Azelastine hydrochloride 盐酸氮卓斯汀
CAS 79307-93-0 MFCD00242783
化学结构图
SMILES: [2H]C([2H])([2H])N1CCCC(CC1)N1N=C(CC2C=CC(Cl)=CC=2)C2=CC=CC=C2C1=O
化学属性
| Mol. Formula | C22H24ClN3O·HCl |
|---|---|
| Mol. Weight | 418 |
| Melting Point | 224.0 to 228.0 deg-C |
别名和识别编码
| Chemical Name | Azelastine hydrochloride |
|---|---|
| Synonym | 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1-one hydrochloride Astelin Azelastine HCl E-0659 Optivar |
| MDL Number | MFCD00242783 |
| Reaxys-RN | 4834474 |
| CAS Number | 79307-93-0 |
| Merck Number | 906 |
| Chemical Name Translation | 盐酸氮卓斯汀 |
| PubChem Substance ID | 329770938 |
| Wiswesser Line Notation | T66 BVNNJ E1R DG& C- DT7NTJ A1 &GH |
| Beilstein Registry Number | 4834474 |
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分类
- {SNA} AN-AZ, Antagonists, Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Histaminergics, Neuroscience, Neurotransmission, Neurotransmitters, Wallace, 生物活性小分子, 细胞信号转导和神经科学, 细胞生物学
- {SNA} AN-AZ, Antagonists, Approved Therapeutics/Drug Candidates, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Histaminergics, Neuroscience, Neurotransmission, Neurotransmitters, Wallace
相关文献及参考
- [2]. Mohamed M Elseweidy, et al. Azelastine a potent antihistamine agent, as hypolipidemic and modulator for aortic calcification in diabetic hyperlipidemic rats model. Arch Physiol Biochem. 2020 Jul 2;1-8.
- [3]. Carlos D. Zappia, et al. Azelastine potentiates antiasthmatic dexamethasone effect on a murine asthma model. Pharmacol Res Perspect. 2019 Dec; 7(6): e00531.
- [4]. Li Yang, et al. Identification of SARS-CoV-2 entry inhibitors among already approved drugs. Acta Pharmacol Sin. 2020 Oct 28 : 1–7.
- [5]. Shao-Cheng Liu, et al. Effect of budesonide and azelastine on histamine signaling regulation in human nasal epithelial cells. Eur Arch Otorhinolaryngol. 2017 Feb;274(2):845-853.
- [1]. Craig La Force. Review of the pharmacology, clinical efficacy, and safety of azelastine hydrochl
- [1]. Craig La Force. Review of the pharmacology, clinical efficacy, and safety of azelastine hydrochloridel. Expert Rev Clin Immunol. 2005 Jul;1(2):191-201.
安全信息
GHS Symbol
- H302 Harmful if swallowed 吞食有害
- R22 Harmful if swallowed 吞咽有害
- P264 Wash hands thoroughly after handling. 处理后要彻底洗净双手。
- P270 Do not eat, drink or smoke when using this product. 使用本产品时不要吃东西，喝水或吸烟。
- P273 Avoid release to the environment. 避免释放到环境中。
- P301+P312
- P301+P312+P330
- P391 Collect spillage. Hazardous to the aquatic environment 收集对水环境有危害的泄漏物。
- P501 Dispose of contents/container to..… 处理内容物/容器.....
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 24600 ug/kg TOXIC EFFECTS : Behavioral - altered sleep time (including c
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 80500 ug/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor Behavioral - convulsions or effect on seizure threshold REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5231,1986
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 580 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor Behavioral - convulsions or effect on seizure threshold REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5231,1986
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 59600 ug/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5231,1986
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 6729 mg/kg
SEX/DURATION : male 11 week(s) pre-mating
female 2 week(s) pre-mating - 7 day(s) after
conception
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in
number of implants per female; total number of implants per corpora lutea)
Reproductive - Fertility - other measures of fertility
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag,
Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951-
Volume(issue)/page/year: 31,1225,1981TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE : 330 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - musculoskeletal system REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,1225,1981
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE : 755 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fe
