Published in J Pharmacol Exp Ther on December 01, 2002
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Predicting efflux ratios and blood-brain barrier penetration from chemical structure: combining passive permeability with active efflux by P-glycoprotein. ACS Chem Neurosci (2012) 0.84
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Evaluation of the P-glycoprotein (Abcb1) affinity status of a series of morphine analogs: comparative study with meperidine analogs to identify opioids with minimal P-glycoprotein interactions. Int J Pharm (2009) 0.82
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Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS Aβ Reduction. ACS Med Chem Lett (2012) 0.81
Cyclosporine A (CsA) affects the pharmacodynamics and pharmacokinetics of the atypical antipsychotic amisulpride probably via inhibition of P-glycoprotein (P-gp). J Neural Transm (Vienna) (2005) 0.81
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Physicochemical selectivity of the BBB microenvironment governing passive diffusion--matching with a porcine brain lipid extract artificial membrane permeability model. Pharm Res (2010) 0.81
Selective κ opioid antagonists nor-BNI, GNTI and JDTic have low affinities for non-opioid receptors and transporters. PLoS One (2013) 0.80
Preparation and evaluation at the delta opioid receptor of a series of linear leu-enkephalin analogues obtained by systematic replacement of the amides. ACS Chem Neurosci (2013) 0.79
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De novo prediction of p-glycoprotein-mediated efflux liability for druglike compounds. ACS Med Chem Lett (2012) 0.79
Characterization of a novel brain barrier ex vivo insect-based P-glycoprotein screening model. Pharmacol Res Perspect (2014) 0.78
Docking applied to the prediction of the affinity of compounds to P-glycoprotein. Biomed Res Int (2014) 0.78
P-glycoprotein- and organic anion-transporting polypeptide-mediated transport of periplocin may lead to drug-herb/drug-drug interactions. Drug Des Devel Ther (2014) 0.78
Identification of Trypanosoma brucei AdoMetDC Inhibitors Using a High-Throughput Mass Spectrometry-Based Assay. ACS Infect Dis (2017) 0.77
Unravelling the complex drug-drug interactions of the cardiovascular drugs, verapamil and digoxin, with P-glycoprotein. Biosci Rep (2016) 0.77
Discovery of 3-substituted aminocyclopentanes as potent and orally bioavailable NR2B subtype-selective NMDA antagonists. ACS Chem Neurosci (2011) 0.77
Ketamine coadministration attenuates morphine tolerance and leads to increased brain concentrations of both drugs in the rat. Br J Pharmacol (2015) 0.77
Anticancer efficacy and absorption, distribution, metabolism, and toxicity studies of aspergiolide A in early drug development. Drug Des Devel Ther (2014) 0.77
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Verification of a Maternal-Fetal Physiologically Based Pharmacokinetic Model for Passive Placental Permeability Drugs. Drug Metab Dispos (2017) 0.76
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Discovery of anthranilamides as a novel class of inhibitors of neurotropic alphavirus replication. Bioorg Med Chem (2015) 0.75
Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders. ACS Med Chem Lett (2016) 0.75
Potent, Selective, and CNS-Penetrant Tetrasubstituted Cyclopropane Class IIa Histone Deacetylase (HDAC) Inhibitors. ACS Med Chem Lett (2015) 0.75
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In vitro inhibitory profile of NDGA against AChE and its in silico structural modifications based on ADME profile. J Mol Model (2012) 0.75
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Anti-Parkinson Drug Biperiden Inhibits Enzyme Acetylcholinesterase. Biomed Res Int (2017) 0.75
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Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus. Proc Natl Acad Sci U S A (2007) 2.02
The role of efflux and uptake transporters in [N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine (GW572016, lapatinib) disposition and drug interactions. Drug Metab Dispos (2008) 1.69
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor. Drug Metab Dispos (2012) 1.69
SCYX-7158, an orally-active benzoxaborole for the treatment of stage 2 human African trypanosomiasis. PLoS Negl Trop Dis (2011) 1.66
In vitro p-glycoprotein inhibition assays for assessment of clinical drug interaction potential of new drug candidates: a recommendation for probe substrates. Drug Metab Dispos (2006) 1.50
Lapatinib distribution in HER2 overexpressing experimental brain metastases of breast cancer. Pharm Res (2011) 1.46
Summary workshop report: biopharmaceutics classification system--implementation challenges and extension opportunities. J Pharm Sci (2004) 1.43
Interaction of native bile acids with human apical sodium-dependent bile acid transporter (hASBT): influence of steroidal hydroxylation pattern and C-24 conjugation. Pharm Res (2006) 1.25
Principles and applicability of CSF sampling for the assessment of CNS drug delivery and pharmacodynamics. Adv Drug Deliv Rev (2004) 1.15
PhRMA CPCDC initiative on predictive models of human pharmacokinetics, part 3: comparative assessement of prediction methods of human clearance. J Pharm Sci (2011) 1.14
Differential involvement of Mrp2 (Abcc2) and Bcrp (Abcg2) in biliary excretion of 4-methylumbelliferyl glucuronide and sulfate in the rat. J Pharmacol Exp Ther (2006) 1.13
PhRMA CPCDC initiative on predictive models of human pharmacokinetics, part 2: comparative assessment of prediction methods of human volume of distribution. J Pharm Sci (2011) 1.04
PHRMA CPCDC initiative on predictive models of human pharmacokinetics, part 5: prediction of plasma concentration-time profiles in human by using the physiologically-based pharmacokinetic modeling approach. J Pharm Sci (2011) 1.03
Influence of charge and steric bulk in the C-24 region on the interaction of bile acids with human apical sodium-dependent bile acid transporter. Mol Pharm (2006) 1.03
Method to screen substrates of apical sodium-dependent bile acid transporter. AAPS J (2008) 1.00
Predicting P-glycoprotein substrates by a quantitative structure-activity relationship model. J Pharm Sci (2004) 1.00
PhRMA white paper on ADME pharmacogenomics. J Clin Pharmacol (2008) 0.99
Toxicity and toxicokinetics of metformin in rats. Toxicol Appl Pharmacol (2010) 0.99
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SAR of 2-amino and 2,4-diamino pyrimidines with in vivo efficacy against Trypanosoma brucei. Bioorg Med Chem Lett (2011) 0.98
The elementary mass action rate constants of P-gp transport for a confluent monolayer of MDCKII-hMDR1 cells. Biophys J (2004) 0.95
P-glycoprotein influences the brain concentrations of cetirizine (Zyrtec), a second-generation non-sedating antihistamine. J Pharm Sci (2003) 0.95
Kinetic identification of membrane transporters that assist P-glycoprotein-mediated transport of digoxin and loperamide through a confluent monolayer of MDCKII-hMDR1 cells. Drug Metab Dispos (2007) 0.94
If the KI is defined by the free energy of binding to P-glycoprotein, which kinetic parameters define the IC50 for the Madin-Darby canine kidney II cell line overexpressing human multidrug resistance 1 confluent cell monolayer? Drug Metab Dispos (2009) 0.92
Multiple mechanisms are involved in the biliary excretion of acetaminophen sulfate in the rat: role of Mrp2 and Bcrp1. Drug Metab Dispos (2005) 0.92
Benzoxaboroles: a new class of potential drugs for human African trypanosomiasis. Future Med Chem (2011) 0.92
Enfuvirtide plasma levels and injection site reactions using a needle-free gas-powered injection system (Biojector). AIDS (2006) 0.89
Midazolam exhibits characteristics of a highly permeable P-glycoprotein substrate. Pharm Res (2003) 0.89
The steady-state Michaelis-Menten analysis of P-glycoprotein mediated transport through a confluent cell monolayer cannot predict the correct Michaelis constant Km. Pharm Res (2005) 0.87
Steady-state brain concentrations of antihistamines in rats: interplay of membrane permeability, P-glycoprotein efflux and plasma protein binding. Pharmacology (2004) 0.87
Use of cassette dosing in sandwich-cultured rat and human hepatocytes to identify drugs that inhibit bile acid transport. Toxicol In Vitro (2009) 0.87
Enfuvirtide cerebrospinal fluid (CSF) pharmacokinetics and potential use in defining CSF HIV-1 origin. Antivir Ther (2008) 0.85
Central nervous system disposition and metabolism of Fosdevirine (GSK2248761), a non-nucleoside reverse transcriptase inhibitor: an LC-MS and Matrix-assisted laser desorption/ionization imaging MS investigation into central nervous system toxicity. Chem Res Toxicol (2012) 0.85
Exact kinetic analysis of passive transport across a polarized confluent MDCK cell monolayer modeled as a single barrier. J Pharm Sci (2004) 0.85
In vitro absorption and secretory quotients: practical criteria derived from a study of 331 compounds to assess for the impact of P-glycoprotein-mediated efflux on drug candidates. J Pharm Sci (2004) 0.84
P-Glycoprotein (P-gp) expressed in a confluent monolayer of hMDR1-MDCKII cells has more than one efflux pathway with cooperative binding sites. Biochemistry (2006) 0.83
Understanding the transport properties of metabolites: case studies and considerations for drug development. Drug Metab Dispos (2013) 0.83
Evaluation of the drug interaction potential of aplaviroc, a novel human immunodeficiency virus entry inhibitor, using a modified cooperstown 5 + 1 cocktail. J Clin Pharmacol (2006) 0.83
In vitro and clinical investigation of the relationship between CCR5 receptor occupancy and anti-HIV activity of Aplaviroc. J Clin Pharmacol (2008) 0.83
First human dose-escalation study with remogliflozin etabonate, a selective inhibitor of the sodium-glucose transporter 2 (SGLT2), in healthy subjects and in subjects with type 2 diabetes mellitus. BMC Pharmacol Toxicol (2013) 0.82
Safety, pharmacokinetics and pharmacodynamics of remogliflozin etabonate, a novel SGLT2 inhibitor, and metformin when co-administered in subjects with type 2 diabetes mellitus. BMC Pharmacol Toxicol (2013) 0.81
The systemic exposure of an N-methyl-D-aspartate receptor antagonist is limited in mice by the P-glycoprotein and breast cancer resistance protein efflux transporters. Drug Metab Dispos (2004) 0.80
Assessment of the drug interaction risk for remogliflozin etabonate, a sodium-dependent glucose cotransporter-2 inhibitor: evidence from in vitro, human mass balance, and ketoconazole interaction studies. Drug Metab Dispos (2012) 0.80
PhRMA CPCDC initiative on predictive models of human pharmacokinetics, part 4: prediction of plasma concentration-time profiles in human from in vivo preclinical data by using the Wajima approach. J Pharm Sci (2011) 0.79
PhRMA CPCDC initiative on predictive models of human pharmacokinetics, part 1: goals, properties of the PhRMA dataset, and comparison with literature datasets. J Pharm Sci (2011) 0.78
The Effect of Dolutegravir on the Pharmacokinetics of Metformin in Healthy Subjects. J Acquir Immune Defic Syndr (2016) 0.77
The ABCG2 C421A polymorphism does not affect oral nitrofurantoin pharmacokinetics in healthy Chinese male subjects. Br J Clin Pharmacol (2008) 0.77
Oral sulfasalazine as a clinical BCRP probe substrate: pharmacokinetic effects of genetic variation (C421A) and pantoprazole coadministration. J Pharm Sci (2010) 0.76
Temporal kinetics and concentration-response relationships for induction of CYP1A, CYP2B, and CYP3A in primary cultures of beagle dog hepatocytes. J Biochem Mol Toxicol (2006) 0.75
Conference report: a hitchhiker's guide to outsourcing ADME studies: the inside of outsourcing. Bioanalysis (2013) 0.75
Monitoring liver safety in drug development: the GSK experience. Regul Toxicol Pharmacol (2007) 0.75
Automated quantitative and qualitative analysis of metabolic stability: a process for compound selection during drug discovery. Methods Enzymol (2002) 0.75
Synthesis and evaluation of potent and selective beta3 adrenergic receptor agonists containing heterobiaryl carboxylic acids. Bioorg Med Chem Lett (2007) 0.75