所有图片(1)
别名:
1-（4-氟苄基）-2-（1-[4-甲氧基苯乙基] 哌啶-4-基）氨基苯并咪唑
经验公式（希尔记法）:
C28H31FN4O
CAS号:
分子量:
458.57
EC 号:
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
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质量水平
检测方案
≥98% (HPLC)
形式
powder
储存条件
desiccated
protect from light
溶解性
DMSO: >20 mg/mL
创始人
Johnson & Johnson
储存温度
2-8°C
SMILES字符串
COc1ccc(CCN2CCC(CC2)Nc3nc4ccccc4n3Cc5ccc(F)cc5)cc1
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
基因信息
human ... HRH1(3269)
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生化/生理作用
阿司咪唑是一种强效 hERG 钾通道阻断剂（IC 50 为 0.9 nM），可用作药理学分子伴侣，以纠正折叠缺陷并恢复一些 hERG 通道突变形式的蛋白功能。它还被研究用于治疗疟疾、癌症中的 hERG 和 hEAG 通道功能以及作为第二代抗组胺药 H-1 拮抗剂。
特点和优势
该化合物由 Johnson & Johnson 开发。如需浏览其他制药公司开发的化合物和批准的药物/候选药物列表，请点击此处。
警示用语：
Warning
危险声明
危险分类
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官
Respiratory system
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
K A Rao et al.
Mayo Clinic proceedings, 69(6), 589-593 (1994-06-01)
An overdose of astemizole predisposes the myocardium to ventricular dysrhythmias, including torsades de pointes. Herein we describe a case of astemizole-induced torsades de pointes ventricular tachycardia and also review previous case reports in the literature. All the patients were young
Fumimasa Nomura et al.
Journal of nanobiotechnology, 9, 39-39 (2011-09-21)
Conventional in vitro approach using human ether-a-go-go related gene (hERG) assay has been considered worldwide as the first screening assay for cardiac repolarization safety. However, it does not always oredict the potential QT prolongation risk or pro-arrhythmic risk correctly. For
Andrew M Sawayama et al.
Chemistry (Weinheim an der Bergstrasse, Germany), 15(43), 11723-11729 (2009-09-24)
Herein we demonstrate that a small panel of variants of cytochrome P450 BM3 from Bacillus megaterium covers the breadth of reactivity of human P450s by producing 12 of 13 mammalian metabolites for two marketed drugs, verapamil and astemizole, and one
Tjøstil Vlaar et al.
Angewandte Chemie (International ed. in English), 51(52), 13058-13061 (2012-11-20)
O(2) in, H(2)O out: Various diamines and related bisnucleophiles readily undergo oxidative isocyanide insertion with Pd(OAc)(2) (1 mol %) as the catalyst and O(2) as the terminal oxidant to give a diverse array of medicinally relevant N heterocycles. The utility
Chitalu C Musonda et al.
Bioorganic & medicinal chemistry letters, 19(2), 481-484 (2008-12-05)
A dual activity, conjugated approach has been taken to form hybrid molecules of two known antimalarial drugs, chloroquine (CQ) and the non-sedating H1 antagonist astemizole. A variety of linkers were investigated to conjugate the two agents into one molecule. Compounds
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