更新于：2024-11-10
Flunarizine
氟桂利嗪
更新于：2024-11-10
概要
基本信息
药物类型 小分子化药 |
别名 1-[bis(4-fluorophenyl)methyl]-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine、Flunarizin Hydrochloride、Flunarizine Hydrochloride + [10] |
作用机制 CACNA1G阻滞剂(calcium voltage-gated channel subunit alpha1 G blockers)、CACNA1H阻滞剂(calcium voltage-gated channel subunit alpha1 H blockers)、CACNA1I阻滞剂(calcium voltage-gated channel subunit alpha1 I blockers) |
非在研适应症- |
在研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期- |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构
分子式C26H28Cl2F2N2 |
InChIKeyRXKMOPXNWTYEHI-RDRKJGRWSA-N |
CAS号30484-77-6 |
关联
40
项与 氟桂利嗪 相关的临床试验Comparison of the Effectiveness of First-line Preventive Treatment of Migraine in Primary Care: a Pragmatic Clinical Trial [PREMI Study]
Efficacy of Flunarizine Vs Amitriptyline in Prophylaxis of Migraine Prophylaxis
盐酸氟桂利嗪胶囊在中国健康受试者中进行的单中心、随机、开放、单次（餐后）口服给药、两制剂、两序列、两周期、交叉的人体生物等效性试验
100 项与 氟桂利嗪 相关的临床结果
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100 项与 氟桂利嗪 相关的转化医学
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100 项与 氟桂利嗪 相关的专利（医药）
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1,819
项与 氟桂利嗪 相关的文献（医药）2024-11-01ANALYTICAL BIOCHEMISTRY
Identification of potential inhibitors for drug resistance in acute lymphoblastic leukemia through differentially expressed gene analysis and in silico screening
Article
作者: Ayna Duran, Gizem ; Kiraz, Yağmur ; Tükel, Ezgi Yağmur ; Özay, Başak
Acute lymphoblastic leukemia (ALL) is a disease of lymphocyte origin predominantly diagnosed in children. While its 5-year survival rate is high, resistance to chemotherapy drugs is still an obstacle. Our aim is to determine differentially expressed genes (DEGs) related to Asparaginase, Daunorubicin, Prednisolone, and Vincristine resistance and identify potential inhibitors via docking. Three datasets were accessed from the Gene Expression Omnibus database; GSE635, GSE19143, and GSE22529. The microarray data was analyzed using R4.2.0 and Bioconductor packages, and pathway and protein-protein interaction analysis were performed. We identified 1294 upregulated DEGs, with 12 genes consistently upregulated in all four resistant groups. KEGG analysis revealed an association with the PI3K-Akt pathway. Among DEGs, 33 hub genes including MDM2 and USP7 were pinpointed. Within common genes, CLDN9 and HS3ST3A1 were subjected to molecular docking against 3556 molecules. Following ADMET analysis, three drugs emerged as potential inhibitors: Flunarizine, Talniflumate, and Eltrombopag. Molecular dynamics analysis for HS3ST3A1 indicated all candidates had the potential to overcome drug resistance, Eltrombopag displaying particularly promising results. This study promotes a further understanding of drug resistance in ALL, introducing novel genes for consideration in diagnostic screening. It also presents potential inhibitor candidates to tackle drug resistance through repurposing.
2024-10-01NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
Insights of potential trypanocidal effect of the synthetic derivative (2E)-1-(4-aminophenyl)-3-(2,4-dichlorophenyl)prop-2-en-1-one: in vitro assay, MEV analysis, quantum study, molecular docking, molecular dynamics, MPO analysis, and predictive ADMET
Article
作者: Dos Santos, Hélcio Silva ; Nunes, João Victor Serra ; de Lima Neto, Pedro ; Magalhães, Emanuel Paula ; Monteiro, Marília Lopes ; Martins, Alice Maria Costa ; Roberto, Caio Henrique Alexandre ; da Rocha, Matheus Nunes ; Marinho, Márcia Machado ; Marinho, Emmanuel Silva ; de Menezes, Ramon Róseo Paula Pessoa Bezerra ; de Queiroz Almeida-Neto, Francisco Wagner ; Ribeiro, Lyanna Rodrigues
This study aims to evaluate the antitrypanosomiasis activity of a synthetic dichloro-substituted aminochalcone via in vitro assays against infected cell cultures, as well as a theoretical characterization of pharmacokinetics and pharmacodynamics against the protein targets of the evolutionary cycle of T. cruzi. The in vitro evaluation of parasite proliferation inhibition was performed via cytotoxicity analysis on mammalian host cells, effect on epimastigote and trypomastigote forms, and cell death analysis, while computer simulations characterized the electronic structure of (2E)-1-(4-aminophenyl)-3-(2,4-dichlorophenyl)prop-2-en-1-one (DCl), the mechanism of action against the proteins of the evolutionary cycle of T. cruzi: Cruzain, Trypanothione reductase, TcGAPDH, and CYP51 by molecular docking and dynamics and predictive pharmacokinetics by MPO-based ADMET. The in vitro tests showed that the DCl LC50 in order of 178.9 ± 23.9 was similar to the BZN, evidencing the effectiveness of chalcone against Trypomastigotes. Molecular docking and dynamics simulations suggest that DCl acts on the active site of the CYP51 receptor, with hydrogen interactions that showed a high degree of occupation, establishing a stable complex with the target. MPO analysis and ADMET prediction tests suggest that the compound presents an alignment between permeability and hepatic clearance, although it presents low metabolic stability. Chalcone showed stable pharmacodynamics against the CYP51 target, but can form reactive metabolites from N-conjugation and C = C epoxidation, as an indication of controlled oral dose, although the estimated LD50 rate > 500 mg/kg is a indicative of low incidence of lethality by ingestion, constituting a promising therapeutic strategy.
2024-10-01JOURNAL OF NEUROLOGY
Natural history of non-polyglutamine CACNA1A disease in Austria
Article
作者: Kiechl, Stefan ; Kaltseis, Katharina ; Indelicato, Elisabetta ; Nachbauer, Wolfgang ; Unterberger, Iris ; Amprosi, Matthias S ; Maier, Sarah ; Boesch, Sylvia ; Broessner, Gregor ; Baumann, Matthias ; Delazer, Margarete
Abstract:
Background and objectives:
Non-polyglutamine CACNA1A variants underlie an extremely variable phenotypic spectrum encompassing developmental delay, hemiplegic migraine, epilepsy, psychiatric symptoms, episodic and chronic cerebellar signs. We provide our experience with the long-term follow-up of CACNA1A patients and their response to interval therapy.
Methods:
Patients with genetically confirmed non-polyglutamine CACNA1A disease were prospectively followed at the Center for Rare Movement Disorders of the Medical University of Innsbruck from 2004 to 2024.
Results:
We recruited 41 subjects with non-polyglutamine CACNA1A disease, of which 38 (93%) familial cases. The mean age at the first examination was 35 ± 22 years. Disease onset was in the childhood/adolescence in 31/41 patients (76%). Developmental delay and episodic symptoms were the first disease manifestation in 9/41 (22%) and 32/41 (78%) patients respectively. Chronic neurological signs encompassed a cerebellar syndrome in 35/41 (85%), which showed almost no progression during the observation period, as well as cognitive deficits in 9/20 (45%, MOCA test score < 26), psychiatric and behavioral symptoms in 11/41(27%). Seizures occurred in two patients concomitant to severe hemiplegic migraine. At the last visit, 27/41 patients (66%) required an interval prophylaxis (including acetazolamide, flunarizine, 4-aminopyridine, topiramate), which was efficacious in reducing the frequency and severity of episodic symptoms in all cases. In one patient in his 70ies with progressively therapy resistant hemiplegic migraine, treatment with the anti-CGRP antibody galcanezumab successfully reduced the frequency of migraine days from 4 to 1/month.
Conclusions:
Non-polyglutamine CACNA1A disease show an evolving age-dependent presentation. Interval prophylaxis is effective in reducing the burden of episodic symptoms.
100 项与 氟桂利嗪 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 偏头痛 | 中国 | - | |
| 眩晕 | 中国 | - |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 非小细胞肺癌 | 药物发现 | 中国 | 2023-04-04 |
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临床结果
临床结果
适应症
分期
评价
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N/A | 一线 | - | Flunarizine-treated group | 壓鹹廠壓憲鏇繭鑰繭鹹(製願憲鏇廠糧憲網蓋餘) = is a cut-off point for predicting future FIP 艱範製遞淵觸範窪鏇積 (網築積艱積鏇夢願憲夢 ) | - | 2020-04-14 | |
Control group (non-exposure to Flunarizine) | |||||||
N/A | 120 | Greater Occipital Nerve Block (Greater Occipital Nerve Block) | 選遞繭窪膚簾鬱憲遞鹹(壓膚積廠廠夢製顧鏇選) = 鹹鏇鏇壓選淵憲窪繭夢 遞簾餘餘鬱選鏇鏇鬱鏇 (蓋鬱夢齋憲餘鬱鬱糧淵, 鏇壓鏇構選製顧夢膚夢 ~ 範網鹹範夢鏇糧範顧夢) 更多 | - | 2020-01-21 | ||
(Topiramate) | 選遞繭窪膚簾鬱憲遞鹹(壓膚積廠廠夢製顧鏇選) = 蓋鹹夢衊糧窪糧選構繭 遞簾餘餘鬱選鏇鏇鬱鏇 (蓋鬱夢齋憲餘鬱鬱糧淵, 積觸壓築鹹選齋構淵鹽 ~ 觸衊壓襯製窪壓糧鑰積) 更多 | ||||||
临床4期 | 70 | 鏇憲簾選範襯製顧鬱憲(網壓願襯鏇願範築鹹築) = 蓋顧淵鏇蓋窪餘夢獵衊 遞積襯鏇願襯鬱憲衊積 (顧憲顧膚鏇獵夢鬱築憲 ) | - | 2008-10-01 | |||
Haloperidol | 鏇憲簾選範襯製顧鬱憲(網壓願襯鏇願範築鹹築) = 簾齋夢壓鬱鏇獵餘蓋遞 遞積襯鏇願襯鬱憲衊積 (顧憲顧膚鏇獵夢鬱築憲 ) |
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