盐酸安他唑啉(Antazoline Hydrochloride) - 药物靶点：H1 receptor_在研适应症：心律失常，超敏反应_专利_临床

概要

基本信息

药物类型

小分子化药

别名

2-(N-Benzylanilinomethyl)-2-imidazoline、2-(N-Phenyl-N-benzylaminomethyl)imidazoline、4,5-Dihydro-N-phenyl-N-phenylmethyl-1H-imidazole-2-methanamine

+ [2]

靶点

H1 receptor

作用机制

H1 receptor拮抗剂(组胺H1受体拮抗剂)

治疗领域

免疫系统疾病心血管疾病

在研适应症

心律失常超敏反应

非在研适应症-

原研机构

上海中西三维药业有限公司

在研机构

上海中西三维药业有限公司

非在研机构-

最高研发阶段批准上市

首次获批日期-

最高研发阶段(中国)批准上市

特殊审评-

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结构

分子式C17H19N3

InChIKeyREYFJDPCWQRWAA-UHFFFAOYSA-N

CAS号91-75-8

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关联

2

项与盐酸安他唑啉相关的临床试验

NCT05720572 / Recruiting临床4期IIT

Clinical Efficacy and Safety of Antazoline in Comparison to Propafenone in Conversion of Paroxysmal Atrial Fibrillation to Sinus Rhythm - a Single Center, Randomized, Double-blinded Study (the AnProAF Study).

The purpose of this randomized, double blind, non-inferiority clinical trial was to compare the clinical efficacy and safety of antazoline with propafenone in the rapid conversion of paroxysmal non-valvular atrial fibrillation to sinus rhythm in patients without heart failure

开始日期2019-09-01

申办/合作机构

International Center for Postgraduate Medical Education LLC

NCT01527279 / Completed临床4期IIT

Clinical Efficacy of Antazoline in Rapid Cardioversion of Paroxysmal Atrial Fibrillation - a Single Centre, Randomized, Double-blind, Placebo-controlled Study (the AnPAF Study)

The purpose of this randomized, double blind, placebo-controlled, superiority clinical trial was to assess clinical efficacy of antazoline in rapid conversion of atrial fibrillation during observation sinus rhythm.

开始日期2012-11-01

申办/合作机构-

100 项与盐酸安他唑啉相关的临床结果

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100 项与盐酸安他唑啉相关的转化医学

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100 项与盐酸安他唑啉相关的专利（医药）

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54

项与盐酸安他唑啉相关的文献（医药）

2021-06-01·Virologica Sinica2区 · 医学

Repurposing of Antazoline Hydrochloride as an Inhibitor of Hepatitis B Virus DNA Secretion

2区 · 医学

Article

作者: Liu, Canyu ; Zhao, Yinan ; Guo, Yu ; Pei, Rongjuan ; Chen, Xinwen ; Wang, Yun ; Li, Jing ; Han, Qiqi ; Wu, Chunchen ; Hu, Xue ; Hu, Yangyang ; Zhou, Yuan ; Yuan, Yifei

Hepatitis B virus (HBV) belongs to Hepadnaviridae family and mainly infects hepatocytes, which can cause acute or chronic hepatitis. Currently, two types of antiviral drugs are approved for chronic infection clinically: interferons and nucleos(t)ide analogues. However, the clinical cure for chronic infection is still rare, and it is a huge challenge for all researchers to develop high-efficiency, safe, non-tolerant, and low-toxicity anti-HBV drugs. Antazoline hydrochloride is a first-generation antihistamine with anticholinergic properties, and it is commonly used to relieve nasal congestion and in eye drops. Recently, an in vitro high-throughput evaluation system was constructed to screen nearly 800 compounds from the Food and Drug Administration (FDA)-approved Drug Library. We found that arbidol hydrochloride and antazoline hydrochloride can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC₅₀ of 4.321 μmol/L and 2.910 μmol/L in HepAD38 cells, respectively. Moreover, the antiviral effects and potential mechanism of action of antazoline hydrochloride were studied in different HBV replication systems. The results indicate that antazoline hydrochloride also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells, with an EC₅₀ of 2.349 μmol/L. These findings provide new ideas for screening and research related to HBV agents.

2020-12-28·Combinatorial Chemistry & High Throughput Screening4区 · 医学

The Development of Spectrophotometric and Validated Stability- Indicating RP-HPLC Methods for Simultaneous Determination of Ephedrine HCL, Naphazoline HCL, Antazoline HCL, and Chlorobutanol in Pharmaceutical Pomade Form

4区 · 医学

Article

作者: Uslu, Bengi ; Erkmen, Cem ; Göğer, Nilgün G. ; Dindar, Çiğdem K.

Background:Allergic rhinitis, acute nasal congestion and sinusitis are one of the most common health problems and have a major effect on the quality of life. Several medications are used to improve the symptoms of such diseases in humans. Pharmaceutical pomade form containing Ephedrine (EPD) HCl, Naphazoline (NPZ) HCl, Antazoline (ANT) HCl, and Chlorobutanol (CLO) is one of them.Objective:For these reasons, this study includes the development of spectrophotometric and chromatographic methods for the determination of EPD HCl, NPZ HCl, ANT HCl, and CLO active agents in the pharmaceutical pomade.Method:In the spectrophotometric method, third-order derivative of the amplitudes at 218 nm n=5 and the first-order derivative of the amplitudes 254 nm n=13 was selected for the determination of EPD, ANT, respectively while NPZ was determined by the second derivative at 234 nm and n=21. Colorimetric detection was applied for assay analysis of CLO at 540 nm. Furthermore, a reverse phase high performance liquid chromatographic (RP- HPLC) method has been developed and optimized by using Agilent Zorbax Eclipse XDB C18 (75 mm x 3.0 mm, 3.5μm) column. The column temperature was 40°C, binary gradient elution was used and the mobile phase consisted of 15 mM phosphate buffer in distilled water (pH 3.0) and methanol, and the flow rate was 0.6 mL min-1 and the UV detector was detected at 210 nm. The linear operating range was obtained as 11.97-70, 0.59-3, 2.79-30, and 2.92-200 μg mL-1 for EPD HCl, NPZ HCl, ANT HCl, and CLO respectively.Results:The LOD values were found to be 3.95, 0.19, 0.92 and 0.96 μg mL-1 for EPD HCl, NPZ HCl, ANT HCl, and CLO in the spectrophotometric method, respectively. The linear ranges in the RP-HPLC method were 8.2-24.36 μg mL-1, 0.083 - 0.75 μg/mL, 2.01-7.5 μg mL-1 and 2.89-24.4 μg mL-1 for EPD HCl, NPZ HCl, ANT HCl, and CLO, respectively. The LOD values in the validation studies were 2.7, 0.025, 0.66 and 0.86 μg mL-1 for EPD HCl, NPZ HCl, ANT HCl, and CLO in RP-HPLC method respectively.Conclusion:The results of the spectrophotometric and chromatographic methods were compared and no differences were found between the two methods.

2018-11-01·Brain Research4区 · 医学

Protective effects of 2-(2-benzonfuranyl)-2-imidazoline combined with tissue plasminogen activator after embolic stroke in rats

4区 · 医学

Article

作者: Chen, Jiaou ; Li, Li ; Zhang, Zheng ; Zhang, Linlei ; Cao, Yungang ; Han, Zhao ; Guo, Xiaoling

Stroke is the third leading cause of death and disability in developing countries. The effective therapy for acute ischemic stroke is thrombolysis with recombinant tissue plasminogen activator (rt-PA) within 4.5 h of stroke onset. An effective post-ischemic neuroprotectant would extend the advantages of rt-PA, and protect against complications of thrombolysis. We previously reported that 2-(2-benzofuranyl)-2-imidazoline (2-BFI), a newly discovered ligand for high-affinity type 2 imidazoline receptor (I2R), provides neuroprotection against ischemic stroke in rats. Here we investigated the protective effects of 2-BFI in combination with delayed intravenous rt-PA after stroke induced by embolic middle cerebral artery occlusion (eMCAO) in rats. Infarct size was determined using 2,3,5-triphenyltrazolium chloride staining, while neurological deficit was assessed based on neurological score. Numbers of apoptotic cells in vivo were estimated using TUNEL stain, and expression of the pro-apoptotic protein BAX and anti-apoptotic protein BCL-2 were quantified by Western blotting. The results showed that 2-BFI (3 mg/kg) administered at 0.5 h after embolic MCAO combined with rt-PA (10 mg/kg) administered at 6 h reduced brain infarct size, mitigated neurological deficit, decreased the number of TUNEL-positive cells, down-regulated BAX expression, and up-regulated BCL-2 expression. These findings suggest that 2-BFI may extend the therapeutic window of rt-PA to 6 h after embolic stroke onset in rats.

100 项与盐酸安他唑啉相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D07459	盐酸安他唑啉	R01AC04 R06AX05	DB08799

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
心律失常	中国	上海中西三维药业有限公司	-
超敏反应	中国	上海中西三维药业有限公司	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01527279 (AnPAF, Pubmed)	临床4期	心房颤动	74	Antazoline	網衊艱鏇憲憲醖積壓範(選簾艱襯獵鏇鏇遞鏇鑰) = 廠願鹽齋鏇築網餘糧窪築廠遞憲艱窪餘範鹹願 (製憲繭積膚廠積艱築範 )	积极	2017-10-01
				Placebo	網衊艱鏇憲憲醖積壓範(選簾艱襯獵鏇鏇遞鏇鑰) = 網艱鏇糧鑰選簾淵醖繭築廠遞憲艱窪餘範鹹願 (製憲繭積膚廠積艱築範 )
ESC2017	N/A	新发房颤	107	Antazoline	窪範鏇窪夢築鑰構鹽範(衊齋積築願鹹製構選鑰) = 鬱範鏇衊窪鏇窪齋顧觸糧廠簾鏇淵構餘衊鹹夢 (鏇衊壓製製鏇憲構壓網 ) 更多	-	2017-08-28
ESC2016	N/A	-	10	Antazoline	築醖廠衊築蓋築構鏇鬱(遞構鑰鏇襯選願鹹觸繭) = 廠艱築鹹鑰積顧餘鏇蓋網鹹鑰遞廠遞淵鏇鬱網 (製醖糧遞遞衊淵窪壓鬱 ) 更多	-	2016-08-29
				Sotalol	築醖廠衊築蓋築構鏇鬱(遞構鑰鏇襯選願鹹觸繭) = 構衊鬱遞觸鏇膚鏇襯構網鹹鑰遞廠遞淵鏇鬱網 (製醖糧遞遞衊淵窪壓鬱 ) 更多