Assessing brain free fraction in early drug discovery

Bibliography

• Di L, Kerns EH, Carter GT. Strategies to assess blood-brain barrier penetration. Expert Opin Drug Discov 2008;3:677-87
   PubMed Web of Science ®Google Scholar
• Reichel A, Begley DJ Abbott NJ. An overview of in vitro techniques for blood-brain barrier studies. In: Nag S, Methods in Molecular medicine. The blood-brain barrier: Biology and research tools. (Volume 89). Humana Press Inc., Totowa, NJ; 2003
   Google Scholar
• Reichel A. The role of blood-brain barrier studies in the pharmaceutical industry. Current Drug Metab 2006;7:183-203
   PubMed Web of Science ®Google Scholar
• Pardridge WM. Holy grails and in vitro blood-brain barrier models. DDT 2004;9:258
   PubMed Web of Science ®Google Scholar
• Di L, Kerns EH, Bezer IF, Comparison of blood-brain barrier permeability assays: in situ brain perfusion, MDR1-MDCKII and PAMPA-BBB. J Pharm Sci 2009;98:1980-91
   PubMed Web of Science ®Google Scholar
• Summerfield SG, Read K, Begley DJ, Central nervous system drug disposition: the relationship between in situ brain permeability and brain free fraction. JPET 2007;322:205-13
   PubMed Web of Science ®Google Scholar
• Hammarlund-Udenaes M, Friden M, Syvanen S, Gupta A. On the rate and extent of drug delivery to the brain. Pharm Res 2008;25:1737-50
   PubMed Web of Science ®Google Scholar
• Hammarlund-Udenaes M, Bredberg U, Friden M. Methodologies to assess brain drug delivery in lead optimisation. Curr Top Med Chem 2009;9:148-62
   PubMed Web of Science ®Google Scholar
• Doran A, Obach RS, Smith BJ, The impact of P-glycoprotein on the disposition of drugs targeted for indications of the central nervous system: evaluation using the MDR1A/1B knockout mouse model. Drug Metab Dispos 2005;33:165-74
   PubMed Web of Science ®Google Scholar
• de Lange EC, Danhof M. Considerations in the use of CSF pharmacokinetics to predict brain target concentrations in the clinical setting: implications of the barriers between blood and brain. Clin Pharmacokinet 2002;41:691-703
   PubMed Web of Science ®Google Scholar
• Martin I. Prediction of blood brain barrier penetration: are we missing the point? DDT 2004;9:161-2
   PubMed Web of Science ®Google Scholar
• Kalvass JC, Maurer TS. Influence of non-specific brain and plasma binding on CNS exposure: Implications for rational drug discovery. Biopharm Drug Dispos 2002;23:327-38
   PubMed Web of Science ®Google Scholar
• Lin JH. CSF as a surrogate for assessing CNS exposure: an industrial perspective. Curr Drug Metab 2008;9:46-59
   PubMed Web of Science ®Google Scholar
• Abbott NJ. Evidence of bulk flow of brain interstitial fluid; significance for physiology and pathology. Neurochem Int 2004;45:545-52
   PubMed Web of Science ®Google Scholar
• Liu X, Smith BJ, Chen C, Evaluation of cerebrospinal fluid concentration and plasma free concentration as a surrogate measurement for brain free concentration. Drug Metab Dispos 2006;34:1443-7
   PubMed Web of Science ®Google Scholar
• Soontornmalai A, Vlaming MLH, Fritschchy J-M. Differential, strain-specific cellular and subcellular distribution of multidrug transporters in murine choroid plexus and blood-brain barrier. Neuroscience 2006;138:159-69
   PubMed Web of Science ®Google Scholar
• Shen DD, Artru AA, Adkinson KK. Principles and applicability of CSF sampling for the assessment of CNS drug delivery and pharmacodynamics. Adv Drug Deliv Rev 2004;56:1825-57
   PubMed Web of Science ®Google Scholar
• Fridén M, Winiwarter S, Jerndal G, Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. J Med Chem 2009;52:6233-43
   PubMed Web of Science ®Google Scholar
• Tillement JP, Urien S, Chaumet-Riffaud P, Blood binding and tissue uptake of drugs. Recent advances and perspectives. Fundam Clin Pharmacol 1988;2:223-38
   PubMed Web of Science ®Google Scholar
• Watson J, Wright S, Lucas A, Receptor occupancy and brain free fraction. Drug Metab Dispos 2009;37:753-60
   PubMed Web of Science ®Google Scholar
• Liu X, Vilenski O, Kwan J, 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;37:1548-56
   PubMed Web of Science ®Google Scholar
• Liu X, Van Natta K, Yeo H, Unbound drug concentration in brain homogenate and cerebral spinal fluid at steady state as a surrogate for unbound concentration in brain interstitial fluid. Drug Metab Dispos 2009;37:787-93
   PubMed Web of Science ®Google Scholar
• Large CH, Kalinichev M, Lucas A, The relationship between sodium channel inhibition and anticonvulsant activity in a model of generalised seizure in the rat. Epilepsy Res 2009;85:96-106
   PubMed Web of Science ®Google Scholar
• Gunn RN, Summerfield SG, Salinas C, Combining PET and equilibrium dialysis to assess blood-brain barrier transport. J Cereb Blood Flow Metab 2007;27(Suppl 1):P004-14
   Google Scholar
• Kalvass JC, Olsen ER, Cassidy MP, Pharmackinetics 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. JPET 2007;323:346-55
   PubMed Web of Science ®Google Scholar
• Bostrom E, Hammarlund-Udenaes M, Simonsson USH. Blood-brain barrier transport helps to explain discrepancies in in vivo potency between oxycodone and morphine. Anaeshesiology 2008;108:495-505
   PubMed Web of Science ®Google Scholar
• Fitzgerald PB, Kapur S, Remington G, Predicting haloperidol occupancy of central dopamine D2 receptors from plasma levels. Psychopharmacology 2000;149:1-5
   PubMed Web of Science ®Google Scholar
• Becker S, Liu X. Evaluation of the utility of brain slice methods to study brain penetration. Drug Metab Dispos 2006;34:855-61
   PubMed Web of Science ®Google Scholar
• Wan H, Rehngren M, Giordanetto F, High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery. J Med Chem 2007;50:4606-15
   PubMed Web of Science ®Google Scholar
• Friden M, Ducrozet F, Middleton B, Development of a high-throughput brain slice method for studying drug distribution in the central nervous system. Drug Metab Dispos 2009;37:1226-33
   PubMed Web of Science ®Google Scholar
• Maurer TS, DeBartolo DB, Tess DA, Scott DO. Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice. Drug Metab Dispos 2005;33:175-81
   PubMed Web of Science ®Google Scholar
• Kalvass JC, Maurer TS, Pollack GM. Use of plasma and brain unbound fractions to assess the extent of brain distribution of 34 drugs: comparison of unbound concentration ratios to in vivo P-glycoprotein efflux ratios. Drug Metab Dispos 2007;35:660-6
   PubMed Web of Science ®Google Scholar
• Summerfield SG, Lucas AJ, Porter RA, Toward an improved prediction of human in vivo brain penetration. Xenobiotica 2008;38:1518-35
   PubMed Web of Science ®Google Scholar
• Jeffrey P, Summerfield SG. Challenges for blood-brain barrier (BBB) screening. Xenobiotica 2007;37:1135-51
   PubMed Web of Science ®Google Scholar