Citations (66)
Keep up to date with the latest research on this topic with citation updates for this article.
Read on this site (9)
Gopinadh Bhyrapuneni, Jagadeesh Babu Thentu, Veera Raghava Choudary Palacharla, Nageswararao Muddana, Raghupathi Reddy Aleti, Devender Reddy Ajjala & Ramakrishna Nirogi. (2018) A definite measure of occupancy exposures, seeking with non-radiolabeled in vivo 5-HT2A receptor occupancy and in vitro free fractions. Journal of Receptors and Signal Transduction 38:4, pages 359-366.
Read now
Read now
Kiril Lanevskij, Pranas Japertas & Remigijus Didziapetris. (2013) Improving the prediction of drug disposition in the brain. Expert Opinion on Drug Metabolism & Toxicology 9:4, pages 473-486.
Read now
Read now
Christoffer Bundgaard, Christina Sveigaard, Lise T. Brennum & Tine B. Stensbøl. (2012) Associating in vitro target binding and in vivo CNS occupancy of serotonin reuptake inhibitors in rats: The role of free drug concentrations. Xenobiotica 42:3, pages 256-265.
Read now
Read now
N. Başaran Mutlu, Zelihagül Değim, Şükran Yılmaz, Dinç Eşsiz & Ahmet Nacar. (2011) New perspective for the treatment of Alzheimer diseases: Liposomal rivastigmine formulations. Drug Development and Industrial Pharmacy 37:7, pages 775-789.
Read now
Read now
Laura Zonzini, Federica Bianchi, Nicola Cesari & Matteo Sartori. (2010) In vivo rat PK profiling in drug discovery: new challenges. Expert Opinion on Drug Discovery 5:11, pages 1031-1037.
Read now
Read now
V Mangas-Sanjuan, M González-Alvarez, I Gonzalez-Alvarez & M Bermejo. (2010) Drug Penetration Across the blood–brain Barrier: an Overview. Therapeutic Delivery 1:4, pages 535-562.
Read now
Read now
Kevin D Read & Simone Braggio. (2010) Assessing brain free fraction in early drug discovery. Expert Opinion on Drug Metabolism & Toxicology 6:3, pages 337-344.
Read now
Read now
Scott Summerfield & Phil Jeffrey. (2009) Discovery DMPK: changing paradigms in the eighties, nineties and noughties. Expert Opinion on Drug Discovery 4:3, pages 207-218.
Read now
Read now
Li Di, Edward H Kerns & Guy T Carter. (2008) Strategies to assess blood–brain barrier penetration. Expert Opinion on Drug Discovery 3:6, pages 677-687.
Read now
Read now
Articles from other publishers (57)
Iva Spreitzer, Josefin Keife, Tobias Strasser, Predrag Kalaba, Jana Lubec, Winfried Neuhaus, Gert Lubec, Thierry Langer, Judith Wackerlig & Irena Loryan. (2023) Pharmacokinetics of Novel Dopamine Transporter Inhibitor CE-123 and Modafinil with a Focus on Central Nervous System Distribution. International Journal of Molecular Sciences 24:23, pages 16956.
Crossref
Crossref
Stine Lund Hansen, Petur Weihe Dalsgaard, Kristian Linnet & Brian Schou Rasmussen. (2022) Comparison of Comprehensive Screening Results in Postmortem Blood and Brain Tissue by UHPLC–QTOF-MS. Journal of Analytical Toxicology 46:9, pages 1053-1058.
Crossref
Crossref
Irena Loryan, Andreas Reichel, Bo Feng, Christoffer Bundgaard, Christopher Shaffer, Cory Kalvass, Dallas Bednarczyk, Denise Morrison, Dominique Lesuisse, Edmund Hoppe, Georg C. Terstappen, Holger Fischer, Li Di, Nicola Colclough, Scott Summerfield, Stephen T. Buckley, Tristan S. Maurer & Markus Fridén. (2022) Unbound Brain-to-Plasma Partition Coefficient, Kp,uu,brain—a Game Changing Parameter for CNS Drug Discovery and Development. Pharmaceutical Research 39:7, pages 1321-1341.
Crossref
Crossref
Scott G. Summerfield, James W. T. Yates & David A. Fairman. (2022) Free Drug Theory – No Longer Just a Hypothesis?. Pharmaceutical Research 39:2, pages 213-222.
Crossref
Crossref
Jobin Jose, Akshay Bandiwadekar, Glain Gloria Figreda & Cleril Macqwin Crasta. 2022. Nanocarriers for Drug-Targeting Brain Tumors. Nanocarriers for Drug-Targeting Brain Tumors
401
430
.
Irena Loryan & Margareta Hammarlund-Udenaes. 2022. Drug Delivery to the Brain. Drug Delivery to the Brain
389
436
.
Giacomo Russo, Giuseppe Ermondi, Giulia Caron, Dieter Verzele & Frederic Lynen. (2021) Into the first biomimetic sphingomyelin stationary phase: Suitability in drugs’ biopharmaceutic profiling and block relevance analysis of selectivity. European Journal of Pharmaceutical Sciences 156, pages 105585.
Crossref
Crossref
Lassina Badolo, Kenneth Thirstrup, Søren Møller Nielsen, Ask Püschl, Thomas Jensen, Steve Watson & Christoffer Bundgaard. (2020) Target-Mediated Brain Tissue Binding for Small Molecule Inhibitors of Heat Shock Protein 90. Pharmaceutics 12:11, pages 1009.
Crossref
Crossref
Priyanka Dhiman, Neelam Malik & Anurag Khatkar. (2019) Lead optimization for promising monoamine oxidase inhibitor from eugenol for the treatment of neurological disorder: synthesis and in silico based study. BMC Chemistry 13:1.
Crossref
Crossref
David A. Lovejoy, David W. Hogg, Thomas L. Dodsworth, Fernando R. Jurado, Casey C. Read, Andrea L. D'Aquila & Dalia Barsyte-Lovejoy. (2019) Synthetic Peptides as Therapeutic Agents: Lessons Learned From Evolutionary Ancient Peptides and Their Transit Across Blood-Brain Barriers. Frontiers in Endocrinology 10.
Crossref
Crossref
Phil Jeffrey & Scott Summerfield. 2017. Pharmacology for Chemists: Drug Discovery in Context. Pharmacology for Chemists: Drug Discovery in Context
316
342
.
Tugba Copur & Levent Oner. 2017. Nanotechnology Methods for Neurological Diseases and Brain Tumors. Nanotechnology Methods for Neurological Diseases and Brain Tumors
69
89
.
S. G. Summerfield, Y. Zhang & H. Liu. (2016) Examining the Uptake of Central Nervous System Drugs and Candidates across the Blood-Brain Barrier. Journal of Pharmacology and Experimental Therapeutics 358:2, pages 294-305.
Crossref
Crossref
Vijay Mishra & Prashant Kesharwani. (2016) Dendrimer technologies for brain tumor. Drug Discovery Today 21:5, pages 766-778.
Crossref
Crossref
Zoran Rankovic. (2015) CNS Drug Design: Balancing Physicochemical Properties for Optimal Brain Exposure. Journal of Medicinal Chemistry 58:6, pages 2584-2608.
Crossref
Crossref
Bruno Stieger & Bo Gao. (2015) Drug Transporters in the Central Nervous System. Clinical Pharmacokinetics 54:3, pages 225-242.
Crossref
Crossref
Scott Summerfield, Phil Jeffrey, Jasminder Sahi & Liangfu Chen. 2015. Blood‐Brain Barrier in Drug Discovery. Blood‐Brain Barrier in Drug Discovery
95
112
.
Jean‐Marie Nicolas. 2015. Blood‐Brain Barrier in Drug Discovery. Blood‐Brain Barrier in Drug Discovery
66
93
.
Kathryn Ball, François Bouzom, Jean‐Michel Scherrmann, Bernard Walther & Xavier Declèves. (2014) Comparing translational population‐PBPK modelling of brain microdialysis with bottom‐up prediction of brain‐to‐plasma distribution in rat and human. Biopharmaceutics & Drug Disposition 35:8, pages 485-499.
Crossref
Crossref
Michael J. Cima, Heejin Lee, Karen Daniel, Laura M. Tanenbaum, Aikaterini Mantzavinou, Kevin C. Spencer, Qunya Ong, Jay C. Sy, John SantiniJr.Jr., Carl M. Schoellhammer, Daniel Blankschtein & Robert S. Langer. (2014) Single compartment drug delivery. Journal of Controlled Release 190, pages 157-171.
Crossref
Crossref
Irena Loryan, Vikash Sinha, Claire Mackie, Achiel Van Peer, Wilhelmus Drinkenburg, An Vermeulen, Denise Morrison, Mario Monshouwer, Donald Heald & Margareta Hammarlund-Udenaes. (2014) Mechanistic Understanding of Brain Drug Disposition to Optimize the Selection of Potential Neurotherapeutics in Drug Discovery. Pharmaceutical Research 31:8, pages 2203-2219.
Crossref
Crossref
Therese S. Salameh & William A. Banks. 2014. Pharmacology of the Blood Brain Barrier: Targeting CNS Disorders. Pharmacology of the Blood Brain Barrier: Targeting CNS Disorders
277
299
.
Andreas Reichel. 2014. Drug Delivery to the Brain. Drug Delivery to the Brain
339
374
.
Irena Loryan & Margareta Hammarlund-Udenaes. 2014. Drug Delivery to the Brain. Drug Delivery to the Brain
271
316
.
Kathryn Ball, François Bouzom, Jean-Michel Scherrmann, Bernard Walther & Xavier Declèves. (2013) Physiologically Based Pharmacokinetic Modelling of Drug Penetration Across the Blood–Brain Barrier—Towards a Mechanistic IVIVE-Based Approach. The AAPS Journal 15:4, pages 913-932.
Crossref
Crossref
Alan M. Palmer & Mohammad S. Alavijeh. (2018) Overview of Experimental Models of the Blood‐Brain Barrier in CNS Drug Discovery. Current Protocols in Pharmacology 62:1.
Crossref
Crossref
Scott G. Summerfield & Kelly C. Dong. (2013) In vitro, in vivo and in silico models of drug distribution into the brain. Journal of Pharmacokinetics and Pharmacodynamics 40:3, pages 301-314.
Crossref
Crossref
Anand K. Deo, Frank-Peter Theil & Jean-Marie Nicolas. (2013) Confounding Parameters in Preclinical Assessment of Blood–Brain Barrier Permeation: An Overview With Emphasis on Species Differences and Effect of Disease States. Molecular Pharmaceutics 10:5, pages 1581-1595.
Crossref
Crossref
Douglas B. Kell, Paul D. Dobson, Elizabeth Bilsland & Stephen G. Oliver. (2013) The promiscuous binding of pharmaceutical drugs and their transporter-mediated uptake into cells: what we (need to) know and how we can do so. Drug Discovery Today 18:5-6, pages 218-239.
Crossref
Crossref
James A. Baker & Iain J. Martin. 2012. Drug Discovery for Psychiatric Disorders. Drug Discovery for Psychiatric Disorders
445
464
.
Éva Hellinger, Szilvia Veszelka, Andrea E. Tóth, Fruzsina Walter, Ágnes Kittel, Mónika Laura Bakk, Károly Tihanyi, Viktor Háda, Shinsuke Nakagawa, Thuy Dinh Ha Duy, Masami Niwa, Mária A. Deli & Monika Vastag. (2012) Comparison of brain capillary endothelial cell-based and epithelial (MDCK-MDR1, Caco-2, and VB-Caco-2) cell-based surrogate blood–brain barrier penetration models. European Journal of Pharmaceutics and Biopharmaceutics 82:2, pages 340-351.
Crossref
Crossref
Wei‐Ye Liu, Zhi‐Bin Wang, Li‐Chao Zhang, Xin Wei & Ling Li. (2012) Tight Junction in Blood‐Brain Barrier: An Overview of Structure, Regulation, and Regulator Substances. CNS Neuroscience & Therapeutics 18:8, pages 609-615.
Crossref
Crossref
Stephen A. Hitchcock. (2012) Structural Modifications that Alter the P-Glycoprotein Efflux Properties of Compounds. Journal of Medicinal Chemistry 55:11, pages 4877-4895.
Crossref
Crossref
Alex Avdeef. 2012. Absorption and Drug Development. Absorption and Drug Development
575
680
.
Roger N Gunn, Scott G Summerfield, Cristian A Salinas, Kevin D Read, Qi Guo, Graham E Searle, Christine A Parker, Phil Jeffrey & Marc Laruelle. (2012) Combining PET Biodistribution and Equilibrium Dialysis Assays to Assess the Free Brain Concentration and BBB Transport of CNS Drugs. Journal of Cerebral Blood Flow & Metabolism 32:5, pages 874-883.
Crossref
Crossref
Adriana Alexandre S. Tavares, James Lewsey, Deborah Dewar & Sally L. Pimlott. (2012) Radiotracer properties determined by high performance liquid chromatography: a potential tool for brain radiotracer discovery. Nuclear Medicine and Biology 39:1, pages 127-135.
Crossref
Crossref
Matthew D. Thompson & Daniel A. Beard. (2012) Physiologically Based Pharmacokinetic Tissue Compartment Model Selection in Drug Development and Risk Assessment. Journal of Pharmaceutical Sciences 101:1, pages 424-435.
Crossref
Crossref
Jeannie M. Padowski & Gary M. Pollack. (2011) The influence of distributional kinetics into a peripheral compartment on the pharmacokinetics of substrate partitioning between blood and brain tissue. Journal of Pharmacokinetics and Pharmacodynamics 38:6, pages 743-767.
Crossref
Crossref
Li Di, John P. Umland, George Chang, Youping Huang, Zhen Lin, Dennis O. Scott, Matthew D. Troutman & Theodore E. Liston. (2011) Species Independence in Brain Tissue Binding Using Brain Homogenates. Drug Metabolism and Disposition 39:7, pages 1270-1277.
Crossref
Crossref
E Ballini, C Virginio, SJ Medhurst, SG Summerfield, L Aldegheri, A Buson, C Carignani, YH Chen, A Giacometti, I Lago, AJ Powell & W Jarolimek. (2011)
Characterization of three diaminopyrimidines as potent and selective antagonists of P2X3 and P2X2/3 receptors with
in vivo
efficacy in a pain model
. British Journal of Pharmacology 163:6, pages 1315-1325.
Crossref
Crossref
Olivier Lacombe, Orianne Videau, Delphine Chevillon, Anne-Cécile Guyot, Christelle Contreras, Sandrine Blondel, Laurence Nicolas, Aurélie Ghettas, Henri Bénech, Etienne Thevenot, Alain Pruvost, Sébastien Bolze, Lucie Krzaczkowski, Colette Prévost & Aloïse Mabondzo. (2011)
In Vitro
Primary Human and Animal Cell-Based Blood−Brain Barrier Models as a Screening Tool in Drug Discovery
. Molecular Pharmaceutics 8:3, pages 651-663.
Crossref
Crossref
Kiril Lanevskij, Justas Dapkunas, Liutauras Juska, Pranas Japertas & Remigijus Didziapetris. (2011) QSAR Analysis of Blood–Brain Distribution: The Influence of Plasma and Brain Tissue Binding. Journal of Pharmaceutical Sciences 100:6, pages 2147-2160.
Crossref
Crossref
Alex Avdeef & Na Sun. (2010) A New In Situ Brain Perfusion Flow Correction Method for Lipophilic Drugs Based on the pH-Dependent Crone-Renkin Equation. Pharmaceutical Research 28:3, pages 517-530.
Crossref
Crossref
Oksana Tsinman, Konstantin Tsinman, Na Sun & Alex Avdeef. (2010) Physicochemical Selectivity of the BBB Microenvironment Governing Passive Diffusion—Matching with a Porcine Brain Lipid Extract Artificial Membrane Permeability Model. Pharmaceutical Research 28:2, pages 337-363.
Crossref
Crossref
Dennis A. Smith, Li Di & Edward H. Kerns. (2010) The effect of plasma protein binding on in vivo efficacy: misconceptions in drug discovery. Nature Reviews Drug Discovery 9:12, pages 929-939.
Crossref
Crossref
Mikko Gynther, Aaro Jalkanen, Marko Lehtonen, Markus Forsberg, Krista Laine, Jarmo Ropponen, Jukka Leppänen, Johanna Knuuti & Jarkko Rautio. (2010) Brain uptake of ketoprofen–lysine prodrug in rats. International Journal of Pharmaceutics 399:1-2, pages 121-128.
Crossref
Crossref
Stephen M. CarlDavid J. LindleyPierre O. CouraudBabette B. WekslerIgnacio RomeroStephanie A. MoweryGregory T. Knipp. (2010) ABC and SLC Transporter Expression and Pot Substrate Characterization across the Human CMEC/D3 Blood−Brain Barrier Cell Line. Molecular Pharmaceutics 7:4, pages 1057-1068.
Crossref
Crossref
Jurgen Mensch, Libuse Jaroskova L, Wendy Sanderson, Anouche Melis, Claire Mackie, Geert Verreck, Marcus E. Brewster & Patrick Augustijns. (2010) Application of PAMPA-models to predict BBB permeability including efflux ratio, plasma protein binding and physicochemical parameters. International Journal of Pharmaceutics 395:1-2, pages 182-197.
Crossref
Crossref
Phil Jeffrey & Scott Summerfield. (2010) Assessment of the blood–brain barrier in CNS drug discovery. Neurobiology of Disease 37:1, pages 33-37.
Crossref
Crossref
Jurgen Mensch, Julen Oyarzabal, Claire Mackie & Patrick Augustijns. (2009) In vivo, in vitro and in silico methods for small molecule transfer across the BBB. Journal of Pharmaceutical Sciences 98:12, pages 4429-4468.
Crossref
Crossref
Ahmad Reza Mehdipour & Mehrdad Hamidi. (2009) Brain drug targeting: a computational approach for overcoming blood–brain barrier. Drug Discovery Today 14:21-22, pages 1030-1036.
Crossref
Crossref
Andreas Reichel. (2009) Addressing Central Nervous System (CNS) Penetration in Drug Discovery: Basics and Implications of the Evolving New Concept. Chemistry & Biodiversity 6:11, pages 2030-2049.
Crossref
Crossref
Kiril Lanevskij, Pranas Japertas, Remigijus Didziapetris & Alanas Petrauskas. (2009) Ionization‐Specific QSAR Models of Blood–Brain Penetration of Drugs. Chemistry & Biodiversity 6:11, pages 2050-2054.
Crossref
Crossref
Claude Dagenais, Alex Avdeef, Oksana Tsinman, Adam Dudley & Richard Beliveau. (2009) P-glycoprotein deficient mouse in situ blood–brain barrier permeability and its prediction using an in combo PAMPA model. European Journal of Pharmaceutical Sciences 38:2, pages 121-137.
Crossref
Crossref
Li Di, Edward H. Kerns, Ian F. Bezar, Susan L. Petusky & Youping Huang. (2009) Comparison of blood–brain barrier permeability assays: in situ brain perfusion, MDR1-MDCKII and PAMPA-BBB. Journal of Pharmaceutical Sciences 98:6, pages 1980-1991.
Crossref
Crossref
Ho Lun Wong, Xiao Yu Wu & Reina Bendayan. 2009. Pharmaceutical Perspectives of Cancer Therapeutics. Pharmaceutical Perspectives of Cancer Therapeutics
121
148
.
Andras J. Bauer & Brent R. Stockwell. (2008) Neurobiological Applications of Small Molecule Screening. Chemical Reviews 108:5, pages 1774-1786.
Crossref
Crossref