Delving into the Latest Updates on Antazoline Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

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

+ [2]

Target

H1 receptor

Mechanism

H1 receptor antagonists(Histamine H1 receptor antagonists)

Therapeutic Areas

Immune System DiseasesCardiovascular Diseases

Active Indication

Arrhythmias, CardiacHypersensitivity

Inactive Indication-

Originator Organization

Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.

Active Organization

Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure

Molecular FormulaC17H19N3

InChIKeyREYFJDPCWQRWAA-UHFFFAOYSA-N

CAS Registry91-75-8

View All Structures (2)

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.

28 Dec 2020·Combinatorial Chemistry & High Throughput ScreeningQ4 · MEDICINE

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

Q4 · MEDICINE

Article

Author: 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.

01 Nov 2018·Brain ResearchQ4 · MEDICINE

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

Q4 · MEDICINE

Article

Author: 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 Deals associated with Antazoline Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D07459	Antazoline Hydrochloride	R01AC04 R06AX05	DB08799

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Arrhythmias, Cardiac	CN	Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.	-
Hypersensitivity	CN	Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01527279 (AnPAF, Pubmed)	Phase 4	Atrial Fibrillation	74	Antazoline	aenocdlqmq(ldnopyvusf) = xabockamri plfktwxmvb (rlcyprqctx )	Positive	01 Oct 2017
				Placebo	aenocdlqmq(ldnopyvusf) = vdswvmcwdv plfktwxmvb (rlcyprqctx )
ESC2017	Not Applicable	Atrial fibrillation new onset	107	Antazoline	dqqiutjfkg(wwqotkysal) = gbflwumgfp mbpzglvshn (abwyslliss ) View more	-	28 Aug 2017
ESC2016	Not Applicable	-	10	Antazoline	jvyogqyxud(ysllqmmiye) = srudwwgqrd ugmhunzzop (erfgeyppfe ) View more	-	29 Aug 2016
				Sotalol	jvyogqyxud(ysllqmmiye) = nkslhtnxja ugmhunzzop (erfgeyppfe ) View more