This webpage contains legacy information. The product is either no longer available from the supplier or has been delisted at Labome.
product summary
company name :
MilliporeSigma
other brands :
FLUKA, Sigma-Aldrich, Roche Applied Science
product type :
chemical
product name :
Astemizole
catalog :
A2861
citations: 47
Reference
Hayes H, Nicolini A, Arrowood C, Chvatal S, Wolfson D, Cho H, et al. Novel method for action potential measurements from intact cardiac monolayers with multiwell microelectrode array technology. Sci Rep. 2019;9:11893 pubmed publisher
Clements M, Millar V, Williams A, Kalinka S. Bridging Functional and Structural Cardiotoxicity Assays Using Human Embryonic Stem Cell-Derived Cardiomyocytes for a More Comprehensive Risk Assessment. Toxicol Sci. 2015;148:241-60 pubmed publisher
Lee E, Wu Z, Shon J, Liu K. Danazol Inhibits Cytochrome P450 2J2 Activity in a Substrate-independent Manner. Drug Metab Dispos. 2015;43:1250-3 pubmed publisher
Doherty K, TALBERT D, Trusk P, Moran D, Shell S, Bacus S. Structural and functional screening in human induced-pluripotent stem cell-derived cardiomyocytes accurately identifies cardiotoxicity of multiple drug types. Toxicol Appl Pharmacol. 2015;285:51-60 pubmed publisher
Kim H, Lee W, Lee K, Bae S, Kim M, Joo Y, et al. Efficacy of Helicobacter pylori eradication for the 1st line treatment of immune thrombocytopenia patients with moderate thrombocytopenia. Ann Hematol. 2015;94:739-46 pubmed publisher
Back H, Lee J, Yun H, Kwon K. Development of QTc prolongation model incorporating circadian rhythm using harmonic model. Xenobiotica. 2015;45:420-7 pubmed publisher
Yun J, Kim S. Antihistamines modulate the integrin signaling pathway in h9c2 rat cardiomyocytes: Possible association with cardiotoxicity. Hum Exp Toxicol. 2015;34:796-807 pubmed publisher
Anwar Mohamed A, Barakat K, Bhat R, Noskov S, Tyrrell D, Tuszynski J, et al. A human ether-á-go-go-related (hERG) ion channel atomistic model generated by long supercomputer molecular dynamics simulations and its use in predicting drug cardiotoxicity. Toxicol Lett. 2014;230:382-92 pubmed publisher
Eksterowicz J, Rock D, Rock B, Wienkers L, Foti R. Characterization of the active site properties of CYP4F12. Drug Metab Dispos. 2014;42:1698-707 pubmed publisher
Prado A, Petroianu G, Lorke D, Chambers J. A trivalent approach for determining in vitro toxicology: Examination of oxime K027. J Appl Toxicol. 2015;35:219-27 pubmed publisher
Lee B, Wu Z, Sung S, Lee T, Song K, Lee M, et al. Potential of decursin to inhibit the human cytochrome P450 2J2 isoform. Food Chem Toxicol. 2014;70:94-9 pubmed publisher
Girault A, Privé A, Trinh N, Bardou O, Ferraro P, Joubert P, et al. Identification of KvLQT1 K+ channels as new regulators of non-small cell lung cancer cell proliferation and migration. Int J Oncol. 2014;44:838-48 pubmed publisher
Karapetyan Y, Sferrazza G, Zhou M, Ottenberg G, Spicer T, Chase P, et al. Unique drug screening approach for prion diseases identifies tacrolimus and astemizole as antiprion agents. Proc Natl Acad Sci U S A. 2013;110:7044-9 pubmed publisher
Vlaar T, Cioc R, Mampuys P, Maes B, Orru R, Ruijter E. Sustainable synthesis of diverse privileged heterocycles by palladium-catalyzed aerobic oxidative isocyanide insertion. Angew Chem Int Ed Engl. 2012;51:13058-61 pubmed publisher
Fano S, Caliskan G, Heinemann U. Differential effects of blockade of ERG channels on gamma oscillations and excitability in rat hippocampal slices. Eur J Neurosci. 2012;36:3628-35 pubmed publisher
García Quiroz J, García Becerra R, Barrera D, Santos N, Avila E, Ordaz Rosado D, et al. Astemizole synergizes calcitriol antiproliferative activity by inhibiting CYP24A1 and upregulating VDR: a novel approach for breast cancer therapy. PLoS ONE. 2012;7:e45063 pubmed publisher
Garg V, Sachse F, Sanguinetti M. Tuning of EAG K(+) channel inactivation: molecular determinants of amplification by mutations and a small molecule. J Gen Physiol. 2012;140:307-24 pubmed publisher
Lee C, Jones J, Katayama J, Kaspera R, Jiang Y, Freiwald S, et al. Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. Drug Metab Dispos. 2012;40:943-51 pubmed publisher
Nomura F, Kaneko T, Hattori A, Yasuda K. 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. J Nanobiotechnology. 2011;9:39 pubmed publisher
García Quiroz J, Camacho J. Astemizole: an old anti-histamine as a new promising anti-cancer drug. Anticancer Agents Med Chem. 2011;11:307-14 pubmed
Nishimuta H, Sato K, Mizuki Y, Yabuki M, Komuro S. Species differences in intestinal metabolic activities of cytochrome P450 isoforms between cynomolgus monkeys and humans. Drug Metab Pharmacokinet. 2011;26:300-6 pubmed publisher
Borowiec A, Hague F, Gouilleux Gruart V, Lassoued K, Ouadid Ahidouch H. 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. Biochim Biophys Acta. 2011;1813:723-30 pubmed publisher
Li F, Hsieh Y, Kang L, Sondey C, Lachowicz J, Korfmacher W. MALDI-tandem mass spectrometry imaging of astemizole and its primary metabolite in rat brain sections. Bioanalysis. 2009;1:299-307 pubmed publisher
Ghosal A, Lu X, Penner N, Gao L, Ramanathan R, Chowdhury S, et al. 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 Metab Dispos. 2011;39:30-8 pubmed publisher
Shim W, Back H, Jung S, Kim J, Jang Y, Lee B, et al. An aqueous extract of Poncirus fructus activates the prokinetic activity of 5-HT receptor subtype 4 without hERG interaction. J Ethnopharmacol. 2010;132:328-33 pubmed publisher
Hsieh Y, Li F, Korfmacher W. Mapping pharmaceuticals in rat brain sections using MALDI imaging mass spectrometry. Methods Mol Biol. 2010;656:147-58 pubmed publisher
Tsutsui H, Higashijima S, Miyawaki A, Okamura Y. Visualizing voltage dynamics in zebrafish heart. J Physiol. 2010;588:2017-21 pubmed publisher
Lee E, Oh J, Park H, Kim D, Lee J, Kim C, et al. Simultaneous gene expression signature of heart and peripheral blood mononuclear cells in astemizole-treated rats. Arch Toxicol. 2010;84:609-18 pubmed publisher
Nilsson M, Danielsson C, Skold A, Johansson A, Blomgren B, Wilson J, et al. Improved methodology for identifying the teratogenic potential in early drug development of hERG channel blocking drugs. Reprod Toxicol. 2010;29:156-63 pubmed publisher
Margulis M, Sorota S, Chu I, Soares A, Priestley T, Nomeir A. Protein binding-dependent decreases in hERG channel blocker potency assessed by whole-cell voltage clamp in serum. J Cardiovasc Pharmacol. 2010;55:368-76 pubmed publisher
Rojo L, Alzate Morales J, Saavedra I, Davies P, Maccioni R. Selective interaction of lansoprazole and astemizole with tau polymers: potential new clinical use in diagnosis of Alzheimer's disease. J Alzheimers Dis. 2010;19:573-89 pubmed publisher
Phan H, Moeller M, Nahata M. Treatment of allergic rhinitis in infants and children: efficacy and safety of second-generation antihistamines and the leukotriene receptor antagonist montelukast. Drugs. 2009;69:2541-76 pubmed publisher
Sawayama A, Chen M, Kulanthaivel P, Kuo M, Hemmerle H, Arnold F. A panel of cytochrome P450 BM3 variants to produce drug metabolites and diversify lead compounds. Chemistry. 2009;15:11723-9 pubmed publisher
Vu K, Gelli A. Astemizole and an analogue promote fungicidal activity of fluconazole against Cryptococcus neoformans var. grubii and Cryptococcus gattii. Med Mycol. 2010;48:255-62 pubmed publisher
Wible B, Kuryshev Y, Smith S, Liu Z, Brown A. An ion channel library for drug discovery and safety screening on automated platforms. Assay Drug Dev Technol. 2008;6:765-80 pubmed publisher
Musonda C, Whitlock G, Witty M, Brun R, Kaiser M. Chloroquine-astemizole hybrids with potent in vitro and in vivo antiplasmodial activity. Bioorg Med Chem Lett. 2009;19:481-4 pubmed publisher
Rossignoli P, Rodrigues A, Tinti T, Pereira O, Ellinger F, Chies A. The possible involvement of hyperpolarizing mechanisms in histamine-induced relaxation of the rat portal vein. J Smooth Muscle Res. 2008;44:129-41 pubmed
Gutierrez Castrellon P, Ramirez Mayans J, López Pérez G. [Efficacy and safety of astemizole in the treatment of allergic rhinitis and urticaria: a systematic review with meta-analysis]. Rev Alerg Mex. 2005;52:113-26 pubmed
Heidemann S, Sarnaik A. Arrhythmias after astemizole overdose. Pediatr Emerg Care. 1996;12:102-4 pubmed
Burke T, Mutnick A. Ventricular fibrillation and anoxic encephalopathy secondary to astemizole overdose. Ann Pharmacother. 1993;27:239-41 pubmed
Janssens M. Astemizole. A nonsedating antihistamine with fast and sustained activity. Clin Rev Allergy. 1993;11:35-63 pubmed
Rao K, Adlakha A, Verma Ansil B, Meloy T, Stanton M. Torsades de pointes ventricular tachycardia associated with overdose of astemizole. Mayo Clin Proc. 1994;69:589-93 pubmed
Richards D, Brogden R, Heel R, Speight T, Avery G. Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1984;28:38-61 pubmed
Krstenansky P, Cluxton R. Astemizole: a long-acting, nonsedating antihistamine. Drug Intell Clin Pharm. 1987;21:947-53 pubmed
Levron J, Gillardin J, Sabbah A. [Astemizole: its pharmacokinetics and pharmacologic properties]. Allerg Immunol (Paris). 1990;22:233-41 pubmed
Janssens M, Caers L. Onset of action of astemizole. Int J Clin Pharmacol Res. 1991;11:219-29 pubmed
Hedrick C, Abate M. Astemizole effects on skin testing. Ann Pharmacother. 1992;26:1388-9 pubmed
product information
Catalog Number :
A2861
Product Name :
Astemizole
Product Type :
SMALL MOLECULES
Product Group :
Protein & Pathway Technologies
Product Description :
≥98% (HPLC)
company information
MilliporeSigma
PO Box 14508
St. Louis, MO 63178
https://www.sigmaaldrich.com
1-800-325-3010
headquarters: USA