Astemizole (BioDeep_00000001891)
Secondary id: BioDeep_00001867674
human metabolite blood metabolite
代谢物信息卡片
化学式: C28H31FN4O (458.2482)
中文名称: 阿司咪唑
谱图信息:
最多检出来源 Homo sapiens(general) 20.11%
分子结构信息
SMILES: COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F
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)
描述信息
Astemizole is a long-acting, non-sedating second generation antihistamine used in the treatment of allergy symptoms. It was withdrawn from market by the manufacturer in 1999 due to the potential to cause arrhythmias at high doses, especially when when taken with CYP inhibitors or grapefruit juice.
R - Respiratory system > R06 - Antihistamines for systemic use > R06A - Antihistamines for systemic use
D018377 - Neurotransmitter Agents > D018494 - Histamine Agents > D006633 - Histamine Antagonists
C308 - Immunotherapeutic Agent > C29578 - Histamine-1 Receptor Antagonist
D018926 - Anti-Allergic Agents
Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects[1][2].
同义名列表
69 个代谢物同义名
1-[(4-fluorophenyl)methyl]-N-{1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl}-1H-1,3-benzodiazol-2-amine; 1-(p-Fluorobenzyl)-2-((1-(2-(p-methoxyphenyl)ethyl)piperid-4-yl)amino)benzimidazole; 1-(p-Fluorobenzyl)-2-((1-(p-methoxyphenethyl)-4-piperidyl)amino)benzimidazole; Reig jofre brand OF astemizole; Ratiopharm brand OF astemizole; Senosiain brand OF astemizole; Medinsa brand OF astemizole; Smaller brand OF astemizole; Janssen brand OF astemizole; Astemizole ratiopharm brand; Fustery brand OF astemizole; Astemizole senosiain brand; Alacan brand OF astemizole; Esteve brand OF astemizole; Urbion brand OF astemizole; Alonga brand OF astemizole; McNeil brand OF astemizole; Merck brand OF astemizole; Septa brand OF astemizole; Elfar brand OF astemizole; Lesvi brand OF astemizole; Astemizole janssen brand; Astemizole fustery brand; Vita brand OF astemizole; Astemizole smaller brand; Diba brand OF astemizole; Astemizole medinsa brand; Astemizole mcneil brand; Astemizole alacan brand; Byk brand OF astemizole; Astemizole urbion brand; ICN brand OF astemizole; Astemizole alonga brand; Astemizole esteve brand; Astemizole merck brand; Astemizole elfar brand; Astemizole septa brand; Astemizole lesvi brand; Ratiopharm, astemizol; Astemizole diba brand; Astemizole vita brand; Astemizol ratiopharm; Astemizole icn brand; Astemizole byk brand; Alonga, astemizol; Astemizol alonga; Fustermizol; Astemizolum; Paralergin; Hubermizol; astemizole; Histaminos; Alermizol; Astemison; Astemizol; Astemina; Hismanal; Laridal; Simprox; Esmacen; Romadin; Rifedot; Retolen; Astesen; Rimbol; Urdrim; Emdar; R 43512; Astemizole
数据库引用编号
19 个数据库交叉引用编号
- ChEBI: CHEBI:2896
- KEGG: C06832
- KEGGdrug: D00234
- PubChem: 2247
- HMDB: HMDB0014775
- Metlin: METLIN1122
- DrugBank: DB00637
- ChEMBL: CHEMBL296419
- Wikipedia: Astemizole
- MeSH: Astemizole
- chemspider: 2160
- CAS: 68844-77-9
- PMhub: MS000001397
- PubChem: 9050
- PDB-CCD: XB7
- NIKKAJI: J18.595G
- RefMet: Astemizole
- medchemexpress: HY-12532
- KNApSAcK: 2896
分类词条
相关代谢途径
Reactome(0)
BioCyc(0)
PlantCyc(0)
代谢反应
0 个相关的代谢反应过程信息。
Reactome(0)
BioCyc(0)
WikiPathways(0)
Plant Reactome(0)
INOH(0)
PlantCyc(0)
COVID-19 Disease Map(0)
PathBank(0)
PharmGKB(0)
1 个相关的物种来源信息
在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有:
- PubMed: 来源于PubMed文献库中的文献信息,我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表,这个列表按照代谢物同时出现的文献数量降序排序,取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
- NCBI Taxonomy: 通过文献数据挖掘,得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序,取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
- Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
- Chemical Reaction: 在化学反应过程中,存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。
点击图上的相关代谢物的名称,可以跳转到相关代谢物的信息页面。
文献列表
- Xiangjun Wang, Jiayu Lu, Shuai Ge, Yajing Hou, Tian Hu, Yuexin Lv, Cheng Wang, Huaizhen He. Astemizole as a drug to inhibit the effect of SARS-COV-2 in vitro.
Microbial pathogenesis.
2021 Jul; 156(?):104929. doi:
10.1016/j.micpath.2021.104929
. [PMID: 33932547] - Mark J Henderson, Kathleen A Trychta, Shyh-Ming Yang, Susanne Bäck, Adam Yasgar, Emily S Wires, Carina Danchik, Xiaokang Yan, Hideaki Yano, Lei Shi, Kuo-Jen Wu, Amy Q Wang, Dingyin Tao, Gergely Zahoránszky-Kőhalmi, Xin Hu, Xin Xu, David Maloney, Alexey V Zakharov, Ganesha Rai, Fumihiko Urano, Mikko Airavaara, Oksana Gavrilova, Ajit Jadhav, Yun Wang, Anton Simeonov, Brandon K Harvey. A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
Cell reports.
2021 04; 35(4):109040. doi:
10.1016/j.celrep.2021.109040
. [PMID: 33910017] - Derek J Leishman. Improving prediction of torsadogenic risk in the CiPA in silico model by appropriately accounting for clinical exposure.
Journal of pharmacological and toxicological methods.
2020 Jan; 101(?):106654. doi:
10.1016/j.vascn.2019.106654
. [PMID: 31730936] - Tobie D Lee, Olivia W Lee, Kyle R Brimacombe, Lu Chen, Rajarshi Guha, Sabrina Lusvarghi, Bethilehem G Tebase, Carleen Klumpp-Thomas, Robert W Robey, Suresh V Ambudkar, Min Shen, Michael M Gottesman, Matthew D Hall. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology.
2019 11; 96(5):629-640. doi:
10.1124/mol.119.115964
. [PMID: 31515284] - Kenta Watanabe, Tadashi Tsubouchi, Toru Yamada, Eiichi Hinoi, Izuru Miyawaki. Telemetered common marmosets is useful for the assessment of electrocardiogram parameters changes induced by multiple cardiac ion channel inhibitors.
The Journal of toxicological sciences.
2019; 44(7):441-457. doi:
10.2131/jts.44.441
. [PMID: 31270301] - Sandip B Bharate, Vikas Kumar, Shreyans K Jain, Mubashir J Mintoo, Santosh K Guru, Vijay K Nuthakki, Mohit Sharma, Sonali S Bharate, Sumit G Gandhi, Dilip M Mondhe, Shashi Bhushan, Ram A Vishwakarma. Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor.
Journal of medicinal chemistry.
2018 02; 61(4):1664-1687. doi:
10.1021/acs.jmedchem.7b01765
. [PMID: 29370702] - Meng Yan, Lifang Feng, Yanhui Shi, Junnan Wang, Yan Liu, Fengmei Li, Baoxin Li. 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.
2017 08; 158(2):379-390. doi:
10.1093/toxsci/kfx098
. [PMID: 28521025] - Jia-Nan Tian, Xiao-Dong Shi, Xiao-Kun Wang, Shuang Wang, Jing-Xue Xu, Chun-Xiao Yang. Astemizole protects against human umbilical vein endothelial cell injury induced by hydrogen peroxide via the p53 signaling pathway.
Molecular medicine reports.
2017 Jun; 15(6):4286-4290. doi:
10.3892/mmr.2017.6497
. [PMID: 28440512] - Youngsu You, Hee Sun Kim, Il Hak Bae, Seung Gi Lee, Min Hyeok Jee, Gyochang Keum, Sung Key Jang, B Moon Kim. New potent biaryl sulfate-based hepatitis C virus inhibitors.
European journal of medicinal chemistry.
2017 Jan; 125(?):87-100. doi:
10.1016/j.ejmech.2016.09.031
. [PMID: 27657807] - Shotaro Uehara, Yasuhiro Uno, Takashi Inoue, Eriko Okamoto, Erika Sasaki, Hiroshi Yamazaki. Marmoset cytochrome P450 2J2 mainly expressed in small intestines and livers effectively metabolizes human P450 2J2 probe substrates, astemizole and terfenadine.
Xenobiotica; the fate of foreign compounds in biological systems.
2016 Nov; 46(11):977-85. doi:
10.3109/00498254.2016.1146366
. [PMID: 26899760] - Hyun-moon Back, Jong-Hwa Lee, Jung-woo Chae, Byungjeong Song, Joung-Wook Seo, Hwi-yeol Yun, Kwang-il Kwon. A novel HPLC-MS/MS method for the simultaneous determination of astemizole and its major metabolite in dog or monkey plasma and application to pharmacokinetics.
Journal of pharmaceutical and biomedical analysis.
2015 Oct; 114(?):121-6. doi:
10.1016/j.jpba.2015.04.036
. [PMID: 26037160] - Il Hak Bae, Hee Sun Kim, Youngsu You, Chieyeon Chough, Weonu Choe, Min Kyung Seon, Seung Gi Lee, Gyochang Keum, Sung Key Jang, B Moon Kim. Novel benzidine and diaminofluorene prolinamide derivatives as potent hepatitis C virus NS5A inhibitors.
European journal of medicinal chemistry.
2015 Aug; 101(?):163-78. doi:
10.1016/j.ejmech.2015.06.033
. [PMID: 26134551] - Marta M Wells, Tommy S Tillman, David D Mowrey, Tianmo Sun, Yan Xu, Pei Tang. Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain.
Journal of medicinal chemistry.
2015 Apr; 58(7):2958-2966. doi:
10.1021/jm501873p
. [PMID: 25790278] - John Eksterowicz, Dan A Rock, Brooke M Rock, Larry C Wienkers, Robert S Foti. Characterization of the active site properties of CYP4F12.
Drug metabolism and disposition: the biological fate of chemicals.
2014 Oct; 42(10):1698-707. doi:
10.1124/dmd.114.059626
. [PMID: 25074871] - Candice M Klingerman, Michelle E Stipanovic, Mohammad Bader, Christopher J Lynch. Second-generation antipsychotics cause a rapid switch to fat oxidation that is required for survival in C57BL/6J mice.
Schizophrenia bulletin.
2014 Mar; 40(2):327-40. doi:
10.1093/schbul/sbs196
. [PMID: 23328157] - Liang Guo, Luke Coyle, Rory M C Abrams, Raymond Kemper, Eric T Chiao, Kyle L Kolaja. Refining the human iPSC-cardiomyocyte arrhythmic risk assessment model.
Toxicological sciences : an official journal of the Society of Toxicology.
2013 Dec; 136(2):581-94. doi:
10.1093/toxsci/kft205
. [PMID: 24052561] - Cho-Ming Loi, Dennis A Smith, Deepak Dalvie. Which metabolites circulate?.
Drug metabolism and disposition: the biological fate of chemicals.
2013 May; 41(5):933-51. doi:
10.1124/dmd.112.050278
. [PMID: 23454828] - Daniel J Warner, Hongming Chen, Louis-David Cantin, J Gerry Kenna, Simone Stahl, Clare L Walker, Tobias Noeske. Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
Drug metabolism and disposition: the biological fate of chemicals.
2012 Dec; 40(12):2332-41. doi:
10.1124/dmd.112.047068
. [PMID: 22961681] - Mehdi Hammadi, Valérie Chopin, Fabrice Matifat, Isabelle Dhennin-Duthille, Maud Chasseraud, Henri Sevestre, Halima Ouadid-Ahidouch. 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.
2012 Dec; 227(12):3837-46. doi:
10.1002/jcp.24095
. [PMID: 22495877] - Piotr Lutz. [Benzimidazole and its derivatives--from fungicides to designer drugs. A new occupational and environmental hazards].
Medycyna pracy.
2012; 63(4):505-13. doi:
. [PMID: 22994080]
- Olaf Scheel, Herbert Himmel, Gesa Rascher-Eggstein, Thomas Knott. 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.
2011 Dec; 9(6):600-7. doi:
10.1089/adt.2010.0352
. [PMID: 21675869] - Ye Chen, Araceli Sánchez, María E Rubio, Tobias Kohl, Luis A Pardo, Walter Stühmer. Functional K(v)10.1 channels localize to the inner nuclear membrane.
PloS one.
2011 May; 6(5):e19257. doi:
10.1371/journal.pone.0019257
. [PMID: 21559285] - Carmen Cifuentes-Diaz, Fabrice Chareyre, Marta Garcia, Jérôme Devaux, Michèle Carnaud, Grégoire Levasseur, Michiko Niwa-Kawakita, Sheila Harroch, Jean-Antoine Girault, Marco Giovannini, Laurence Goutebroze. Protein 4.1B contributes to the organization of peripheral myelinated axons.
PloS one.
2011; 6(9):e25043. doi:
10.1371/journal.pone.0025043
. [PMID: 21966409] - Asma Lat, George R Thompson. Update on the optimal use of voriconazole for invasive fungal infections.
Infection and drug resistance.
2011; 4(?):43-53. doi:
10.2147/idr.s12714
. [PMID: 21694908] - Offie P Soldin, Sarah H Chung, Donald R Mattison. Sex differences in drug disposition.
Journal of biomedicine & biotechnology.
2011; 2011(?):187103. doi:
10.1155/2011/187103
. [PMID: 21403873] - Falgun I Vyas, Shiv Prakash, A J Singh. 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.
2010 Dec; 42(6):366-9. doi:
10.4103/0253-7613.71919
. [PMID: 21189907] - Won-Sik Shim, Heejung Back, Sang-Won Jung, Jun-Woo Kim, Yongwoo Jang, Byeongjun Lee, Eun-Kyoung Seo, Uhtaek Oh, Chang-Koo Shim. An aqueous extract of Poncirus fructus activates the prokinetic activity of 5-HT receptor subtype 4 without hERG interaction.
Journal of ethnopharmacology.
2010 Oct; 132(1):328-33. doi:
10.1016/j.jep.2010.08.042
. [PMID: 20736054] - Michael Margulis, Steve Sorota, Inhou Chu, Anthony Soares, Tony Priestley, Amin A Nomeir. Protein binding-dependent decreases in hERG channel blocker potency assessed by whole-cell voltage clamp in serum.
Journal of cardiovascular pharmacology.
2010 Apr; 55(4):368-76. doi:
10.1097/fjc.0b013e3181d2ce39
. [PMID: 20125032] - Sayaka Kato, Yukio Kato, Tadakatsu Nakamura, Tomoko Sugiura, Yoshiyuki Kubo, Yoshiharu Deguchi, Akira Tsuji. Genetic deficiency of carnitine/organic cation transporter 2 (slc22a5) is associated with altered tissue distribution of its substrate pyrilamine in mice.
Biopharmaceutics & drug disposition.
2009 Dec; 30(9):495-507. doi:
10.1002/bdd.681
. [PMID: 19821448] - Hee-Kyung Hong, Weon-Jong Yoon, Young Ho Kim, Eun-Sook Yoo, Su-Hyun Jo. Inhibition of the human ether-a-go-go-related gene (HERG) K+ channels by Lindera erythrocarpa.
Journal of Korean medical science.
2009 Dec; 24(6):1089-98. doi:
10.3346/jkms.2009.24.6.1089
. [PMID: 19949665] - Franco Maggiolo. Efavirenz: a decade of clinical experience in the treatment of HIV.
The Journal of antimicrobial chemotherapy.
2009 Nov; 64(5):910-28. doi:
10.1093/jac/dkp334
. [PMID: 19767318] - Ji-Hyun Kim, Seong-Hae Park, Young Wha Moon, Sungmin Hwang, Donghoon Kim, Su-Hyun Jo, Seog Bae Oh, Joong Soo Kim, Jeong Won Jahng, Jong-Ho Lee, Sung Joong Lee, Se-Young Choi, Kyungpyo Park. Histamine H1 receptor induces cytosolic calcium increase and aquaporin translocation in human salivary gland cells.
The Journal of pharmacology and experimental therapeutics.
2009 Aug; 330(2):403-12. doi:
10.1124/jpet.109.153023
. [PMID: 19443731] - Sudha Yadav, A K Bajaj. Management of difficult urticaria.
Indian journal of dermatology.
2009 Jul; 54(3):275-9. doi:
10.4103/0019-5154.55641
. [PMID: 20161863] - Walid Beghdadi, Adeline Porcherie, Bradley S Schneider, Séverine Morisset, David Dubayle, Roger Peronet, Michel Dy, Jacques Louis, Jean-Michel Arrang, Salaheddine Mécheri. Histamine H(3) receptor-mediated signaling protects mice from cerebral malaria.
PloS one.
2009 Jun; 4(6):e6004. doi:
10.1371/journal.pone.0006004
. [PMID: 19547708] - B Seruga, H K Gan, J J Knox. Managing toxicities and optimal dosing of targeted drugs in advanced kidney cancer.
Current oncology (Toronto, Ont.).
2009 May; 16 Suppl 1(?):S52-9. doi:
10.3747/co.v16i0.402
. [PMID: 19478903] - Barbara A Wible, Yuri A Kuryshev, Stephen S Smith, Zhiqi Liu, Arthur M Brown. An ion channel library for drug discovery and safety screening on automated platforms.
Assay and drug development technologies.
2008 Dec; 6(6):765-80. doi:
10.1089/adt.2008.171
. [PMID: 19090691] - Mitsuyasu Tabo, Toshiko Hara, Sachiko Sone, Nobuyuki Shishido, Shino Kuramoto, Kounosuke Nakano, Hideko Onodera, Kazuya Kimura, Kazuko Kobayashi. Prediction of drug-induced QT interval prolongation in telemetered common marmosets.
The Journal of toxicological sciences.
2008 Aug; 33(3):315-25. doi:
10.2131/jts.33.315
. [PMID: 18670163] - Rebecca J Syed Sheriff, Katie Au, Caroline Cahill, Lorna Duggan, Yanling He, Victor Udu, Jun Xia. Pharmacological interventions for clozapine-induced hypersalivation.
Schizophrenia bulletin.
2008 Jul; 34(4):611-2. doi:
10.1093/schbul/sbn043
. [PMID: 18495644] - Matteo Masetti, Andrea Cavalli, Maurizio Recanatini. Modeling the hERG potassium channel in a phospholipid bilayer: Molecular dynamics and drug docking studies.
Journal of computational chemistry.
2008 Apr; 29(5):795-808. doi:
10.1002/jcc.20842
. [PMID: 17926340] - Ian N Olver. Prevention of chemotherapy-induced nausea and vomiting: focus on fosaprepitant.
Therapeutics and clinical risk management.
2008 Apr; 4(2):501-6. doi:
10.2147/tcrm.s2345
. [PMID: 18728837] - J S Silvestre, J R Prous. Comparative evaluation of hERG potassium channel blockade by antipsychotics.
Methods and findings in experimental and clinical pharmacology.
2007 Sep; 29(7):457-65. doi:
10.1358/mf.2007.29.7.1119172
. [PMID: 17982510] - Yasuhiro Masubuchi, Toshiharu Horie. Toxicological significance of mechanism-based inactivation of cytochrome p450 enzymes by drugs.
Critical reviews in toxicology.
2007 Jun; 37(5):389-412. doi:
10.1080/10408440701215233
. [PMID: 17612953] - R Lever, A Hefni, J D Moffatt, W Paul, C P Page. Effect of tecastemizole on pulmonary and cutaneous allergic inflammatory responses.
Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology.
2007 Jun; 37(6):909-17. doi:
10.1111/j.1365-2222.2007.02730.x
. [PMID: 17517105] - Denis Caillaud, Charles Le Merre, Yan Martinat, Bernard Aguilaniu, Demetri Pavia. A dose-ranging study of tiotropium delivered via Respimat Soft Mist Inhaler or HandiHaler in COPD patients.
International journal of chronic obstructive pulmonary disease.
2007; 2(4):559-65. doi:
NULL
. [PMID: 18268929] - Boni Elewski, Amir Tavakkol. Safety and tolerability of oral antifungal agents in the treatment of fungal nail disease: a proven reality.
Therapeutics and clinical risk management.
2005 Dec; 1(4):299-306. doi:
. [PMID: 18360572]
- Mariusz J Swiader, Jarogniew J Łuszczki, Marian Wielosz, Stanisław J Czuczwar. Effect of histamine receptor antagonists on aminophylline-induced seizures and lethality in mice.
Pharmacological reports : PR.
2005 Jul; 57(4):531-5. doi:
. [PMID: 16129921]
- G Peytavin, C Gautran, C Otoul, A C Cremieux, B Moulaert, F Delatour, M Melac, M Strolin-Benedetti, R Farinotti. Evaluation of pharmacokinetic interaction between cetirizine and ritonavir, an HIV-1 protease inhibitor, in healthy male volunteers.
European journal of clinical pharmacology.
2005 Jun; 61(4):267-73. doi:
10.1007/s00228-005-0917-6
. [PMID: 15889300] - Steve Sorota, Xue-Song Zhang, Michael Margulis, Kristal Tucker, Tony Priestley. Characterization of a hERG screen using the IonWorks HT: comparison to a hERG rubidium efflux screen.
Assay and drug development technologies.
2005 Feb; 3(1):47-57. doi:
10.1089/adt.2005.3.47
. [PMID: 15798395] - Shigeki Toyoshima, Akihiro Kanno, Tetsuya Kitayama, Koji Sekiya, Keiko Nakai, Masao Haruna, Terumasa Mino, Hiroyasu Miyazaki, Koji Yano, Keiji Yamamoto. 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.
2005; 99(5):459-71. doi:
10.1254/jphs.qt-a2
. [PMID: 16493187] - Kentaro Ando, Toshiyasu Hombo, Akihiro Kanno, Hironobu Ikeda, Masakazu Imaizumi, Noritsugu Shimizu, Kengo Sakamoto, Shin-ichi Kitani, Yoshinori Yamamoto, Shingo Hizume, Keiko Nakai, Tetsuya Kitayama, Keiji Yamamoto. 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.
2005; 99(5):487-500. doi:
10.1254/jphs.qt-a4
. [PMID: 16493189] - Rafael E García-Ferreiro, Daniel Kerschensteiner, Felix Major, Francisco Monje, Walter Stühmer, Luis A Pardo. Mechanism of block of hEag1 K+ channels by imipramine and astemizole.
The Journal of general physiology.
2004 Oct; 124(4):301-17. doi:
10.1085/jgp.200409041
. [PMID: 15365094] - Pekka Suomalainen, Christoffer Johans, Tim Söderlund, Paavo K J Kinnunen. Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability.
Journal of medicinal chemistry.
2004 Mar; 47(7):1783-8. doi:
10.1021/jm0309001
. [PMID: 15027870] - S G O'Brien, P Meinhardt, E Bond, J Beck, B Peng, C Dutreix, G Mehring, S Milosavljev, C Huber, R Capdeville, T Fischer. 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.
2003 Nov; 89(10):1855-9. doi:
10.1038/sj.bjc.6601152
. [PMID: 14612892] - Mariusz Swiader, Marian Wielosz, Stanisław J Czuczwar. Interaction of astemizole, an H1 receptor antagonist, with conventional antiepileptic drugs in mice.
Pharmacology, biochemistry, and behavior.
2003 Aug; 76(1):169-78. doi:
10.1016/s0091-3057(03)00212-0
. [PMID: 13679230] - Risto S Cvetkovic, Karen L Goa. Lopinavir/ritonavir: a review of its use in the management of HIV infection.
Drugs.
2003; 63(8):769-802. doi:
10.2165/00003495-200363080-00004
. [PMID: 12662125] - Eckhard Ficker, Carlos A Obejero-Paz, Shuxia Zhao, Arthur M Brown. 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.
2002 Feb; 277(7):4989-98. doi:
10.1074/jbc.m107345200
. [PMID: 11741928] - V Furlan, A M Taburet. [Drug interactions with antiretroviral agents].
Therapie.
2001 May; 56(3):267-71. doi:
NULL
. [PMID: 11475806] - S Gupta, C Banfield, B Kantesaria, M Marino, R Clement, M Affrime, V Batra. Pharmacokinetic and safety profile of desloratadine and fexofenadine when coadministered with azithromycin: a randomized, placebo-controlled, parallel-group study.
Clinical therapeutics.
2001 Mar; 23(3):451-66. doi:
10.1016/s0149-2918(01)80049-7
. [PMID: 11318079] - K Yamamoto, T Tamura, R Imai, M Yamamoto. 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.
2001 Mar; 60(1):165-76. doi:
10.1093/toxsci/60.1.165
. [PMID: 11222883] - J Gill, J Feinberg. Saquinavir soft gelatin capsule: a comparative safety review.
Drug safety.
2001; 24(3):223-32. doi:
10.2165/00002018-200124030-00005
. [PMID: 11347724] - M Swiader, K Chwalczuk, M Wielosz, S J Czuczwar. Influence of chronic treatment with H1 receptor antagonists on the anticonvulsant activity of antiepileptic drugs.
Polish journal of pharmacology.
2001 Jan; 53(1):93-6. doi:
NULL
. [PMID: 11785920] - M Taglialatela, A Pannaccione, P Castaldo, G Giorgio, L Annunziato. Inhibition of HERG1 K(+) channels by the novel second-generation antihistamine mizolastine.
British journal of pharmacology.
2000 Nov; 131(6):1081-8. doi:
10.1038/sj.bjp.0703654
. [PMID: 11082114] - J M Nicolas, R Whomsley, P Collart, J Roba. In vitro inhibition of human liver drug metabolizing enzymes by second generation antihistamines.
Chemico-biological interactions.
1999 Nov; 123(1):63-79. doi:
10.1016/s0009-2797(99)00131-3
. [PMID: 10597902] - Z Zhou, Q Gong, C T January. 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.
1999 Oct; 274(44):31123-6. doi:
10.1074/jbc.274.44.31123
. [PMID: 10531299] - T Ohmura, M Chachin, S Tarui, A Nagakura, T Igarashi, H Ikeda, K Ikegami, H Kitagawa, S Uchida. Effects of terfenadine, astemizole and epinastine on electrocardiogram in conscious cynomolgus monkeys.
European journal of pharmacology.
1999 Aug; 378(2):169-75. doi:
10.1016/s0014-2999(99)00457-4
. [PMID: 10478629] - Z Zhou, V R Vorperian, Q Gong, S Zhang, C T January. Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole.
Journal of cardiovascular electrophysiology.
1999 Jun; 10(6):836-43. doi:
10.1111/j.1540-8167.1999.tb00264.x
. [PMID: 10376921] - M Taglialatela, A Pannaccione, P Castaldo, G Giorgio, Z Zhou, C T January, A Genovese, G Marone, L Annunziato. 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.
1998 Jul; 54(1):113-21. doi:
10.1124/mol.54.1.113
. [PMID: 9658196] - A Pagliara, B Testa, P A Carrupt, P Jolliet, C Morin, D Morin, S Urien, J P Tillement, J P Rihoux. Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
Journal of medicinal chemistry.
1998 Mar; 41(6):853-63. doi:
10.1021/jm9704311
. [PMID: 9526560] - S Ikeda, H Oka, K Matunaga, S Kubo, S Asai, Y Miyahara, A Osaka, S Kohno. Astemizole-induced torsades de pointes in a patient with vasospastic angina.
Japanese circulation journal.
1998 Mar; 62(3):225-7. doi:
10.1253/jcj.62.225
. [PMID: 9583453] - A Sugiyama, N N Aye, S Katahira, A Hagihara, K Hashimoto. Effects of magnesium sulfate on the canine cardiovascular system complicating astemizole overdose.
Journal of cardiovascular pharmacology.
1997 Jun; 29(6):795-800. doi:
10.1097/00005344-199706000-00013
. [PMID: 9234661] - A Sugiyama, N N Aye, S Katahira, M Saitoh, A Hagihara, Y Matsubara, K Hashimoto. Effects of nonsedating antihistamine, astemizole, on the in situ canine heart assessed by cardiohemodynamic and monophasic action potential monitoring.
Toxicology and applied pharmacology.
1997 Mar; 143(1):89-95. doi:
10.1006/taap.1996.8061
. [PMID: 9073596] - R A Lefebvre, A Van Peer, R Woestenborghs. Influence of itraconazole on the pharmacokinetics and electrocardiographic effects of astemizole.
British journal of clinical pharmacology.
1997 Mar; 43(3):319-22. doi:
10.1046/j.1365-2125.1997.00548.x
. [PMID: 9088588] - K Bachmann, T J Sullivan, J H Reese, L Jauregui, K Miller, M Scott, J Stotka, J Harris. A study of the interaction between dirithromycin and astemizole in healthy adults.
American journal of therapeutics.
1997 Feb; 4(2-3):73-9. doi:
10.1097/00045391-199702000-00004
. [PMID: 10423595] - V R Vorperian, Z Zhou, S Mohammad, T J Hoon, C Studenik, C T January. Torsade de pointes with an antihistamine metabolite: potassium channel blockade with desmethylastemizole.
Journal of the American College of Cardiology.
1996 Nov; 28(6):1556-61. doi:
10.1016/s0735-1097(96)00352-x
. [PMID: 8917271] - C H Nightingale. Treating allergic rhinitis with second-generation antihistamines.
Pharmacotherapy.
1996 Sep; 16(5):905-14. doi:
NULL
. [PMID: 8888086] - D A Bukstein, R M Biondi, M M Blumenthal, R J Dockhorn, W V Filley, J Fink, S Goldstein, D F Graft, S R Hirsch, T H Joos, J Melamed, M S Rowe, R G Townley. Tilarin in combination with astemizole.
Allergy.
1996; 51(28 Suppl):20-7. doi:
10.1111/j.1398-9995.1996.tb04775.x
. [PMID: 8651473] - C I Berul, M Morad. Regulation of potassium channels by nonsedating antihistamines.
Circulation.
1995 Apr; 91(8):2220-5. doi:
10.1161/01.cir.91.8.2220
. [PMID: 7697852] - W W Storms. Treatment of seasonal allergic rhinitis with fluticasone propionate aqueous nasal spray: review of comparator studies.
Allergy.
1995; 50(23 Suppl):25-9. doi:
10.1111/j.1398-9995.1995.tb02738.x
. [PMID: 7604951] - S J Smith. Cardiovascular toxicity of antihistamines.
Otolaryngology--head and neck surgery : official journal of American Academy of Otolaryngology-Head and Neck Surgery.
1994 Sep; 111(3 Pt 2):348-54. doi:
10.1177/01945998941113p203
. [PMID: 7916150] - K Laine, K T Kivistö, P J Neuvonen. The effect of activated charcoal on the absorption and elimination of astemizole.
Human & experimental toxicology.
1994 Jul; 13(7):502-5. doi:
10.1177/096032719401300709
. [PMID: 7917508] - J J Melvin, R D Anbar, J M Becker. Does the histamine skin prick test identify patients at risk for toxicity after the ingestion of astemizole?.
Pediatric emergency care.
1994 Jun; 10(3):166-7. doi:
10.1097/00006565-199406000-00012
. [PMID: 8058561] - P Botstein. Is QT interval prolongation harmful? A regulatory perspective.
The American journal of cardiology.
1993 Aug; 72(6):50B-52B. doi:
10.1016/0002-9149(93)90041-a
. [PMID: 8256756] - P Saviuc, V Danel, F Dixmerias. Prolonged QT interval and torsade de pointes following astemizole overdose.
Journal of toxicology. Clinical toxicology.
1993; 31(1):121-5. doi:
10.3109/15563659309000380
. [PMID: 8433408] - T M Hollis, H W Sill, C Butler, M J Campos, T W Gardner. Astemizole reduces blood-retinal barrier leakage in experimental diabetes.
Journal of diabetes and its complications.
1992 Oct; 6(4):230-5. doi:
10.1016/1056-8727(92)90057-r
. [PMID: 1482780] - O A al-Deeb, E M Abdel-Moety, S M Bayomi, N A Khattab. Spectrophotometric quantification of astemizole and its demethylated metabolite in urine after TLC separation.
European journal of drug metabolism and pharmacokinetics.
1992 Oct; 17(4):251-5. doi:
10.1007/bf03190156
. [PMID: 1301353] - C Möller, P Andlin-Sobocki, L O Blychert. Pharmacokinetics of astemizole in children.
Rhinology. Supplement.
1992 Sep; 13(?):21-5. doi:
NULL
. [PMID: 1419223] - A W Nichols. Exercise-induced anaphylaxis and urticaria.
Clinics in sports medicine.
1992 Apr; 11(2):303-12. doi:
10.1016/s0278-5919(20)30532-9
. [PMID: 1591787] - S Mangalan, R B Patel, T P Gandhi, B K Chakravarthy. Detection and determination of free and plasma protein-bound astemizole by thin-layer chromatography: a useful technique for bioavailability studies.
Journal of chromatography.
1991 Jul; 567(2):498-503. doi:
10.1016/0378-4347(91)80158-9
. [PMID: 1939483] - N A Soter. Treatment of urticaria and angioedema: low-sedating H1-type antihistamines.
Journal of the American Academy of Dermatology.
1991 Jun; 24(6 Pt 2):1084-7. doi:
10.1016/0190-9622(91)70161-t
. [PMID: 1677011] - D Rosenthal, P E LeBoit, L Klumpp, T G Berger. Human immunodeficiency virus-associated eosinophilic folliculitis. A unique dermatosis associated with advanced human immunodeficiency virus infection.
Archives of dermatology.
1991 Feb; 127(2):206-9. doi:
. [PMID: 1671328]
- E Tani, E Rekka, P N Kourounakis. Modification of lipid peroxidation by some known substituted imidazole derivatives. An attempt to correlate their antioxidant activity with lipophilicity.
Die Pharmazie.
1991 Feb; 46(2):118-9. doi:
"
. [PMID: 1677199] - M M Janssens, L I Caers. Onset of action of astemizole.
International journal of clinical pharmacology research.
1991; 11(5):219-29. doi:
. [PMID: 1814843]
- H L Waldum, T Lehy, E Brenna, A K Sandvik, H Petersen, B S Søgnen, S Bonfils, M J Lewin. Effect of the histamine-1 antagonist astemizole alone or with omeprazole on rat gastric mucosa.
Scandinavian journal of gastroenterology.
1991 Jan; 26(1):23-35. doi:
10.3109/00365529108996480
. [PMID: 1706533] - J K Woodward. Pharmacology of antihistamines.
The Journal of allergy and clinical immunology.
1990 Oct; 86(4 Pt 2):606-12. doi:
10.1016/s0091-6749(05)80224-6
. [PMID: 1977782] - M J Ellison, R D Horner, F H Lawler, J G Jones. Lack of weight gain associated with short-term astemizole treatment.
DICP : the annals of pharmacotherapy.
1990 Jul; 24(7-8):682-4. doi:
10.1177/106002809002400703
. [PMID: 1973865] - J C Levron, J M Gillardin, A Sabbah. [Astemizole: its pharmacokinetics and pharmacologic properties].
Allergie et immunologie.
1990 Jun; 22(6):233-41. doi:
. [PMID: 1974137]
- A Malet i Casajuana, J Ruiz de León, A Valero Santiago, J Sanosa Valls, M Zamorano Calderón, P A García Calderón. "In vivo" and "in vitro" evaluation of four antihistamines (astemizole, azatadine, mequitazine, terfenadine).
Allergologia et immunopathologia.
1989 Mar; 17(2):85-93. doi:
. [PMID: 2476015]
- F E Simons, K J Simons, M Chung, J Yeh. The comparative pharmacokinetics of H1-receptor antagonists.
Annals of allergy.
1987 Dec; 59(6 Pt 2):20-4. doi:
. [PMID: 2892445]
- T M Craft, G Vanden Bussche, J De Cree, J V Griffiths. ECG studies with astemizole.
Human toxicology.
1987 Nov; 6(6):527-8. doi:
10.1177/096032718700600614
. [PMID: 2891609]