Drug metabolism and pharmacokinetics, the blood-brain barrier, and central nervous system drug discovery.
paper
Cited
Public
Unavailable
- Authors
- Alavijeh, Mohammad S; Chishty, Mansoor; Qaiser, M Zeeshan; Palmer, Alan M
- Year
- 2005
- Journal
- NeuroRx : the journal of the American Society for Experimental NeuroTherapeutics
- PMID
- 16489365
- DOI
- 10.1602/neurorx.2.4.554
- PMCID
- PMC1201315
The worldwide market for therapies for CNS disorders is worth more than 50 billion dollars and is set to grow substantially in the years ahead. This is because: 1) the incidence of many CNS disorders (e.g., Alzheimer's disease, stroke, and Parkinson's disease) increase exponentially after age 65 and 2) the number of people in the world over 65 is about to increase sharply because of a marked rise in fertility after World War II. However, CNS research and development are associated with significant challenges: it takes longer to get a CNS drug to market (12-16 years) compared with a non-CNS drug (10-12 years) and there is a higher attrition rate for CNS drug candidates than for non-CNS drug candidates. This is attributable to a variety of factors, including the complexity of the brain, the liability of CNS drugs to cause CNS side effects, and the requirement of CNS drugs to cross the blood-brain barrier (BBB). This review focuses on BBB penetration, along with pharmacokinetics and drug metabolism, in the process of the discovery and development of safe and effective medicines for CNS disorders.
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| Isolation and in vitro permeation of phenylpropylamino alkaloids from Khat (Catha edulis) across oral and intestinal mucosal tissues. | Atlabachew M et al. | β | 2016 | β |
| Measuring blood-brain barrier penetration using the NeuroCart, a CNS test battery. | Groeneveld GJ et al. | β | 2016 | β |
| Modelling of compound combination effects and applications to efficacy and toxicity: state-of-the-art, challenges and perspectives. | Bulusu KC et al. | β | 2016 | β |
| Nanoparticle transport across the blood brain barrier. | Grabrucker AM et al. | β | 2016 | β |
| Nanoscale effects in dendrimer-mediated targeting of neuroinflammation. | Nance E et al. | β | 2016 | β |
| Random Forest Segregation of Drug Responses May Define Regions of Biological Significance. | Bukhari Q et al. | β | 2016 | β |
| Redox Modulations, Antioxidants, and Neuropsychiatric Disorders. | Fraunberger EA et al. | β | 2016 | β |
| Single nucleotide polymorphisms in clinics: Fantasy or reality for cancer? | Srinivasan S et al. | β | 2016 | β |
| Synthesis and Determination of Physicochemical Properties of New 3-(4-Arylpiperazin-1-yl)-2-hydroxypropyl 4-Alkoxyethoxybenzoates. | Marvanova P et al. | β | 2016 | β |
| Synthesis, characterisation and in vitro investigation of photodynamic activity of 5-(4-octadecanamidophenyl)-10,15,20-tris(N-methylpyridinium-3-yl)porphyrin trichloride on HeLa cells using low light fluence rate. | Malatesti N et al. | β | 2016 | β |
| Therapeutic Potential of Natural Product-Based Oral Nanomedicines for Stroke Prevention. | Mutoh T et al. | β | 2016 | β |
| Antisense oligonucleotides in therapy for neurodegenerative disorders. | Evers MM et al. | β | 2015 | β |
| Aspidosperma (Apocynaceae) plant cytotoxicity and activity towards malaria parasites. Part II: experimental studies withAspidosperma ramiflorum in vivo and in vitro. | Aguiar AC et al. | β | 2015 | β |
| Combined effect of rifampicin-induced P-glycoprotein expression and lipopolysaccharide-induced intestinal sepsis on the effective permeability and pharmacokinetics of an anti-malarial candidate CDRI 97/78 in rats. | Singh Y et al. | β | 2015 | β |
| Computational analysis reveal inhibitory action of nimbin against dengue viral envelope protein. | Lavanya P et al. | β | 2015 | β |
| Developing Enhanced Blood-Brain Barrier Permeability Models: Integrating External Bio-Assay Data in QSAR Modeling. | Wang W et al. | β | 2015 | β |
| Efficacy of cabazitaxel in mouse models of pediatric brain tumors. | Girard E et al. | β | 2015 | β |
| Glycyrrhetinic acid and E.resveratroloside act as potential plant derived compounds against dopamine receptor D3 for Parkinson's disease: a pharmacoinformatics study. | Mirza MU et al. | β | 2015 | β |
| Mapping drug distribution in brain tissue using liquid extraction surface analysis mass spectrometry imaging. | Swales JG et al. | β | 2015 | β |
| Nanoparticle-mediated growth factor delivery systems: A new way to treat Alzheimer's disease. | Lauzon MA et al. | β | 2015 | β |
| Neuroprotective Strategies after Neonatal Hypoxic Ischemic Encephalopathy. | Dixon BJ et al. | β | 2015 | β |
| Pharmacoinformatics approach for investigation of alternative potential hepatitis C virus nonstructural protein 5B inhibitors. | Mirza MU et al. | β | 2015 | β |
| Preclinical studies of the potent and selective nicotinic Ξ±4Ξ²2 receptor ligand VMY-2-95. | Kong H et al. | β | 2015 | β |
| Preparation of silica nanoparticles loaded with nootropics and their in vivo permeation through blood-brain barrier. | Jampilek J et al. | β | 2015 | β |
| Screening of Methanol Extract and Ethyl Acetate Fraction of Abies webbiana Lindl. for Neuropharmacological Activities. | Parkash O et al. | β | 2015 | β |
| Targeting brain metastases in ALK-rearranged non-small-cell lung cancer. | Zhang I et al. | β | 2015 | β |
| Targeting therapeutics across the blood brain barrier (BBB), prerequisite towards thrombolytic therapy for cerebrovascular disorders-an overview and advancements. | Pulicherla KK et al. | β | 2015 | β |
| Tertiary Amine Pyrazolones and Their Salts as Inhibitors of Mutant Superoxide Dismutase 1-Dependent Protein Aggregation for the Treatment of Amyotrophic Lateral Sclerosis. | Zhang Y et al. | β | 2015 | β |
| Tuscan black kale sprout extract bioactivated with myrosinase: a novel natural product for neuroprotection by inflammatory and oxidative response during cerebral ischemia/reperfusion injury in rat. | Giacoppo S et al. | β | 2015 | β |
| Can formulation and drug delivery reduce attrition during drug discovery and development-review of feasibility, benefits and challenges. | Basavaraj S et al. | β | 2014 | β |
| Delivery of therapeutic peptides and proteins to the CNS. | Salameh TS et al. | β | 2014 | β |
| Design, economical synthesis and antiplasmodial evaluation of vanillin derived allylated chalcones and their marked synergism with artemisinin against chloroquine resistant strains of Plasmodium falciparum. | Sharma N et al. | β | 2014 | β |
| Developmental and pathological angiogenesis in the central nervous system. | Vallon M et al. | β | 2014 | β |
| Dual binding site and selective acetylcholinesterase inhibitors derived from integrated pharmacophore models and sequential virtual screening. | Gupta S et al. | β | 2014 | β |
| Effect of saikosaponins and extracts of vinegar-baked Bupleuri Radix on the activity of Ξ²-glucuronidase. | Chen X et al. | β | 2014 | β |
| Identification of a functional homolog of the mammalian CYP3A4 in locusts. | Olsen LR et al. | β | 2014 | β |
| In vitro cerebrovascular modeling in the 21st century: current and prospective technologies. | Palmiotti CA et al. | β | 2014 | β |
| In vitro models of the blood-brain barrier for the study of drug delivery to the brain. | Wilhelm I et al. | β | 2014 | β |
| Lead optimization studies of cinnamic amide EP2 antagonists. | Ganesh T et al. | β | 2014 | β |
| Monitoring therapeutic monoclonal antibodies in brain tumor. | Ait-Belkacem R et al. | β | 2014 | β |
| Nanoscale drug delivery systems and the blood-brain barrier. | Alyautdin R et al. | β | 2014 | β |
| Perifosine induced release of contents of trans cell-barrier transport efficient liposomes. | Koklic T | β | 2014 | β |
| Synthesis, modelling and biological characterization of 3-substituted-1H-indoles as ligands of GluN2B-containing N-methyl-d-aspartate receptors. | Gitto R et al. | β | 2014 | β |
| The effect of the Pheroid delivery system on the in vitro metabolism and in vivo pharmacokinetics of artemisone. | Grobler L et al. | β | 2014 | β |
| Theoretical and practical applications of the intracerebroventricular route for CSF sampling and drug administration in CNS drug discovery research: a mini review. | Kuo A et al. | β | 2014 | β |
| Cerebral microdialysis in clinical studies of drugs: pharmacokinetic applications. | Shannon RJ et al. | β | 2013 | β |
| Clinical drug interactions: a holistic view. | Rahal A et al. | β | 2013 | β |
| Concurrent middle cerebral artery occlusion and intra-arterial drug infusion via ipsilateral common carotid artery catheter in the rat. | Van Winkle JA et al. | β | 2013 | β |
| Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery. | Yu DD et al. | β | 2013 | β |
| Flavonoid from Carica papaya inhibits NS2B-NS3 protease and prevents Dengue 2 viral assembly. | Senthilvel P et al. | β | 2013 | β |
| Frontotemporal degeneration, the next therapeutic frontier: molecules and animal models for frontotemporal degeneration drug development. | Boxer AL et al. | β | 2013 | β |
| Interpenetrating polymer network of locust bean gum-poly (vinyl alcohol) for controlled release drug delivery. | Kaity S et al. | β | 2013 | β |
| In vitro inhibitory profile of NDGA against AChE and its in silico structural modifications based on ADME profile. | Remya C et al. | β | 2013 | β |
| Methodologies to assess drug permeation through the blood-brain barrier for pharmaceutical research. | Passeleu-Le Bourdonnec C et al. | β | 2013 | β |
| Overview of experimental models of the blood-brain barrier in CNS drug discovery. | Palmer AM et al. | β | 2013 | β |
| Physiologically based pharmacokinetic modelling of drug penetration across the blood-brain barrier--towards a mechanistic IVIVE-based approach. | Ball K et al. | β | 2013 | β |
| Synthesis of new 1-phenyl-2-(4-substituted-piperazin-1-yl)-propanol derivatives and evaluation of their antidepressant-like effects. | Demir Γzkay Γ et al. | β | 2013 | β |
| Systems approaches and polypharmacology for drug discovery from herbal medicines: an example using licorice. | Liu H et al. | β | 2013 | β |
| Total flavonoid of Litsea coreana leve exerts anti-oxidative effects and alleviates focal cerebral ischemia/reperfusion injury. | Dong S et al. | β | 2013 | β |
| Brainpeps: the blood-brain barrier peptide database. | Van Dorpe S et al. | β | 2012 | β |
| Delivery of drugs to the brain via the blood brain barrier using colloidal carriers. | Tucker IG et al. | β | 2012 | β |
| Insights into the structural determinants required for high-affinity binding of chiral cyclopropane-containing ligands to Ξ±4Ξ²2-nicotinic acetylcholine receptors: an integrated approach to behaviorally active nicotinic ligands. | Zhang HK et al. | β | 2012 | β |
| In vivo acetylcholinesterase inhibition in the tissues of spinosad exposed Oreochromis niloticus. | Piner P et al. | β | 2012 | β |
| Nanotechnology: from fundamental concepts to clinical applications for healthy aging. | Rees M et al. | β | 2012 | β |
| Neuroprotective activityof Cymbopogon martinii against cerebral ischemia/reperfusion-induced oxidative stress in rats. | Buch P et al. | β | 2012 | β |
| Radiotracer properties determined by high performance liquid chromatography: a potential tool for brain radiotracer discovery. | Tavares AA et al. | β | 2012 | β |
| Synthesis and biological characterization of 3-substituted 1H-indoles as ligands of GluN2B-containing N-methyl-D-aspartate receptors. Part 2. | Gitto R et al. | β | 2012 | β |
| Synthesis and profiling of a diverse collection of azetidine-based scaffolds for the development of CNS-focused lead-like libraries. | Lowe JT et al. | β | 2012 | β |
| Three dimensional structure prediction and proton nuclear magnetic resonance analysis of toxic pesticides in human blood plasma. | Sharma AK et al. | β | 2012 | β |
| Translational CNS medicines research. | Palmer AM et al. | β | 2012 | β |
| Antitumor agents 288: design, synthesis, SAR, and biological studies of novel heteroatom-incorporated antofine and cryptopleurine analogues as potent and selective antitumor agents. | Yang X et al. | β | 2011 | β |
| Assessments of tight junction proteins occludin, claudin 5 and scaffold proteins ZO1 and ZO2 in endothelial cells of the rat blood-brain barrier: cellular responses to neurotoxicants malathion and lead acetate. | Balbuena P et al. | β | 2011 | β |
| Discovery of dual binding site acetylcholinesterase inhibitors identified by pharmacophore modeling and sequential virtual screening techniques. | Gupta S et al. | β | 2011 | β |
| Drug delivery to the brain via the blood-brain barrier: a review of the literature and some recent patent disclosures. | Tucker IG | β | 2011 | β |
| Metabolic conversion of dietary flavonoids alters their anti-inflammatory and antioxidant properties. | Lotito SB et al. | β | 2011 | β |
| Neuroprotective therapeutics for Alzheimer's disease: progress and prospects. | Palmer AM | β | 2011 | β |
| New perspective for the treatment of Alzheimer diseases: liposomal rivastigmine formulations. | Mutlu NB et al. | β | 2011 | β |
| Shuttle-mediated drug delivery to the brain. | Malakoutikhah M et al. | β | 2011 | β |
| A novel quantification of blood-brain barrier damage and histochemical typing after embolic stroke in rats. | Michalski D et al. | β | 2010 | β |
| Connecting vascular and nervous system development: angiogenesis and the blood-brain barrier. | Tam SJ et al. | β | 2010 | β |
| Drug penetration across the blood-brain barrier: an overview. | Mangas-Sanjuan V et al. | β | 2010 | β |
| Measurement of the pharmacokinetics and pharmacodynamics of neuroactive compounds. | Alavijeh MS et al. | β | 2010 | β |
| The role of the blood-CNS barrier in CNS disorders and their treatment. | Palmer AM | β | 2010 | β |
| Challenges and opportunities in CNS delivery of therapeutics for neurodegenerative diseases. | Barchet TM et al. | β | 2009 | β |
| Interpretation of antibiotic concentration ratios measured in epithelial lining fluid. | Kiem S et al. | β | 2008 | β |
| In vitro and in vivo neuroprotective effect and mechanisms of glabridin, a major active isoflavan from Glycyrrhiza glabra (licorice). | Yu XQ et al. | β | 2008 | β |
| Strategies to assess blood-brain barrier penetration. | Di L et al. | β | 2008 | β |
| Tanshinone IIB, a primary active constituent from Salvia miltiorrhiza, exerts neuroprotective effect via inhibition of neuronal apoptosis in vitro. | Yu XQ et al. | β | 2008 | β |
| Toward an optimal blood-brain barrier shuttle by synthesis and evaluation of peptide libraries. | Malakoutikhah M et al. | β | 2008 | β |
| Central nervous system drug disposition: the relationship between in situ brain permeability and brain free fraction. | Summerfield SG et al. | β | 2007 | β |
| Effects of traditionally used anxiolytic botanicals on enzymes of the gamma-aminobutyric acid (GABA) system. | Awad R et al. | β | 2007 | β |
| Recent progress toward nonpeptide ligands for the melanocortin-4 receptor. | Chen C | β | 2007 | β |
| InΒ vitro prediction of brain penetration - a case for free thinking? | Summerfield SG et al. | β | 2006 | β |
| Pharmacological and functional magnetic resonance imaging techniques in CNS drug discovery. | Fox GB et al. | β | 2006 | β |