Astemizole 阿司咪唑
CAS 68844-77-9 MFCD00153919
化学结构图
SMILES: COC1=CC=C(CCN2CCC(CC2)NC2=NC3=CC=CC=C3N2CC2C=CC(F)=CC=2)C=C1
化学属性
| Mol. Formula | C28H31FN4O |
|---|---|
| Mol. Weight | 458.57 |
别名和识别编码
| Chemical Name | Astemizole |
|---|---|
| CAS Number | 68844-77-9 |
| Synonym | 1-(4-Fluorobenzyl)-2-(1-[4-methoxyphenethyl]piperidin-4-yl)aminobenzimidazole 1-(p-Fluorobenzyl)-2-((1-(2-(p-methoxyphenyl)ethyl)piperid-4-yl)amino)benzimidazole 1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine Astemisan Astemizol Astemizole Hismanal Histamen Paralergin R 42512 R 43512 Retolen Waruzol |
| MDL Number | MFCD00153919 |
| EC Number | 272-441-9 |
| Chemical Name Translation | 阿司咪唑 |
| Wiswesser Line Notation | T56 BN DNJ B1R DF& CM- DT6NTJ A2R DO1 |
| Beilstein Registry Number | 4830190 |
| PubChem Substance ID | 329770802 |
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分类
- {SNA} AN-AZ, Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Ion Channels, Johnson & Johnson, Monovalent Ion Channels, Other Sodium Channel Modulators, Sodium Channel Modulators, Voltage-gated Ion Channels, 生物活性小分子, 细胞信号转导和神经科学, 细胞生物学
- Approved Therapeutics/Drug Candidates, Cell Biology, Cell Signaling and Neuroscience, Ion Channels, Johnson & Johnson, Monovalent Ion Channels, Other Sodium Channel Modulators, Sodium Channel Modulators, Voltage-gated Ion Channels
- {SNA} Approved Therapeutics/Drug Candidates, Cell Biology, Cell Signaling and Neuroscience, Ion Channels,
产品应用
- Nonsedating-type histamine H1-receptor antagonist. Potential for combination therapy with antivancer drugs such as doxorubicin in resistant leukemia. Antihistaminic.
相关文献及参考
- [2]. Richards DM, et al. Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1984 Jul;28(1):38-61.
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- Ficker, E., et al., The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations. J. Biol. Chem. 277 , 4989-4998, (2002)
- Merck 14 ,856
- Roy, J., et al., Pharmacological separation of hEAG and hERG K+ channel function in the human mammary carcinoma cell line MCF-7. Oncol. Rep. 19 , 1511-1526, (2008) 摘要
- Wang, L., et al., Intracellular potassium stabilizes hERG channels for export from endoplasmic reticulum. Mol. Pharmacol. , (2009)
- [1]. Laduron PM, et al. In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, as
- [1]. Laduron PM, et al. In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole. Mol Pharmacol. 1982 Mar;21(2):294-300.
安全信息
GHS Symbol
- P261 Avoid breathing dust/fume/gas/mist/vapours/spray. 避免吸入粉尘/烟/气体/烟雾/蒸汽/喷雾。
- P305+P351+P338
- H315 Causes skin irritation 会刺激皮肤
- H319 Causes serious eye irritation 严重刺激眼睛
- H335 May cause respiratory irritation 可能导致呼吸道刺激
- S26 In case of contact with eyes, rinse immediately with plenty of water and seek medical advice 眼睛接触后，立即用大量水冲洗并征求医生意见；
- S36 Wear suitable protective clothing 穿戴适当的防护服；
- R36/37/38 Irritating to eyes, respiratory system and skin 对眼睛、呼吸系统和皮肤有刺激性
- R22 Harmful if swallowed 吞咽有害
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE/DURATION : 4 mg/kg TOXIC EFFECTS : Cardiac - change in rate REFERENCE : JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 31,121,1993
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcu
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE/DURATION : 5400 ug/kg TOXIC EFFECTS : Behavioral - general anesthetic Cardiac - EKG changes not diagnostic of specified effects Cardiac - pulse rate increase, without fall in BP REFERENCE : PECAE5 Pediatric Emergency Care. (Williams & Wilkins, 428 E. Preston St., Baltimore, MD 21202) V.1- 1985- Volume(issue)/page/year: 9,23,1993
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 21800 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 33,381,1983
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - guinea pig DOSE/DURATION : 933 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE : 220 mg/kg SEX/DURATION : female 1-22 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - physical REFERENCE : CBPCEE Comparative Biochemistry and Physiology, C: Pharmacology, Toxicology and Endocrinology. (Elsevier Science, 660 White Plains Rd., Tarrytown, NY 10591) V.74- 1983- Volume(issue)/page/year: 114,123,1996
