68844-77-9 | 1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine

Packsize	Purity	Availability	Price	Discounted Price
10mg	98%	in stock	$60.00	$42.00
25mg	98%	in stock	$63.00	$45.00
50mg	98%	in stock	$119.00	$83.00
100mg	98%	in stock	$222.00	$155.00

Description

• Catalog Number: AB57649
• Chemical Name: 1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine
• CAS Number: 68844-77-9
• Molecular Formula: C28H31FN4O
• Molecular Weight: 458.5703432000001
• MDL Number: MFCD00153919
• SMILES: COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2

Computed Properties

• Complexity: 599
• Covalently-Bonded Unit Count: 1
• Heavy Atom Count: 34
• Hydrogen Bond Acceptor Count: 5
• Hydrogen Bond Donor Count: 1
• Rotatable Bond Count: 8
• XLogP3: 6

Literature

• Mechanism of As2O3-Induced Action Potential Prolongation and Using hiPS-CMs to Evaluate the Rescue Efficacy of Drugs With Different Rescue Mechanism.

  Toxicological sciences : an official journal of the Society of Toxicology 20170801

• Identification of potential drugs for Parkinson's disease based on a sub-pathway method.

  The International journal of neuroscience 20160101

• Bridging Functional and Structural Cardiotoxicity Assays Using Human Embryonic Stem Cell-Derived Cardiomyocytes for a More Comprehensive Risk Assessment.

  Toxicological sciences : an official journal of the Society of Toxicology 20151101

• Novel benzidine and diaminofluorene prolinamide derivatives as potent hepatitis C virus NS5A inhibitors.

  European journal of medicinal chemistry 20150828

• Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2.

  Journal of medicinal chemistry 20141126

• Allosteric modulators of the hERG K(+) channel: radioligand binding assays reveal allosteric characteristics of dofetilide analogs.

  Toxicology and applied pharmacology 20140101

• The central role of EED in the orchestration of polycomb group complexes.

  Nature communications 20140101

• Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11).

  Toxicological sciences : an official journal of the Society of Toxicology 20131201

• Refining the human iPSC-cardiomyocyte arrhythmic risk assessment model.

  Toxicological sciences : an official journal of the Society of Toxicology 20131201

• Human ether à-gogo K(+) channel 1 (hEag1) regulates MDA-MB-231 breast cancer cell migration through Orai1-dependent calcium entry.

  Journal of cellular physiology 20121201

• Validation of visualized transgenic zebrafish as a high throughput model to assay bradycardia related cardio toxicity risk candidates.

  Journal of applied toxicology : JAT 20121001

• Regulation of cell proliferation of human induced pluripotent stem cell-derived mesenchymal stem cells via ether-à-go-go 1 (hEAG1) potassium channel.

  American journal of physiology. Cell physiology 20120715

• An overview of bilastine metabolism during preclinical investigations.

  Drug and chemical toxicology 20120601

• Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.

  Journal of medicinal chemistry 20120524

• Effects of single therapeutic doses of promethazine, fexofenadine and olopatadine on psychomotor function and histamine-induced wheal- and flare-responses: a randomized double-blind, placebo-controlled study in healthy volunteers.

  Archives of dermatological research 20120501

• Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.

  Drug metabolism and disposition: the biological fate of chemicals 20120501

• Blood-brain barrier in vitro models as tools in drug discovery: assessment of the transport ranking of antihistaminic drugs.

  Die Pharmazie 20120501

• Drug screen targeted at Plasmodium liver stages identifies a potent multistage antimalarial drug.

  The Journal of infectious diseases 20120415

• Characterization of primary human hepatocytes, HepG2 cells, and HepaRG cells at the mRNA level and CYP activity in response to inducers and their predictivity for the detection of human hepatotoxins.

  Cell biology and toxicology 20120401

• Reversed chloroquine molecules as a strategy to overcome resistance in malaria.

  Current topics in medicinal chemistry 20120301

• Molecular determinants of pentamidine-induced hERG trafficking inhibition.

  Molecular pharmacology 20120201

• Selecting an invertebrate model host for the study of fungal pathogenesis.

  PLoS pathogens 20120201

• Using functional signatures to identify repositioned drugs for breast, myelogenous leukemia and prostate cancer.

  PLoS computational biology 20120201

• Experimental models of cryptococcosis.

  International journal of microbiology 20120101

• Toward a New Gold Standard for Early Safety: Automated Temperature-Controlled hERG Test on the PatchLiner.

  Frontiers in pharmacology 20120101

• Histamine H1 antagonists and clinical characteristics of febrile seizures.

  International journal of general medicine 20120101

• High throughput screening for small molecule enhancers of the interferon signaling pathway to drive next-generation antiviral drug discovery.

  PloS one 20120101

• Development and validation of an automated high-throughput system for zebrafish in vivo screenings.

  PloS one 20120101

• Triarylmethanes, a new class of cx50 inhibitors.

  Frontiers in pharmacology 20120101

• Astemizole synergizes calcitriol antiproliferative activity by inhibiting CYP24A1 and upregulating VDR: a novel approach for breast cancer therapy.

  PloS one 20120101

• [Benzimidazole and its derivatives--from fungicides to designer drugs. A new occupational and environmental hazards].

  Medycyna pracy 20120101

• Introduction of a modular automated voltage-clamp platform and its correlation with manual human Ether-à-go-go related gene voltage-clamp data.

  Assay and drug development technologies 20111201

• Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).

  PLoS computational biology 20111201

• Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R.

  Bioorganic & medicinal chemistry letters 20111101

• Estimating the risk of drug-induced proarrhythmia using human induced pluripotent stem cell-derived cardiomyocytes.

  Toxicological sciences : an official journal of the Society of Toxicology 20110901

• Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.

  Cardiovascular research 20110701

• [Material and mechanisms for evaluation of Shuanghuanglian injection induced pseudoanaphylactoid reactions].

  Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 20110701

• Species differences in intestinal metabolic activities of cytochrome P450 isoforms between cynomolgus monkeys and humans.

  Drug metabolism and pharmacokinetics 20110601

• Regulation of IGF-1-dependent cyclin D1 and E expression by hEag1 channels in MCF-7 cells: the critical role of hEag1 channels in G1 phase progression.

  Biochimica et biophysica acta 20110501

• Human EAG1 potassium channels in the epithelial-to-mesenchymal transition in lung cancer cells.

  Anticancer research 20110401

• Astemizole: an old anti-histamine as a new promising anti-cancer drug.

  Anti-cancer agents in medicinal chemistry 20110301

• Analysis of Relationship between Levofloxacin and Corrected QT Prolongation Using a Clinical Data Warehouse.

  Healthcare informatics research 20110301

• Roles of affinity and lipophilicity in the slow kinetics of prostanoid receptor antagonists on isolated smooth muscle preparations.

  British journal of pharmacology 20110201

• Overview of diagnosis and management of paediatric headache. Part II: therapeutic management.

  The journal of headache and pain 20110201

• Identification of human liver cytochrome P450 enzymes involved in the metabolism of SCH 530348 (Vorapaxar), a potent oral thrombin protease-activated receptor 1 antagonist.

  Drug metabolism and disposition: the biological fate of chemicals 20110101

• A research agenda for malaria eradication: basic science and enabling technologies.

  PLoS medicine 20110101

• Sex differences in drug disposition.

  Journal of biomedicine & biotechnology 20110101

• Functional K(v)10.1 channels localize to the inner nuclear membrane.

  PloS one 20110101

• hERGAPDbase: a database documenting hERG channel inhibitory potentials and APD-prolongation activities of chemical compounds.

  Database : the journal of biological databases and curation 20110101

• Fluticasone/formoterol combination therapy is as effective as fluticasone/salmeterol in the treatment of asthma, but has a more rapid onset of action: an open-label, randomized study.

  BMC pulmonary medicine 20110101

• Update on the optimal use of voriconazole for invasive fungal infections.

  Infection and drug resistance 20110101

• Diabetic microvascular complications: possible targets for improved macrovascular outcomes.

  International journal of nephrology and renovascular disease 20110101

• A novel study design for antibiotic trials in acute exacerbations of COPD: MAESTRAL methodology.

  International journal of chronic obstructive pulmonary disease 20110101

• Tumor cell-selective apoptosis induction through targeting of K(V)10.1 via bifunctional TRAIL antibody.

  Molecular cancer 20110101

• Identification of novel functional inhibitors of acid sphingomyelinase.

  PloS one 20110101

• On-chip constructive cell-network study (II): on-chip quasi-in vivo cardiac toxicity assay for ventricular tachycardia/fibrillation measurement using ring-shaped closed circuit microelectrode with lined-up cardiomyocyte cell network.

  Journal of nanobiotechnology 20110101

• Discovery of potent, novel, non-toxic anti-malarial compounds via quantum modelling, virtual screening and in vitro experimental validation.

  Malaria journal 20110101

• Protein 4.1B contributes to the organization of peripheral myelinated axons.

  PloS one 20110101

• Parallel screening of FDA-approved antineoplastic drugs for identifying sensitizers of TRAIL-induced apoptosis in cancer cells.

  BMC cancer 20110101

• A predictive ligand-based Bayesian model for human drug-induced liver injury.

  Drug metabolism and disposition: the biological fate of chemicals 20101201

• Identification of human Ether-à-go-go related gene modulators by three screening platforms in an academic drug-discovery setting.

  Assay and drug development technologies 20101201

• QTc interval prolongation by fexofenadine in healthy human volunteers and its correlation with plasma levels of fexofenadine: A demonstration of anticlockwise hysteresis.

  Indian journal of pharmacology 20101201

• Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method.

  Healthcare informatics research 20101201

• Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.

  Bioorganic & medicinal chemistry letters 20101101

• An aqueous extract of Poncirus fructus activates the prokinetic activity of 5-HT receptor subtype 4 without hERG interaction.

  Journal of ethnopharmacology 20101028

• Discovery of potent small-molecule inhibitors of multidrug-resistant Plasmodium falciparum using a novel miniaturized high-throughput luciferase-based assay.

  Antimicrobial agents and chemotherapy 20100901

• Simultaneous gene expression signature of heart and peripheral blood mononuclear cells in astemizole-treated rats.

  Archives of toxicology 20100801

• Lack of appreciable species differences in nonspecific microsomal binding.

  Journal of pharmaceutical sciences 20100801

• Effects of K openers on the QT prolongation induced by HERG-blocking drugs in guinea-pigs.

  The Journal of pharmacy and pharmacology 20100701

• Visualizing voltage dynamics in zebrafish heart.

  The Journal of physiology 20100615

• Protein binding-dependent decreases in hERG channel blocker potency assessed by whole-cell voltage clamp in serum.

  Journal of cardiovascular pharmacology 20100401

• Improved methodology for identifying the teratogenic potential in early drug development of hERG channel blocking drugs.

  Reproductive toxicology (Elmsford, N.Y.) 20100401

• The pathophysiology, diagnosis and treatment of allergic rhinitis.

  Allergy, asthma & immunology research 20100401

• Astemizole and an analogue promote fungicidal activity of fluconazole against Cryptococcus neoformans var. grubii and Cryptococcus gattii.

  Medical mycology 20100301

• Neuropharmacology of vestibular system disorders.

  Current neuropharmacology 20100301

• Identification of novel substrates for human cytochrome P450 2J2.

  Drug metabolism and disposition: the biological fate of chemicals 20100201

• Calcitriol inhibits Ether-à go-go potassium channel expression and cell proliferation in human breast cancer cells.

  Experimental cell research 20100201

• The intermediate conductance Ca2+-activated K+ channel inhibitor TRAM-34 stimulates proliferation of breast cancer cells via activation of oestrogen receptors.

  British journal of pharmacology 20100201

• The potassium channel Ether à go-go is a novel prognostic factor with functional relevance in acute myeloid leukemia.

  Molecular cancer 20100101

• Selective interaction of lansoprazole and astemizole with tau polymers: potential new clinical use in diagnosis of Alzheimer's disease.

  Journal of Alzheimer's disease : JAD 20100101

• Are the immunocompetence and the presence of metazoan parasites in cyprinid fish affected by reproductive efforts of cyprinid fish?

  Journal of biomedicine & biotechnology 20100101

• Treatment of congestion in upper respiratory diseases.

  International journal of general medicine 20100101

• Preparation and evaluation of transdermal plasters containing norfloxacin: a novel treatment for burn wound healing.

  Eplasty 20100101

• Mapping pharmaceuticals in rat brain sections using MALDI imaging mass spectrometry.

  Methods in molecular biology (Clifton, N.J.) 20100101

• Selective inhibitors of Kv11.1 regulate IL-6 expression by macrophages in response to TLR/IL-1R ligands.

  TheScientificWorldJournal 20100101

• Emerging treatments in the management of schizophrenia - focus on sertindole.

  Drug design, development and therapy 20100101

• Fosaprepitant and aprepitant: an update of the evidence for their place in the prevention of chemotherapy-induced nausea and vomiting.

  Core evidence 20100101

• Development, clinical utility, and place in therapy of posaconazole for prevention and treatment of invasive fungal infections.

  Drug design, development and therapy 20100101

• Eag and HERG potassium channels as novel therapeutic targets in cancer.

  World journal of surgical oncology 20100101

• Clinical utility and patient adherence with ebastine for allergic rhinitis.

  Patient preference and adherence 20100101

• Retinal redox stress and remodeling in cardiometabolic syndrome and diabetes.

  Oxidative medicine and cellular longevity 20100101

• Management of tinea capitis in childhood.

  Clinical, cosmetic and investigational dermatology 20100101

• Role of posaconazole in the treatment of oropharyngeal candidiasis.

  Infection and drug resistance 20100101

• Natural product taking its own place!!!

  Pharmacognosy research 20100101

• Stereoselective Inhibition of the hERG1 Potassium Channel.

  Frontiers in pharmacology 20100101

• Genetic deficiency of carnitine/organic cation transporter 2 (slc22a5) is associated with altered tissue distribution of its substrate pyrilamine in mice.

  Biopharmaceutics & drug disposition 20091201

• Inhibition of the human ether-a-go-go-related gene (HERG) K+ channels by Lindera erythrocarpa.

  Journal of Korean medical science 20091201

• A panel of cytochrome P450 BM3 variants to produce drug metabolites and diversify lead compounds.

  Chemistry (Weinheim an der Bergstrasse, Germany) 20091102

• A new homogeneous high-throughput screening assay for profiling compound activity on the human ether-a-go-go-related gene channel.

  Analytical biochemistry 20091101

• Efavirenz: a decade of clinical experience in the treatment of HIV.

  The Journal of antimicrobial chemotherapy 20091101

• Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonists.

  Bioorganic & medicinal chemistry letters 20091101

• Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs.

  Bioorganic & medicinal chemistry letters 20090901

• Histamine H1 receptor induces cytosolic calcium increase and aquaporin translocation in human salivary gland cells.

  The Journal of pharmacology and experimental therapeutics 20090801

• Iatrogenic QT Abnormalities and Fatal Arrhythmias: Mechanisms and Clinical Significance.

  Current cardiology reviews 20090801

• Drug discovery for schistosomiasis: hit and lead compounds identified in a library of known drugs by medium-throughput phenotypic screening.

  PLoS neglected tropical diseases 20090701

• Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease.

  Journal of medicinal chemistry 20090514

• Managing toxicities and optimal dosing of targeted drugs in advanced kidney cancer.

  Current oncology (Toronto, Ont.) 20090501

• MALDI-tandem mass spectrometry imaging of astemizole and its primary metabolite in rat brain sections.

  Bioanalysis 20090501

• Estrogens and human papilloma virus oncogenes regulate human ether-à-go-go-1 potassium channel expression.

  Cancer research 20090415

• Intracellular potassium stabilizes human ether-à-go-go-related gene channels for export from endoplasmic reticulum.

  Molecular pharmacology 20090401

• Chloroquine-astemizole hybrids with potent in vitro and in vivo antiplasmodial activity.

  Bioorganic & medicinal chemistry letters 20090115

• The role of ether-a-go-go-related gene K(+) channels in glucocorticoid inhibition of adrenocorticotropin release by rat pituitary cells.

  Regulatory peptides 20090108

• Use of high-density tiling microarrays to identify mutations globally and elucidate mechanisms of drug resistance in Plasmodium falciparum.

  Genome biology 20090101

• Prevalence and characteristics of aquagenic pruritus in a young African population.

  BMC dermatology 20090101

• A chemogenomics view on protein-ligand spaces.

  BMC bioinformatics 20090101

• Histamine H(3) receptor-mediated signaling protects mice from cerebral malaria.

  PloS one 20090101

• Treatment of allergic rhinitis in infants and children: efficacy and safety of second-generation antihistamines and the leukotriene receptor antagonist montelukast.

  Drugs 20090101

• Sudden elevation of liver enzymes in a 64-year-old patient: a case report.

  Cases journal 20090101

• Autologous serum skin test.

  Indian journal of dermatology 20090101

• Contact urticaria: present scenario.

  Indian journal of dermatology 20090101

• Management of difficult urticaria.

  Indian journal of dermatology 20090101

• Malarial parasite pathogenesis and drug targets.

  F1000 biology reports 20090101

• Ebastine in the light of CONGA recommendations for the development of third-generation antihistamines.

  Journal of asthma and allergy 20090101

• Eag1 expression interferes with hypoxia homeostasis and induces angiogenesis in tumors.

  The Journal of biological chemistry 20081226

• An ion channel library for drug discovery and safety screening on automated platforms.

  Assay and drug development technologies 20081201

• Drug binding to the inactivated state is necessary but not sufficient for high-affinity binding to human ether-à-go-go-related gene channels.

  Molecular pharmacology 20081101

• (E)-1,1'-Bis[(E)-but-2-en-yl]-3,3'-(propane-1,3-di-yl)bis-(1H-benzimidazol-3-ium) dibromide monohydrate.

  Acta crystallographica. Section E, Structure reports online 20081101

• Prediction of drug-induced QT interval prolongation in telemetered common marmosets.

  The Journal of toxicological sciences 20080801

• The effects of topical (gel) astemizole and terfenadine on wound healing.

  Indian journal of pharmacology 20080801

• Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.

  Journal of medicinal chemistry 20080724

• Pharmacological interventions for clozapine-induced hypersalivation.

  Schizophrenia bulletin 20080701

• Receptor-independent, vacuolar ATPase-mediated cellular uptake of histamine receptor-1 ligands: possible origin of pharmacological distortions and side effects.

  Toxicology and applied pharmacology 20080615

• Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).

  Journal of medicinal chemistry 20080612

• Pharmacological separation of hEAG and hERG K+ channel function in the human mammary carcinoma cell line MCF-7.

  Oncology reports 20080601

• Enzyme systems of detoxication - overview of recent approaches.

  Interdisciplinary toxicology 20080601

• Practical recommendations on the use of lenalidomide in the management of myelodysplastic syndromes.

  Annals of hematology 20080501

• Modeling the hERG potassium channel in a phospholipid bilayer: Molecular dynamics and drug docking studies.

  Journal of computational chemistry 20080415

• Development of the predictor HERG fluorescence polarization assay using a membrane protein enrichment approach.

  Assay and drug development technologies 20080401

• Prevention of chemotherapy-induced nausea and vomiting: focus on fosaprepitant.

  Therapeutics and clinical risk management 20080401

• Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.

  Journal of medicinal chemistry 20080124

• Canadian supportive care recommendations for the management of neutropenia in patients with cancer.

  Current oncology (Toronto, Ont.) 20080101

• Temporal variability of QT interval and changes in T wave morphology in dogs as markers of the clinical risk of drug-induced proarrhythmia.

  Journal of pharmacological and toxicological methods 20080101

• Pharmacological interventions for clozapine-induced hypersalivation.

  The Cochrane database of systematic reviews 20080101

• The possible involvement of hyperpolarizing mechanisms in histamine-induced relaxation of the rat portal vein.

  Journal of smooth muscle research = Nihon Heikatsukin Gakkai kikanshi 20080101

• Role of cytochrome P450 in drug interactions.

  Nutrition & metabolism 20080101

• Clofazimine inhibits human Kv1.3 potassium channel by perturbing calcium oscillation in T lymphocytes.

  PloS one 20080101

• [Histamine and the convulsive threshold or effectiveness of antiepileptic drugs].

  Przeglad lekarski 20080101

• Generalized lichen nitidus in childhood.

  Indian journal of dermatology 20080101

• Discovery of the first nonpeptidic, small-molecule, highly selective somatostatin receptor subtype 5 antagonists: a chemogenomics approach.

  Journal of medicinal chemistry 20071213

• From astemizole to a novel hit series of small-molecule somatostatin 5 receptor antagonists via GPCR affinity profiling.

  Journal of medicinal chemistry 20071213

• A dose-ranging study of tiotropium delivered via Respimat Soft Mist Inhaler or HandiHaler in COPD patients.

  International journal of chronic obstructive pulmonary disease 20071201

• IGF-1 activates hEAG K(+) channels through an Akt-dependent signaling pathway in breast cancer cells: role in cell proliferation.

  Journal of cellular physiology 20070901

• Comparative evaluation of hERG potassium channel blockade by antipsychotics.

  Methods and findings in experimental and clinical pharmacology 20070901

• QT prolongation and safety in the Indian population.

  Current drug safety 20070901

• Role of posaconazole in the management of oropharyngeal and esophageal candidiasis.

  Therapeutics and clinical risk management 20070801

• Embryonic cardiac arrhythmia and generation of reactive oxygen species: common teratogenic mechanism for IKr blocking drugs.

  Reproductive toxicology (Elmsford, N.Y.) 20070701

• Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel.

  Journal of medicinal chemistry 20070628

• Effect of tecastemizole on pulmonary and cutaneous allergic inflammatory responses.

  Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology 20070601

• Toxicological significance of mechanism-based inactivation of cytochrome p450 enzymes by drugs.

  Critical reviews in toxicology 20070601

• A cell-based Rb(+)-flux assay of the Kv1.3 potassium channel.

  Assay and drug development technologies 20070601

• A brief review of moxifloxacin in the treatment of elderly patients with community-acquired pneumonia (CAP).

  Clinical interventions in aging 20070601

• Seasonal allergic rhinitis in adolescents and adults.

  BMJ clinical evidence 20070401

• Selective inhibition of Kir currents by antihistamines.

  European journal of pharmacology 20070308

• Solubility-excipient classification gradient maps.

  Pharmaceutical research 20070301

• Generalized lichen nitidus successfully treated with narrow-band UVB phototherapy: two cases report.

  Journal of Korean medical science 20070201

• Methodological validation of an existing telemetry system for QT evaluation in conscious guinea pigs.

  Journal of pharmacological and toxicological methods 20070101

• QT prolongation in guinea pigs for preliminary screening of torsadogenicity of drugs and drug-candidates. II.

  Journal of applied toxicology : JAT 20070101

• Combinatorial computational approaches to identify tetracycline derivatives as flavivirus inhibitors.

  PloS one 20070101

• New proposals for testing drugs with IKr-blocking activity to determine their teratogenic potential.

  Current pharmaceutical design 20070101

• Aprepitant: the evidence for its place in the prevention of chemotherapy-induced nausea and vomiting.

  Core evidence 20070101

• Electrophysiological effects of brompheniramine on cardiac ion channels and action potential.

  Pharmacological research 20061201

• Inter-individual variation of cytochrome P4502J2 expression and catalytic activities in liver microsomes from Japanese and Caucasian populations.

  Xenobiotica; the fate of foreign compounds in biological systems 20061201

• Long QT syndrome in a patient with allergic rhinoconjunctivitis and auto-immune diabetes: focus on the choice of anti-H1 drugs.

  European annals of allergy and clinical immunology 20061201

• Contribution of solid-state properties to the aqueous solubility of drugs.

  European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 20061101

• PAMPA - excipient classification gradient map.

  Pharmaceutical research 20061101

• QT-RR relationships and suitable QT correction formulas for halothane-anesthetized dogs.

  The Journal of toxicological sciences 20061001

• Different relevance of inactivation and F468 residue in the mechanisms of hEag1 channel blockage by astemizole, imipramine and dofetilide.

  FEBS letters 20060918

• H1 histamine receptor antagonists induce genotoxic and caspase-2-dependent apoptosis in human melanoma cells.

  Carcinogenesis 20060901

• A clinical drug library screen identifies astemizole as an antimalarial agent.

  Nature chemical biology 20060801

• In vivo recording of adult zebrafish electrocardiogram and assessment of drug-induced QT prolongation.

  American journal of physiology. Heart and circulatory physiology 20060701

• Merg1a K+ channel induces skeletal muscle atrophy by activating the ubiquitin proteasome pathway.

  FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20060701

• An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.

  Journal of medicinal chemistry 20060601

• An extension of the Early Treatment Diabetic Retinopathy Study (ETDRS) system for grading of diabetic macular edema in the Astemizole Retinopathy Trial.

  Current eye research 20060601

• Microsphere-based protease assays and screening application for lethal factor and factor Xa.

  Cytometry. Part A : the journal of the International Society for Analytical Cytology 20060501

• Development, validation and utility of an in vitro technique for assessment of potential clinical drug-drug interactions involving P-glycoprotein.

  European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 20060401

• A lingering mistake.

  CMAJ : Canadian Medical Association journal = journal de l'Association medicale canadienne 20060227

• Life-threatening bradyarrhythmia after massive azithromycin overdose.

  Pharmacotherapy 20060101

• A possible case of spontaneous Loa loa encephalopathy associated with a glomerulopathy.

  Filaria journal 20060101

• Treatment for allergic rhinitis and chronic idiopathic urticaria: focus on oral antihistamines.

  The Annals of pharmacotherapy 20051201

• Safety and tolerability of oral antifungal agents in the treatment of fungal nail disease: a proven reality.

  Therapeutics and clinical risk management 20051201

• Grape fruit juice-drug interactions.

  Pakistan journal of pharmaceutical sciences 20051001

• Histamine H1 antagonists block M-currents in dissociated rat cortical neurons.

  Brain research 20050928

• Evaluation of pharmacokinetic interaction between cetirizine and ritonavir, an HIV-1 protease inhibitor, in healthy male volunteers.

  European journal of clinical pharmacology 20050601

• Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk).

  Journal of medicinal chemistry 20050505

• Molecular cloning and kinetic characterization of an aldehyde dehydrogenase gene in Klebsiella pneumoniae.

  Journal of the Formosan Medical Association = Taiwan yi zhi 20050401

• Effect of trazodone on hERG channel current and QT-interval.

  European journal of pharmacology 20050307

• Identifying modulators of hERG channel activity using the PatchXpress planar patch clamp.

  Journal of biomolecular screening 20050301

• A case of pheniramine dependence.

  Substance abuse 20050301

• Clinical outcomes and management of mechanism-based inhibition of cytochrome P450 3A4.

  Therapeutics and clinical risk management 20050301

• Identification of human P450 isoforms involved in the metabolism of the antiallergic drug, oxatomide, and its kinetic parameters and inhibition constants.

  Biological & pharmaceutical bulletin 20050201

• [Torsades de pointes caused by cetirizine overdose].

  Archives des maladies du coeur et des vaisseaux 20050201

• Characterization of a hERG screen using the IonWorks HT: comparison to a hERG rubidium efflux screen.

  Assay and drug development technologies 20050201

• Identification and functional characterization of novel CYP2J2 variants: G312R variant causes loss of enzyme catalytic activity.

  Pharmacogenetics and genomics 20050201

• Mechanism-based inhibition of cytochrome P450 3A4 by therapeutic drugs.

  Clinical pharmacokinetics 20050101

• Generalized lichen nitidus.

  Pediatric dermatology 20050101

• Estimation of potency of HERG channel blockers: impact of voltage protocol and temperature.

  Journal of pharmacological and toxicological methods 20050101

• In vivo antimuscarinic actions of the third generation antihistaminergic agent, desloratadine.

  BMC pharmacology 20050101

• Effect of histamine receptor antagonists on aminophylline-induced seizures and lethality in mice.

  Pharmacological reports : PR 20050101

• [Efficacy and safety of astemizole in the treatment of allergic rhinitis and urticaria: a systematic review with meta-analysis].

  Revista alergia Mexico (Tecamachalco, Puebla, Mexico : 1993) 20050101

• Digital drug discovery.

  Genome biology 20050101

• QT PRODACT: in vivo QT assay in the conscious dog for assessing the potential for QT interval prolongation by human pharmaceuticals.

  Journal of pharmacological sciences 20050101

• QT PRODACT: in vivo QT assay with a conscious monkey for assessment of the potential for drug-induced QT interval prolongation.

  Journal of pharmacological sciences 20050101

• Comparison of alamar blue and MTT assays for high through-put screening.

  Toxicology in vitro : an international journal published in association with BIBRA 20041001

• Mechanism of block of hEag1 K+ channels by imipramine and astemizole.

  The Journal of general physiology 20041001

• Automated tight seal electrophysiology for assessing the potential hERG liability of pharmaceutical compounds.

  Assay and drug development technologies 20041001

• Functional and molecular identification of intermediate-conductance Ca(2+)-activated K(+) channels in breast cancer cells: association with cell cycle progression.

  American journal of physiology. Cell physiology 20040701

• Validation of a [3H]astemizole binding assay in HEK293 cells expressing HERG K+ channels.

  Journal of pharmacological sciences 20040701

• Identification of human p450 isoforms involved in the metabolism of the antiallergic drug, oxatomide, and its inhibitory effect on enzyme activity.

  Biological & pharmaceutical bulletin 20040501

• Gateways to clinical trials.

  Methods and findings in experimental and clinical pharmacology 20040101

• Quinolone safety and efficacy more important than potency.

  Emerging infectious diseases 20040101

• QT prolongation in anaesthetized guinea-pigs: an experimental approach for preliminary screening of torsadogenicity of drugs and drug candidates.

  Journal of applied toxicology : JAT 20040101

• Actual therapeutic management of allergic and hyperreactive nasal disorders.

  GMS current topics in otorhinolaryngology, head and neck surgery 20040101

• Zebrafish embryos express an orthologue of HERG and are sensitive toward a range of QT-prolonging drugs inducing severe arrhythmia.

  Toxicology and applied pharmacology 20031215

• Gateways to clinical trials.

  Methods and findings in experimental and clinical pharmacology 20031201

• Effects of imatinib mesylate (STI571, Glivec) on the pharmacokinetics of simvastatin, a cytochrome p450 3A4 substrate, in patients with chronic myeloid leukaemia.

  British journal of cancer 20031117

• Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.

  Bioorganic & medicinal chemistry letters 20030818

• Interaction of astemizole, an H1 receptor antagonist, with conventional antiepileptic drugs in mice.

  Pharmacology, biochemistry, and behavior 20030801

• Role of the cytosolic chaperones Hsp70 and Hsp90 in maturation of the cardiac potassium channel HERG.

  Circulation research 20030627

• Pregnancy outcome after gestational exposure to loratadine or antihistamines: a prospective controlled cohort study.

  The Journal of allergy and clinical immunology 20030601

• [Effects of clinically available drugs on the repolarization process of the heart assessed by the in vivo canine models].

  Nihon yakurigaku zasshi. Folia pharmacologica Japonica 20030601

• In vitro inhibition of human small intestinal and liver microsomal astemizole O-demethylation: different contribution of CYP2J2 in the small intestine and liver.

  Xenobiotica; the fate of foreign compounds in biological systems 20030601

• Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior.

  Journal of medicinal chemistry 20030522

• Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.

  Journal of medicinal chemistry 20030424

• Sedation and performance impairment of diphenhydramine and second-generation antihistamines: a meta-analysis.

  The Journal of allergy and clinical immunology 20030401

• Detection of proarrhythmia in the female rabbit heart: blinded validation.

  Journal of cardiovascular electrophysiology 20030301

• Functional and pharmacological properties of canine ERG potassium channels.

  American journal of physiology. Heart and circulatory physiology 20030101

• Lopinavir/ritonavir: a review of its use in the management of HIV infection.

  Drugs 20030101

• Antihistamines.

  Psychosomatics 20030101

• Development of neuroleptic agents: pharmacogenetics and current safety issues of regulatory concern.

  Dialogues in clinical neuroscience 20021201

• Involvement of CYP2J2 on the intestinal first-pass metabolism of antihistamine drug, astemizole.

  Drug metabolism and disposition: the biological fate of chemicals 20021101

• Posttranslational modulation of glucocorticoid feedback inhibition at the pituitary level.

  Endocrinology 20021001

• Histamine inhibits KCNQ2/KCNQ3 channel current via recombinant histamine H(1) receptors.

  Neuroscience letters 20020816

• The functional properties of the human ether-à-go-go-like (HELK2) K+ channel.

  The European journal of neuroscience 20020801

• Next generation antihistamines: therapeutic rationale, accomplishments and advances.

  Expert opinion on investigational drugs 20020601

• Development of telemetry system in the common marmoset--cardiovascular effects of astemizole and nicardipine.

  The Journal of toxicological sciences 20020501

• Cardiotoxicity of new antihistamines and cisapride.

  Toxicology letters 20020227

• The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations.

  The Journal of biological chemistry 20020215

• Antihistamines in late-phase clinical development for allergic disease.

  Expert opinion on investigational drugs 20020201

• Assessment of the relationship between hyperalgesia and peripheral inflammation in magnesium-deficient rats.

  Life sciences 20020118

• Relationship between direct-to-consumer advertising and physician diagnosing and prescribing.

  American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists 20020101

• Comparative effects of maternal prenatal and postnatal exposures to astemizole on reproductive parameters of rats.

  Neurotoxicology and teratology 20020101

• Potential cardiac toxicity of H1-antihistamines.

  Clinical allergy and immunology 20020101

• [Risk of drug interactions. Combinations of drugs associated with ventricular arrhythmias].

  Revista de investigacion clinica; organo del Hospital de Enfermedades de la Nutricion 20020101

• Second generation antihistamines in the treatment of seasonal allergic rhinitis due to Parietaria and cypress pollen.

  Pharmacological research 20011201

• A case series of drug-induced long QT syndrome and Torsade de Pointes.

  Singapore medical journal 20011201

• Inhibition of depolarization-induced [3H]noradrenaline release from SH-SY5Y human neuroblastoma cells by some second-generation H(1) receptor antagonists through blockade of store-operated Ca(2+) channels (SOCs).

  Biochemical pharmacology 20011101

• Development and evaluation of high throughput functional assay methods for HERG potassium channel.

  Journal of biomolecular screening 20011001

• Triamcinolone: new and old indications.

  Expert opinion on pharmacotherapy 20010701

• Determination of astemizole in pharmaceutical preparations using spectrophotometric methods.

  Journal of pharmaceutical and biomedical analysis 20010601

• [Effect of olopatadine hydrochloride, a novel antiallergic agent, on the QT interval in dogs].

  Nihon yakurigaku zasshi. Folia pharmacologica Japonica 20010601

• Recurrent syncope. Drug induced long QT syndrome.

  Postgraduate medical journal 20010501

• Transgenic mice overexpressing human KvLQT1 dominant-negative isoform. Part II: Pharmacological profile.

  Cardiovascular research 20010501

• Role of central histaminergic system in lorazepam withdrawal syndrome in rats.

  Pharmacology, biochemistry, and behavior 20010401

• Acute canine model for drug-induced Torsades de Pointes in drug safety evaluation-influences of anesthesia and validation with quinidine and astemizole.

  Toxicological sciences : an official journal of the Society of Toxicology 20010301

• Pharmacokinetic and safety profile of desloratadine and fexofenadine when coadministered with azithromycin: a randomized, placebo-controlled, parallel-group study.

  Clinical therapeutics 20010301

• Involvement of multiple human cytochromes P450 in the liver microsomal metabolism of astemizole and a comparison with terfenadine.

  British journal of clinical pharmacology 20010201

• Safety of antihistamines in children.

  Drug safety 20010101

• Saquinavir soft gelatin capsule: a comparative safety review.

  Drug safety 20010101

• [Drug interactions with antiretroviral agents].

  Therapie 20010101

• Comparative safety of the different macrolides.

  International journal of antimicrobial agents 20010101

• [The effect of second generation histamine antagonists on the heart].

  Pneumonologia i alergologia polska 20010101

• Changes in the K+ current-density of MCF-7 cells during progression through the cell cycle: possible involvement of a h-ether.a-gogo K+ channel.

  Receptors & channels 20010101

• Influence of chronic treatment with H1 receptor antagonists on the anticonvulsant activity of antiepileptic drugs.

  Polish journal of pharmacology 20010101

• Effect of oxatomide, an antiallergic agent, on QT interval in dogs.

  Arzneimittel-Forschung 20010101

• Antihistamines and the torsade de point in children with allergic rhinitis.

  European review for medical and pharmacological sciences 20010101

• Emerging role of drug interaction studies in drug development: the good, the bad, and the unknown.

  Psychopharmacology bulletin 20010101

• Pharmacological blockade of ERG K(+) channels and Ca(2+) influx through store-operated channels exerts opposite effects on intracellular Ca(2+) oscillations in pituitary GH(3) cells.

  Molecular pharmacology 20001101

• Inhibition of HERG1 K(+) channels by the novel second-generation antihistamine mizolastine.

  British journal of pharmacology 20001101

• A new model of allergic rhinitis in rats by topical sensitization and evaluation of H(1)-receptor antagonists.

  Immunopharmacology 20000601

• Redox state dependency of HERGS631C channel pharmacology: relation to C-type inactivation.

  FEBS letters 20000526

• Correction of defective protein trafficking of a mutant HERG potassium channel in human long QT syndrome. Pharmacological and temperature effects.

  The Journal of biological chemistry 19991029

• Epinastine, a nonsedating histamine H1 receptor antagonist, has a negligible effect on HERG channel.

  European journal of pharmacology 19990625

• Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole.

  Journal of cardiovascular electrophysiology 19990601

• Risk of ventricular arrhythmias associated with nonsedating antihistamine drugs.

  British journal of clinical pharmacology 19990301

• Molecular basis for the lack of HERG K+ channel block-related cardiotoxicity by the H1 receptor blocker cetirizine compared with other second-generation antihistamines.

  Molecular pharmacology 19980701

• Astemizole-induced torsades de pointes in a patient with vasospastic angina.

  Japanese circulation journal 19980301

• Seizure during risperidone treatment in an elderly woman treated with concomitant medications.

  The Journal of clinical psychiatry 19980201

• Quinine may trigger torsades de pointes during astemizole therapy.

  Pacing and clinical electrophysiology : PACE 19970801

• Effects of magnesium sulfate on the canine cardiovascular system complicating astemizole overdose.

  Journal of cardiovascular pharmacology 19970601

• Effects of the anti-allergics astemizole and norastemizole on Fc epsilon RI receptor-mediated signal transduction processes.

  European journal of pharmacology 19970312

• Combined use of astemizole and ketoconazole resulting in torsade de pointes.

  Journal of the Formosan Medical Association = Taiwan yi zhi 19970201

• [Serous otitis media. Comparative study of carbinoxamine- pseudoephedrine vs astemizole-pseudoephedrine].

  Revista alergia Mexico (Tecamachalco, Puebla, Mexico : 1993) 19970101

• Torsade de pointes with an antihistamine metabolite: potassium channel blockade with desmethylastemizole.

  Journal of the American College of Cardiology 19961115

• Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole.

  FEBS letters 19960429

• Drug-induced torsades de pointes in one patient with congenital long QT syndrome.

  International journal of cardiology 19960419

• Astemizole in the treatment of granulocyte colony-stimulating factor-induced bone pain.

  Annals of internal medicine 19950801

• Inhibition of mediator release in RBL-2H3 cells by some H1-antagonist derived anti-allergic drugs: relation to lipophilicity and membrane effects.

  Inflammation research : official journal of the European Histamine Research Society ... [et al.] 19950201

• Astemizole-D causes less sleep impairment than loratadine-D.

  The Journal of international medical research 19950101

• Torsades de pointes ventricular tachycardia associated with overdose of astemizole.

  Mayo Clinic proceedings 19940601

• Torsades de pointes associated with astemizole (Hismanal) therapy.

  Archives of internal medicine 19931213

• Cardiac arrest in a young woman with the long QT syndrome and concomitant astemizole ingestion.

  British heart journal 19931101

• Public health problems and the rapid estimation of the size of the population at risk. Torsades de pointes and the use of terfenadine and astemizole in The Netherlands.

  Pharmacy world & science : PWS 19931015

• Is QT interval prolongation harmful? A regulatory perspective.

  The American journal of cardiology 19930826

• Torsade de pointes induced by astemizole in a patient with prolongation of the QT interval.

  American heart journal 19930501

• Effect of astemizole on antigen-mediated histamine release from the blood of patients with allergic rhinitis.

  Allergy 19921201

• Canine in vivo tracheal chemotaxis of eosinophils to antigen in sensitized dogs: inhibition by a steroid, a systemic lazaroid U-78517F, and several topical H1 antihistamines.

  The American review of respiratory disease 19920901

• Controlled trial of H1 antagonists in the treatment of chronic idiopathic urticaria.

  Annals of allergy 19911001

• Human immunodeficiency virus-associated eosinophilic folliculitis. A unique dermatosis associated with advanced human immunodeficiency virus infection.

  Archives of dermatology 19910201

• Prolonged benefit in the treatment of chronic idiopathic urticaria with astemizole.

  Annals of allergy 19900901

• Effects of azatadine, terfenadine, and astemizole on allergen-induced nasal provocation.

  Annals of allergy 19900201

• Cetirizine vs astemizole in the treatment of chronic idiopathic urticaria.

  The Journal of international medical research 19900101

• [Therapy of acute and chronic urticaria and of Quincke's edema].

  Schweizerische Rundschau fur Medizin Praxis = Revue suisse de medecine Praxis 19890516

• Treatment of chronic idiopathic urticaria with astemizole.

  Cleveland Clinic journal of medicine 19890501

• Comparative study of astemizole and terfenadine in the treatment of chronic idiopathic urticaria. A randomized double-blind study of 40 patients.

  Annals of allergy 19890401

• 'In vivo' and 'in vitro' evaluation of four antihistamines (astemizole, azatadine, mequitazine, terfenadine).

  Allergologia et immunopathologia 19890101

• Generalized lichen nitidus. Report of two cases treated with astemizol.

  International journal of dermatology 19890101

• Astemizole. Its use in the treatment of patients with chronic vertigo.

  Archives of otolaryngology--head & neck surgery 19870501

• Controlled clinical assessment of astemizole in the treatment of chronic idiopathic urticaria and angioedema.

  Journal of the American Academy of Dermatology 19870401

• [Treatment of chronic urticaria with astemizole: a multicenter pediatric study].

  Allergie et immunologie 19870401

• The treatment of mild to severe chronic idiopathic urticaria with astemizole: double-blind and open trials.

  The Journal of allergy and clinical immunology 19861201

• Double-blind comparison of astemizole and terfenadine in the treatment of chronic urticaria.

  Pharmatherapeutica 19860101

• Efficacy and safety of astemizole, a long-acting and nonsedating H1 antagonist for the treatment of chronic idiopathic urticaria.

  The Journal of allergy and clinical immunology 19860101

• Effect of the nonsedative H1-receptor antagonist astemizole in perennial allergic and nonallergic rhinitis.

  The Journal of allergy and clinical immunology 19850601

• [Comparison of astemizole and terfenadine in the treatment of chronic urticaria. A randomized double-blind study of 40 patients].

  Zeitschrift fur Hautkrankheiten 19850101

• Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines).

  Clinical pharmacokinetics 19850101

• Astemizole: its use in patients with chronic vertigo and eng signs--a pilot study of a new drug.

  The Laryngoscope 19830701