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68844-77-9 | 1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine
CAS No: 68844-77-9 Catalog No: AG003DSP MDL No:MFCD00153919
Product Description
Catalog Number:
AG003DSP
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:
458.5703
MDL Number:
MFCD00153919
IUPAC Name:
1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl]benzimidazol-2-amine
InChI:
InChI=1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31)
InChI Key:
GXDALQBWZGODGZ-UHFFFAOYSA-N
SMILES:
COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2
EC Number:
272-441-9
UNII:
7HU6337315
Properties
Complexity:
599
Compound Is Canonicalized:
Yes
Covalently-Bonded Unit Count:
1
Defined Atom Stereocenter Count:
0
Defined Bond Stereocenter Count:
0
Exact Mass:
458.248g/mol
Formal Charge:
0
Heavy Atom Count:
34
Hydrogen Bond Acceptor Count:
5
Hydrogen Bond Donor Count:
1
Isotope Atom Count:
0
Molecular Weight:
458.581g/mol
Monoisotopic Mass:
458.248g/mol
Rotatable Bond Count:
8
Topological Polar Surface Area:
42.3A^2
Undefined Atom Stereocenter Count:
0
Undefined Bond Stereocenter Count:
0
XLogP3:
6
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| 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 |
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| Automated tight seal electrophysiology for assessing the potential hERG liability of pharmaceutical compounds. | Assay and drug development technologies 20041001 |
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| Validation of a [3H]astemizole binding assay in HEK293 cells expressing HERG K+ channels. | Journal of pharmacological sciences 20040701 |
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| 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 |
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| 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 |
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| 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 |
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| Next generation antihistamines: therapeutic rationale, accomplishments and advances. | Expert opinion on investigational drugs 20020601 |
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| 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 |
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| 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 |
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| 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 |
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| Saquinavir soft gelatin capsule: a comparative safety review. | Drug safety 20010101 |
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| 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 |
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| 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 |
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| 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 |
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| 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 |
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