预约演示
更新于：2025-04-16
Mizolastine
咪唑斯汀
更新于：2025-04-16
概要
基本信息
原研机构- |
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- |
登录后查看时间轴
结构/序列
分子式C24H25FN6O |
InChIKeyPVLJETXTTWAYEW-UHFFFAOYSA-N |
CAS号108612-45-9 |
关联
2
项与 咪唑斯汀 相关的临床试验CTR20201671
咪唑斯汀缓释片在空腹及餐后条件下的人体生物等效性试验
NCT01928316
Bioequivalence Study of Home-made and Imported Mizolastine Tablets in Healthy Volunteers
100 项与 咪唑斯汀 相关的临床结果
登录后查看更多信息
100 项与 咪唑斯汀 相关的转化医学
登录后查看更多信息
100 项与 咪唑斯汀 相关的专利（医药）
登录后查看更多信息
339
项与 咪唑斯汀 相关的文献（医药）2025-04-01TOXICOLOGY LETTERS
Discovery of non-steroidal aldo-keto reductase 1D1 inhibitors through automated screening and in vitro evaluation
Article
作者: Odermatt, Alex ; van Diest, Rianne E ; Kȩdzierski, Jacek ; Smieško, Martin ; Allard, Julien A
Steroid hormones regulate a wide range of physiological processes in the human body. However, exposure to xenobiotics can disrupt the hormonal balance by inhibition of enzymes involved in hormone synthesis or metabolism. Aldo-keto reductase 1D1 (AKR1D1) plays a key role in bile acid and steroid hormone metabolism by catalyzing the reduction of the double bond between C4 and C5 atoms of Δ(4)-steroids. In our previous work, we developed a model to screen for steroid-like xenobiotics that inhibit AKR1D1. In the current study, we used this model to screen for novel non-steroidal inhibitors. By applying an automatized screening approach, based on molecular docking and scoring in combination with post-docking refinement, 45 compounds were detected as potential hits and selected for in vitro evaluation. Among them, zardaverine was identified as the most potent inhibitor, with an IC50 value of 2.32 ± 1.27 μM. Other moderate inhibitors included carbamazepine, larotrectinib, endosulfan II, megastigmatrienone A, and mizolastine. The structural diversity of the identified inhibitors demonstrates that the binding site of AKR1D1 is rather promiscuous and can accommodate a broad range of ligands. These findings underscore the importance of toxicity screening and potential to identify structurally different AKR1D1 inhibitors.
2025-04-01JOURNAL OF PHARMACEUTICAL SCIENCES
Optimization of HPLC method for determination of Abraham solvation parameters of pharmaceuticals
Article
作者: Knašienė, Birutė ; Sazonovas, Andrius ; Sadaunykas, Audrius ; Naujalis, Evaldas ; Balčiūnas, Simonas ; Lanevskij, Kiril
Abraham solvation equation (Absolv) is a popular and well-established approach for modeling solute partitioning between phases of different polarity, which finds its applications in both organic chemistry and biomedical fields. Parameters constituting this equation are good quantitative descriptors of solute hydrogen bonding potential that are useful for QSAR modeling of more complex chemical and biological phenomena. Numerous studies dealing with fast determination of Abraham descriptors using HPLC can be found in the literature, but these mostly focus on small un-ionizable industrial and environmental chemicals, whereas experimental data for pharmaceutical molecules are clearly lacking. In the current study we build upon a previously published chromatographic approach, aiming to adapt the method to ionizable drug-like compounds, and optimize it by reducing the number of required HPLC columns. The analysis involves determination of the overall H-bond acidity (A), H-bond basicity (B) and polarity/polarizability (S) descriptors for 62 pharmaceutical molecules with previously unpublished parameter values.
2025-02-01Frontiers of Medicine
Preclinical and clinical studies on Qin-Zhu-Liang-Xue decoction: insights from network pharmacology and implications for atopic dermatitis treatment
Article
作者: Fei, Xiaoya ; Nian, Hua ; Zhang, Ruoxi ; Kuai, Le ; Huang, Keke ; Li, Su ; Luo, Yue ; Ma, Xin ; Liu, Qingkai ; Luo, Ying ; Tan, Yimei ; Li, Bin
To investigate the protective effects and underlying mechanisms of Qin-Zhu-Liang-Xue decoction (QZLX) in atopic dermatitis (AD) and glucocorticoid resistance, we conducted a single-blinded, randomized controlled clinical trial to evaluate the efficacy and safety of this concoction. Network pharmacology analysis was performed and validated through clinical studies. The efficacy, safety, and mechanism of action of QZLX and glucocorticoid receptor (GR) α recombinant protein were assessed in AD mice induced by 2,4-dinitrofluorobenzene (DNFB). Correlation analysis was performed to determine the clinical relevance of GRα. The trial demonstrated that patients who received QZLX showed considerable improvements in their Scoring Atopic Dermatitis (SCORAD) and Dermatology Life Quality Index (DLQI) scores compared with those who received mizolastine at week 4. Network pharmacological analysis identified GRα as a key target for QZLX in AD treatment. QZLX administration increased the serum GRα expression in AD patients, alleviated AD symptoms in mice, decreased inflammatory cytokine expression, and increased GRα expression without affecting liver or kidney function. In addition, GRα recombinant protein improved AD-like skin lesions in DNFB-induced mice. A negative correlation was observed between GRα expression and clinical parameters, including SCORAD, DLQI, and serum IgE levels. QZLX alleviates AD symptoms through the upregulation of GRα and thus presents a novel therapeutic strategy for the prevention of glucocorticoid resistance in AD management.
100 项与 咪唑斯汀 相关的药物交易
登录后查看更多信息
研发状态
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 变应性结膜炎 | 中国 | 2001-03-09 | |
| 过敏性鼻炎 | 欧盟 | - | 1997-04-02 |
| 过敏性鼻炎 | 冰岛 | - | 1997-04-02 |
| 过敏性鼻炎 | 列支敦士登 | - | 1997-04-02 |
| 过敏性鼻炎 | 挪威 | - | 1997-04-02 |
| 荨麻疹 | 欧盟 | - | 1997-04-02 |
| 荨麻疹 | 冰岛 | - | 1997-04-02 |
| 荨麻疹 | 列支敦士登 | - | 1997-04-02 |
| 荨麻疹 | 挪威 | - | 1997-04-02 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
Eureka LS:
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用