab. Dispos., 2006, 34, 855-861.
    • (2006) Drug Metab. Dispos , vol.34 , pp. 855-861
    • Becker, S.1    Liu, X.2
  • 54
    • 63849149894 scopus 로고    scopus 로고
    • Monshouwer, M. Unbound drug concentrations in brain homogenate and cerebral spinal fluid drug concentrations at steady state as a surrogate for unbound drug concentrations in brain interstitial fluid
    • Liu, X., Van Natta, K.; Yeo, H.; Vilenski, O.; Weller, P. E.; Worboys, P. D.; Monshouwer, M. Unbound drug concentrations in brain homogenate and cerebral spinal fluid drug concentrations at steady state as a surrogate for unbound drug concentrations in brain interstitial fluid. Drug Metab. Dispos., 2008, 37, 787-793.
    • (2008) Drug Metab. Dispos , vol.37 , pp. 787-793
    • Liu, X.1    van Natta, K.2    Yeo, H.3    Vilenski, O.4    Weller, P.E.5    Worboys, P.D.6
  • 56
    • 21144451475 scopus 로고    scopus 로고
    • Use of a physiologically based pharmacokinetic model to study the time to reach brain equilibrium: An experimental analysis of the role of blood-brain barrier permeability, plasma protein binding, and brain tissue binding
    • Liu, X.; Smith, B. J.; Chen, C.; Callegari, E.; Becker, S. L.; Chen, X.; Cianfrogna, J.; Doran, A C.; Doran, S. D.; Gibbs, J. P.; Hosea, N.; Liu, J.; Nelson, F. R.; Szewc, M. A.; Van, D. J. Use of a physiologically based pharmacokinetic model to study the time to reach brain equilibrium: an experimental analysis of the role of blood-brain barrier permeability, plasma protein binding, and brain tissue binding. J. Pharmacol. Exp. Ther., 2005, 313, 1254-1262.
    • (2005) J. Pharmacol. Exp. Ther , vol.313 , pp. 1254-1262
    • Liu, X.1    Smith, B.J.2    Chen, C.3    Callegari, E.4    Becker, S.L.5    Chen, X.6    Cianfrogna, J.7    Doran, A.C.8    Doran, S.D.9    Gibbs, J.P.10    Hosea, N.11    Liu, J.12    Nelson, F.R.13    Szewc, M.A.14    Van, D.J.15
  • 57
    • 34548842800 scopus 로고    scopus 로고
    • Pharmacokinetics and pharmacodynamics of seven opioids in P-glycoprotein-competent mice: Assessment of unbound brain EC50,u and correlation of in vitro, preclinical, and clinical data
    • Kalvass, J. C.; Olson, E. R.; Cassidy, M. P.; Selley, D. E.; Pollack, G. M. Pharmacokinetics and pharmacodynamics of seven opioids in P-glycoprotein-competent mice: assessment of unbound brain EC50,u and correlation of in vitro, preclinical, and clinical data. J. Pharmacol. Exp. Ther., 2007, 323, 346-355.
    • (2007) J. Pharmacol. Exp. Ther , vol.323 , pp. 346-355
    • Kalvass, J.C.1    Olson, E.R.2    Cassidy, M.P.3    Selley, D.E.4    Pollack, G.M.5
  • 59
    • 33845937770 scopus 로고    scopus 로고
    • Structure-brain exposure relationships
    • Hitchcock, S. A.; Pennington, L. D. Structure-brain exposure relationships. J. Med. Chem., 2006, 49, 7559-7583.
    • (2006) J. Med. Chem , vol.49 , pp. 7559-7583
    • Hitchcock, S.A.1    Pennington, L.D.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.