布罗佐喷钠(Brozopentyl Sodium) - 药物靶点：Potassium channel_在研适应症：急性缺血性卒中_专利_临床

概要

基本信息

药物类型

小分子化药

别名

BZP

靶点

Potassium channel

作用机制

钾离子通道调节剂

治疗领域

神经系统疾病心血管疾病

在研适应症

急性缺血性卒中

非在研适应症-

原研机构

在研机构

非在研机构

最高研发阶段临床1期

首次获批日期-

最高研发阶段(中国)临床1期

特殊审评特殊审批 (中国)

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结构

分子式C12H15BrNaO3

InChIKeyIVULIEXOQKSHLG-UHFFFAOYSA-N

CAS号1631152-53-8

查看全部结构式(2)

关联

7

项与布罗佐喷钠相关的临床试验

CTR20242161 / Recruiting临床1期

随机、盲法、安慰剂对照、剂量递增、静脉滴注布罗佐喷钠在健康志愿者中的安全性、耐受性及药代动力学特性临床试验

评估健康志愿者静脉滴注布罗佐喷钠的耐受性、安全性及药代动力学特性。

开始日期2024-06-26

申办/合作机构

杭州澳亚生物技术股份有限公司

[+1]

CTR20192145 / Completed临床2期

多中心、随机、双盲、安慰剂平行对照评估不同剂量注射用布罗佐喷钠治疗急性缺血性卒中的临床试验

评价不同剂量注射用BZP对比安慰剂治疗急性缺血性卒中的安全性和可行性，并初步探讨其有效性，为Ⅲ期临床试验设计提供依据

开始日期2020-03-27

申办/合作机构

浙江奥翔药业股份有限公司

[+1]

CTR20171254 / Completed临床1期

随机、单盲、安慰剂对照、剂量递增、多次静脉滴注布罗佐喷钠的安全性、耐受性及药代动力学

评估健康志愿者多次静脉滴注布罗佐喷钠的耐受性、安全性及药代动力学特性

开始日期2017-10-11

申办/合作机构

浙江奥翔药业股份有限公司

[+1]

100 项与布罗佐喷钠相关的临床结果

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100 项与布罗佐喷钠相关的转化医学

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100 项与布罗佐喷钠相关的专利（医药）

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194

项与布罗佐喷钠相关的文献（医药）

2024-10-01·Journal of Chromatography A

Spherical cellulose/chitosan aerogel–supported MOF-199 for the magnetic solid-phase extraction of benzodiazepines from urine

Article

作者: Fu, Defeng ; Lü, Ting ; Zhang, Suling ; Liu, Hengli ; Zhao, Hongting ; Zhang, Dong

Metal-organic frameworks (MOFs) are promising materials for sample pretreatment. The performance improvement of powdered MOFs is hindered by their aggregation and difficult recovery. To overcome these issues, a biodegradable lightweight spherical aerogel was used as a support for the in situ growth of copper-based MOFs (MOF-199). Furthermore, Fe₃O₄ nanoparticles were incorporated into the aerogel to achieve magnetic properties. Thus, hybrid aerogel spheres containing MOF-199 supported on magnetic oxidized cellulose nanofiber/carboxymethyl chitosan (MOF-199@mag-CNF/CMC) were fabricated. The effects of Fe₃O₄ loading amount and organic-ligand concentration on the properties (spherical geometry and mechanical strength) of the hybrid aerogel spheres were studied. Their potential application in the extraction of benzodiazepines (BZPs) from urine samples prior to liquid chromatography-mass spectrometry was evaluated. The highly dispersed MOF-199 crystals on the spherical aerogel effectively overcame the inherent structural shrinkage of the bare aerogel spheres; thus, the MOF-199@mag-CNF/CMC aerogel spheres were robust and could withstand repeated use for at least eight consecutive extraction cycles. Further, MOF-199@mag-CNF/CMC exhibited improved BZP extraction efficiency, which was 2.5-11.6 times higher than that of bare Cu²⁺@mag-CNF/CMC aerogel spheres, primarily due to additional π-π interaction and H-bonding as well as improved specific surface area. Parameters influencing the extraction and desorption processes were also comprehensively investigated. Under optimal conditions, this method provided a wide linear range of 0.1-10 µg/L (R² > 0.995) and good precision (2.8-6.7% for intra-day; 1.9-7.8 % for inter-day). The limits of detection and quantification ranged from 0.02 to 0.11 µg/L and from 0.06 to 0.33 µg/L, respectively. The recoveries for the urine samples spiked with three concentrations of BZPs ranged from 73.9 % to 114.1 %. The proposed method is simple, sensitive and eco-friendly and can be used for the determination of BZPs from urine for clinical and forensic examinations.

2024-05-01·Science of The Total Environment

Estrogenic disruption effects and formation mechanisms of transformation products during photolysis of preservative parabens

Article

作者: Gao, Yanpeng ; Chen, Guanhui ; Niu, Xiaolin ; Ji, Yuemeng ; Chen, Yi ; An, Taicheng ; Wang, Mei ; Bi, Yashi

The ubiquitous presence of emerging contaminants (ECs) in the environment and their associated adverse effects has raised concerns about their potential risks. The increased toxicity observed during the environmental transformation of ECs is often linked to the formation of their transformation products (TPs). However, comprehension of their formation mechanisms and contribution to the increased toxicity remains an unresolved challenge. To address this gap, by combining quantum chemical and molecular simulations with photochemical experiments in water, this study investigated the formation of TPs and their molecular interactions related to estrogenic effect using the photochemical degradation of benzylparaben (BZP) preservative as a representative example. A non-targeted analysis was carried out and three previously unknown TPs were identified during the transformation of BZP. Noteworthy, two of these novel TPs, namely oligomers BZP-o-phenol and BZP-m-phenol, exhibited higher estrogenic activities compared to the parent BZP. Their IC₅₀ values of 0.26 and 0.50 μM, respectively, were found to be lower than that of the parent BZP (6.42 μM). The binding free energies (ΔG_bind) of BZP-o-phenol and BZP-m-phenol (-29.71 to -23.28 kcal·mol^-1) were lower than that of the parent BZP (-20.86 kcal·mol^-1), confirming their stronger binding affinities toward the estrogen receptor (ER) α-ligand binding domain. Subsequent analysis unveiled that these hydrophobic residues contributed most favorably to ER binding, with van der Waals interactions playing a significant role. In-depth examination of the formation mechanisms indicated that these toxic TPs primarily originated from the successive cleavage of ester bonds (OCH₂C₆H₅ and COO group), followed by their combination with BZP*. This study provides valuable insight into the mechanisms underlying the formation of toxic TPs and their binding interactions causing the endocrine-disrupting effects. It offers a crucial framework for elucidating the toxicological patterns of ECs with similar structures.

2024-03-25·Optics Express

Numerical optimization of auxiliary biaxial receiver to detect blind zone of pulsed coherent wind lidar

Article

作者: Zhao, Mingguang ; Wang, Huaijin ; Yu, Zhibin ; Li, Mengpei

The conventional pulsed monostatic coaxial coherent Doppler wind lidar (CDWL) has a blind detection zone of tens of meters, causing the loss of near-field wind field data. While maintaining the long-range detection capabilities of pulsed lidar, we introduce a novel auxiliary biaxial receiver (ABR) aimed at acquiring dependable coherent signals within blind zones. This is achieved by incorporating a receiver in close proximity to the monostatic coaxial transceiver (MCT), thereby mitigating end-face reflections and laser pulse tailing effects. A specific model of multiple aperture coherent wind detection is established for the ABR system without blind zone problem (BZP). The numerical simulations demonstrate that the biaxial receiver with reasonable design can meet the detection needs of the entire range of the blind zone. By using an ABR with a smaller focal length under appropriate transceiver pointing and general pointing accuracy, the BZP can be solved. The study also exhaustively obtained all parameter combinations that can solve the near-field BZP for a specific system. The results provide a new idea and engineering design guidance for the optical system design of pulsed CDWL without BZP.

100 项与布罗佐喷钠相关的药物交易

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