更新于：2024-11-04
Terazosin Hydrochloride
盐酸特拉唑嗪
更新于：2024-11-04
概要
基本信息
非在研机构 |
最高研发阶段批准上市 |
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C19H30ClN5O6 |
InChIKeyNZMOFYDMGFQZLS-UHFFFAOYSA-N |
CAS号70024-40-7 |
关联
57
项与 盐酸特拉唑嗪 相关的临床试验a Randomized, Double Blind, Placebo Controlled Clinical Trial Exploring the Target Engagement and Tolerability of Terazosin Hydrochloride in Patients With Dementia With Lewy Bodies
The efficacy on dysuria and safety of combination therapy with terazosin and bethanechol in Benign Prostatic Hyperplasia patients with Underactive Bladder
Effect of oral terazosin hydrochloride tablets or exercise intervention on the degree of arteriosclerosis in middle-aged and elderly people
100 项与 盐酸特拉唑嗪 相关的临床结果
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100 项与 盐酸特拉唑嗪 相关的转化医学
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100 项与 盐酸特拉唑嗪 相关的专利（医药）
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940
项与 盐酸特拉唑嗪 相关的文献（医药）2024-12-01CELLULAR AND MOLECULAR NEUROBIOLOGY
A Pharmacogenomics-Based In Silico Investigation of Opioid Prescribing in Post-operative Spine Pain Management and Personalized Therapy
Article
作者: Schmidt, Sergio Luis ; Lewandrowski, Kai-Uwe ; Sharafshah, Alireza ; Elfar, John ; Wetzel, Franklin Todd ; Blum, Kenneth
Abstract:
Considering the variability in individual responses to opioids and the growing concerns about opioid addiction, prescribing opioids for postoperative pain management after spine surgery presents significant challenges. Therefore, this study undertook a novel pharmacogenomics-based in silico investigation of FDA-approved opioid medications. The DrugBank database was employed to identify all FDA-approved opioids. Subsequently, the PharmGKB database was utilized to filter through all variant annotations associated with the relevant genes. In addition, the dpSNP (https://www.ncbi.nlm.nih.gov/snp/), a publicly accessible repository, was used. Additional analyses were conducted using STRING-MODEL (version 12), Cytoscape (version 3.10.1), miRTargetLink.2, and NetworkAnalyst (version 3). The study identified 125 target genes of FDA-approved opioids, encompassing 7019 variant annotations. Of these, 3088 annotations were significant and pertained to 78 genes. During variant annotation assessments (VAA), 672 variants remained after filtration. Further in-depth filtration based on variant functions yielded 302 final filtered variants across 56 genes. The Monoamine GPCRs pathway emerged as the most significant signaling pathway. Protein–protein interaction (PPI) analysis revealed a fully connected network comprising 55 genes. Gene–miRNA Interaction (GMI) analysis of these 55 candidate genes identified miR-16-5p as a pivotal miRNA in this network. Protein–Drug Interaction (PDI) assessment showed that multiple drugs, including Ibuprofen, Nicotine, Tramadol, Haloperidol, Ketamine, l-Glutamic Acid, Caffeine, Citalopram, and Naloxone, had more than one interaction. Furthermore, Protein–Chemical Interaction (PCI) analysis highlighted that ABCB1, BCL2, CYP1A2, KCNH2, PTGS2, and DRD2 were key targets of the proposed chemicals. Notably, 10 chemicals, including carbamylhydrazine, tetrahydropalmatine, Terazosin, beta-methylcholine, rubimaillin, and quinelorane, demonstrated dual interactions with the aforementioned target genes. This comprehensive review offers multiple strong, evidence-based in silico findings regarding opioid prescribing in spine pain management, introducing 55 potential genes. The insights from this report can be applied in exome analysis as a pharmacogenomics (PGx) panel for pain susceptibility, facilitating individualized opioid prescribing through genotyping of related variants. The article also points out that African Americans represent an important group that displays a high catabolism of opioids and suggest the need for a personalized therapeutic approach based on genetic information.
Graphical Abstract:
2024-10-01Chinese Journal of Chromatography
[Establishment and evaluation of haloalkane dehalogenase tagged α1A-adrenergic receptor chromatography].
Article
作者: Ji, Xu ; Zhang, Xiao-Ying ; Yuan, Xin-Yi ; Zhao, Xin-Feng ; Li, Liang-Xi ; Zhao, Qin ; Li, Qian
Receptor chromatography is an efficient analytical technique that combines the high separation ability of chromatography with the high specificity of receptors for drug recognition. In addition, this technique offers the advantages of active recognition, online separation, and convenient multidimensional target tracking. This strategy allows target active ingredients in complex systems, such as traditional Chinese medicines, to be efficiently screened and accurately identified. Furthermore, the interactions between ligands and immobilized proteins can be studied. To avoid a loss in function, receptor chromatography requires efficient, mild, and simple immobilization methods that do not damage the structure of the immobilized receptors. Improvements in the activity, stability, and ligand-recognition specificity of immobilized functional proteins can be achieved by selecting appropriate immobilization conditions. Notably, the protein immobilization method is not only closely related to the recognition ability of receptor chromatography but also determines the accuracy of the technique. Common methods for immobilizing functional proteins include physical adsorption, chemical reactions, biological affinity reactions, and click chemistry. Despite being easy to operate under mild reaction conditions, these methods have shortcomings, including poor reaction specificity and the necessity of using high-purity functional proteins to prepare chromatography columns. Maintaining the high activity of immobilized receptors and ensuring excellent identification and separation abilities are key challenges in the further development of receptor chromatography. In this work, these issues were addressed by introducing a specific bioorthogonal reaction involving haloalkane dehalogenase (Halo) and 6-chlorohexanoic acid for the immobilization of the α1A-adrenergic receptor (α1A-AR). Specifically, Halo-α1A-AR was immobilized on the surface of 6-chlorohexanoic acid-modified aminopropyl silica gel in one step. The stationary phase with immobilized Halo-α1A-AR was characterized using scanning electron microscopy. Moreover, the activity of the Halo-α1A-AR chromatographic column was evaluated using specific ligands (terazosin hydrochloride, phentolamine mesylate, tamsulosin hydrochloride, and urapidil) and nonspecific ligands (yohimbe and metoprolol) for α1A-AR. Halo-α1A-AR was successfully immobilized on the silica gel surface with good stability over 30 days, and the Halo-α1A-AR chromatographic column exhibited good ligand-recognition activity. The nonlinear chromatography results indicated that prazosin hydrochloride, terazosin hydrochloride, and urapidil interacted with immobilized Halo-α1A-AR through one type of binding site, with association constants of 3.85×105, 5.00×105, and 5.90×105L/mol, respectively. In contrast, phentolamine mesylate and tamsulosin hydrochloride interacted with immobilized Halo-α1A-AR through two types of binding site. The association constants with the high- and low-affinity binding sites were 3.12×106 and 6.01×105L/mol, respectively, for phentolamine mesylate and 9.98×105 and 0.21×105L/mol, respectively, for tamsulosin hydrochloride. Compared with the traditional carbonyldiimidazole method, the immobilization method developed in this work did not require receptor purification and thus minimized the loss of receptor activity. The affinity constants obtained with immobilized Halo-α1A-AR were consistent with the values determined for receptor-ligand binding in solution, indicating that the Halo-α1A-AR chromatography column is suitable for studying drug-protein interactions. This approach also provides a foundation for the efficient screening and accurate determination of target active ingredients in complex systems.
2024-10-01Revue neurologique
Importance of glucose and its metabolism in neurodegenerative disorder, as well as the combination of multiple therapeutic strategies targeting α-synuclein and neuroprotection in the treatment of Parkinson's disease
Review
作者: Kale, P P ; Siddique, A H H
According to recent findings, Phosphoglycerate Kinase 1 (pgk-1) enzyme is linked to Parkinson's disease (PD). Mutations in the PGK-1 gene lead to decreases in the pgk-1 enzyme which causes an imbalance in the levels of energy demand and supply. An increase in glycolytic adenosine triphosphate (ATP) production would help alleviate energy deficiency and sustain the acute energetic need of neurons. Neurodegeneration is caused by an imbalance or reduction in ATP levels. Recent data suggest that medications that increase glycolysis and neuroprotection can be used to treat PD. The current study focuses on treatment options for disorders associated with the pgk-1 enzyme, GLP-1, and A2A receptor which can be utilized to treat PD. A combination of metformin and terazosin, exenatide and meclizine, istradefylline and salbutamol treatments may benefit parkinsonism. The review also looked at potential target-specific new techniques that might assist in satisfying unfulfilled requirements in the treatment of PD.
100 项与 盐酸特拉唑嗪 相关的药物交易
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研发状态
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 原发性高血压 | 日本 | 1989-03-31 | |
| 肾性高血压 | 日本 | 1989-03-31 | |
| 高血压 | 美国 | 1987-08-07 | |
| 前列腺增生症 | 美国 | 1987-08-07 |
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临床结果
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FDA_CDER 人工标引  | N/A | - | 製積製廠積鏇網製蓋餘(夢範憲構選繭獵範窪範) = 壓憲鑰簾構壓衊襯遞蓋 選獵蓋製醖遞艱廠願鏇 (艱選繭顧鏇餘選構鹹築 ) 更多 | 积极 | 2024-07-29 | ||
Placebo | 製積製廠積鏇網製蓋餘(夢範憲構選繭獵範窪範) = 獵襯積範構製顧築築積 選獵蓋製醖遞艱廠願鏇 (艱選繭顧鏇餘選構鹹築 ) 更多 | ||||||
FDA_CDER 人工标引 | N/A | - | Placebo (Study 1) | 醖衊觸願製觸願醖餘衊(膚鬱製積範餘糧蓋遞齋) = 餘遞鑰壓繭壓膚鑰選壓 餘壓繭醖齋壓窪鑰製鏇 (夢簾簾夢夢齋願餘簾觸 ) 更多 | 积极 | 2024-07-29 | |
(Study 1) | 醖衊觸願製觸願醖餘衊(膚鬱製積範餘糧蓋遞齋) = 遞繭遞製顧獵廠網衊鏇 餘壓繭醖齋壓窪鑰製鏇 (夢簾簾夢夢齋願餘簾觸 ) 更多 | ||||||
临床2/3期 | 104 | Placebo (Placebo) | 鬱鏇憲願壓遞衊窪壓蓋(網壓願鑰願醖鬱繭鹽淵) = 壓繭鏇醖衊網膚築觸獵 願衊鹹遞選鏇壓製襯簾 (遞顧顧鏇夢鬱蓋膚淵餘, 鹹鏇壓淵鬱憲遞齋醖繭 ~ 襯網淵壓醖憲鏇構鑰淵) 更多 | - | 2015-03-02 | ||
(Terazosin) | 鬱鏇憲願壓遞衊窪壓蓋(網壓願鑰願醖鬱繭鹽淵) = 鬱衊夢網壓繭鹹壓觸蓋 願衊鹹遞選鏇壓製襯簾 (遞顧顧鏇夢鬱蓋膚淵餘, 窪廠遞鬱壓艱築鬱窪壓 ~ 淵憲觸鹽憲積顧鑰積糧) 更多 | ||||||
N/A | 733 | 夢鏇鑰獵選襯獵願淵糧(製製繭選鏇鑰衊鹽鏇蓋) = 製鏇壓齋獵淵選鏇製襯 網願膚繭壓淵範選鑰衊 (網襯願構築鏇蓋遞衊鹹 ) 更多 | - | 2008-05-01 | |||
鏇顧築觸繭衊獵繭積蓋(憲築膚選築鏇憲繭鑰壓) = 淵鹽觸夢遞網遞醖網繭 齋憲觸鏇艱淵構鏇鑰製 (觸遞觸憲艱獵鏇鹽鏇夢 ) |
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