醋酸胍那苄(Guanabenz Acetate) - 药物靶点：ADRA2_在研适应症：原发性高血压_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Guanabenz、Guanabenz acetate (JP17/USP)

+ [8]

靶点

ADRA2

作用方式

拮抗剂

作用机制

ADRA2拮抗剂(肾上腺素能受体α-2家族拮抗剂)

治疗领域

心血管疾病

在研适应症

原发性高血压

非在研适应症-

原研机构

Pfizer Inc.

在研机构

Alfresa Pharma Corp.

非在研机构

Wyeth-Ayerst Laboratories

最高研发阶段批准上市

首次获批日期

美国 (1982-09-07),

原发性高血压

最高研发阶段(中国)-

特殊审评孤儿药 (欧盟)

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结构/序列

分子式C8H8Cl2N4

InChIKeyWDZVGELJXXEGPV-UHFFFAOYSA-N

CAS号5051-62-7

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关联

5

项与醋酸胍那苄相关的临床试验

JPRN-jRCT2031210380

/ Completed临床2期IIT

Phase II physician-initiated clinical trial investigating the efficacy and safety of guanabenz acetate for non-alcoholic fatty liver disease associated with hypertension (G-Flash study)

开始日期2021-12-22

申办/合作机构-

EUCTR2017-001438-25-NL

/ Not yet recruiting临床2期IIT

A Study to Explore the Safety, Tolerability, Pharmacokinetic Profile, and Potential Efficacy of Guanabenz in Patients With Early Childhood Onset Vanishing White Matter (VWM)

开始日期2020-04-21

申办/合作机构-

EUCTR2014-005367-32-IT

/ Not yet recruiting临床2期IIT

PROTEIN MISFOLDING, AMYOTROPHIC LATERAL SCLEROSIS AND GUANABENZ: A PHASE II RCT WITH FUTILITY DESIGN - PROMISE

开始日期2016-02-29

申办/合作机构

Fondazione IRCCS Istituto Neurologico Carlo Besta

100 项与醋酸胍那苄相关的临床结果

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100 项与醋酸胍那苄相关的转化医学

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100 项与醋酸胍那苄相关的专利（医药）

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1,034

项与醋酸胍那苄相关的文献（医药）

2025-02-01·Chromatographia

Development and Validation of Confirmatory Quantitative and Screening Methods for 63 Prohibited Substances in Horse Urine Using LC–MS/MS

作者: Goktas, Eylem Funda ; Kabil, Erol

Abstract: The number of potentially abused substances in horse racing is very large and it is not easy to analyze the full range.To facilitate the analyses of substances of abuse, a method has been developed for 63 substances in horse urine using liquid chromatog.-tandem mass spectrometry.The developed method has been validated according to the 2021/808/EC and AORC criteria.The horse urine samples were extracted after enzymic hydrolysis via a C8-BCX SPE cartridge with an automated SPE and analyzed by LC-MS/MS.According to the validation study results, the within-laboratory reproducibility CV was no more than 13.9% and the average recoveries ranged from 90.71 to 117.94% for repeatability and reproducibility.The decision limits (CCα) for quant. anal. and detection capabilities (CCβ) for qual. screening were close to the targeted limit for each substance.The results of the present study showed that the method was able to perform quant. analyses of 54 substances and screening analyses of 9 substances (total 63) in horse urine and that the results were valid and applicable.The validated method was successfully applied to five proficiency tests and three suspected samples.

2024-06-01·Pharmacology Research & Perspectives

Not first‐line antihypertensive agents, but still effective—The efficacy and safety of imidazoline receptor agonists: A network meta‐analysis

Article

作者: Bahar, Muh Akbar ; Vágvölgyi, Anna ; Érszegi, András ; Viola, Réka ; Fejes, Imola ; Tóth, Barbara ; Csupor, Dezső

AbstractCardiovascular disorders are the leading cause of death in the world. Many organ diseases (kidney, heart, and brain) are substantially more prone to develop in people with hypertension. In the treatment of hypertension, first‐line medications are recommended, while imidazoline receptor agonists are not first‐line antihypertensives. Our goal was to conduct a network meta‐analysis to assess the efficacy and safety of imidazoline receptor agonists. The meta‐analysis was performed following the PRISMA guidelines using the PICOS format, considering the CONSORT recommendations. Studies were collected from four databases: PubMed, Cochrane Library, Web of Science, and Embase. A total of 5960 articles were found. After filtering, 27 studies remained eligible for network meta‐analysis. Moxonidine reduced blood pressure in sitting position statistically significantly after 8 weeks of treatment (SBP MD: 23.80; 95% CI: 17.45–30.15; DBP MD: 10.90; 95% CI: 8.45–13.35) compared to placebo. Moreover, moxonidine reduced blood pressure more effectively than enalapril; however, this difference was not significant (SBP MD: 3.10; 95% CI: −2.60–8.80; DBP MD: 1.30; 95% CI: −1.25–3.85). Dry mouth was experienced as a side effect in the case of all imidazoline receptor agonists. After 8 weeks of treatment, the appearance of dry mouth was highest with clonidine (OR: 9.27 95% CI: 4.70–18.29) and lowest with rilmenidine (OR: 6.46 95% CI: 0.85–49.13) compared to placebo. Somnolence was less frequent with moxonidine compared to rilmenidine (OR: 0.63 95% CI: 0.17–2.31). Imidazoline receptor agonists were nearly as effective as the first‐line drugs in the examined studies. However, their utility as antihypertensives is limited due to their side effects. As a result, they are not first‐line antihypertensives and should not be used in monotherapy. However, in the case of resistant hypertension, they are a viable option. According to our findings, from the point of view of safety and efficacy, moxonidine appears to be the best choice among imidazoline receptor agonists.

2023-12-29·Journal of Biomolecular Structure and Dynamics

Highlights in TMPRSS2 inhibition mechanism with guanidine derivatives approved drugs for COVID-19 treatment

Article

作者: Kabrine, Mohamed ; Ul-Haq, Zaheer ; Tachoua, Wafa ; Selmi, Ahmed ; Mushtaq, Mamona

Transmembrane protease serine 2 (TMPRSS2) has been identified as a critical key for the entry of coronaviruses into human cells by cleaving and activating the spike protein of SARS-CoV-2. To block the TMPRSS2 function, 18 approved drugs, containing the guanidine group were tested against TMPRSS2's ectodomain (7MEQ). Among these drugs, Famotidine, Argatroban, Guanadrel and Guanethidine strongly binds with TMPRSS2 S1 pocket with estimated Fullfitness energies of -1847.12, -1630.87, -1605.81 and -1600.52 kcal/mol, respectively. A significant number of non-covalent interactions such as hydrogen bonding, hydrophobic and electrostatic interactions were detected in protein-ligand complexes. In addition, the ADMET analysis revealed a perfect concurrence with the aptitude of these drugs to be developed as an anti-SARS-CoV-2 therapeutics. Further, MD simulation and binding free energy calculations were performed to evaluate the dynamic behavior and stability of protein-ligand complexes. The results obtained herein highlight the enhanced stability and good binding affinities of the Argatroban and Famotidine towards the target protein, hence might act as new scaffolds for TMPRSS2 inhibition.Communicated by Ramaswamy H. Sarma.

100 项与醋酸胍那苄相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00605	醋酸胍那苄	-	DB00629

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
原发性高血压	日本	Alfresa Pharma Corp.	1985-08-22

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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


NCT02443103 (CTgov)	N/A	骨癌 \| 骨转移癌	4	Guanabenz acetate	(齋襯遞繭構鏇積憲積積) = 簾獵齋膚築膚願選襯鹽窪衊繭憲鏇網醖鹽積齋 (衊醖觸鏇淵齋壓蓋鹹繭, 願廠簾餘築構醖遞齋選 ~ 艱鑰簾範選積築製醖膚) 更多	-	2018-02-13