更新于：2024-12-22
Flunarizine
氟桂利嗪
更新于：2024-12-22
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 + [15] |
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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1,834
项与 氟桂利嗪 相关的文献（医药）2024-12-01Autophagy
RAB37-mediated autophagy guards ovarian homeostasis and function
Article
作者: Hou, Yu ; Lan, Tian ; Lin, Lan ; Xu, Xu ; Ying, Ruhong ; Zhou, Rongjia ; Hu, Mengxin ; Zou, Juan ; Du, Zhuoyue ; Wang, Haoyu ; Cheng, Hanhua
Loss of ovarian homeostasis is associated with ovary dysfunction and female diseases; however, the underlying mechanisms responsible for the establishment of homeostasis and its function in the ovary have not been fully elucidated. Here, we showed that conditional knockout of Rab37 in oocytes impaired macroautophagy/autophagy proficiency in the ovary and interfered with follicular homeostasis and ovary development in mice. Flunarizine treatment upregulated autophagy, thus rescuing the impairment of follicular homeostasis and ovarian dysfunction in rab37 knockout mice by reprogramming of homeostasis. Notably, both the E2F1 and EGR2 transcription factors synergistically activated Rab37 transcription and promoted autophagy. Thus, RAB37-mediated autophagy ensures ovary function by maintaining ovarian homeostasis.Abbreviations: AMH: anti-Mullerian hormone; ATG: autophagy related; BECN1: beclin 1; cKO: conditional knockout; Cre: cyclization recombination enzyme; dpp: days postpartum; E2: estradiol; E2F1: E2F transcription factor 1; EBF1: EBF transcription factor 1; EGR2: early growth response 2; FSH: follicle stimulating hormone; LH: luteinizing hormone; mpp: months postpartum; MAP1LC3/LC3: microtubule associated protein 1 light chain 3; RAB37: RAB37, member RAS oncogene family; SQSTM1: sequestosome 1; TFEB: transcription factor EB; Zp3: zona pellucida glycoprotein 3.
2024-12-01Expert Review of Neurotherapeutics
An overview of the current and emerging treatment options for vestibular migraine
Review
作者: Calandre, Elena P. ; Slim, Mahmoud ; Rico-Villademoros, Fernando ; Bassila, Christine
INTRODUCTION:
Vestibular migraine is a relatively common syndrome characterized by the occurrence of vertigo and other vestibular symptoms, frequently -but not always- accompanied by migraine symptoms, such as headache, photophobia, and phonophobia.
AREAS COVERED:
The authors review the acute or abortive treatment during an attack and prophylactic treatment of vestibular migraines, including pharmacological and non-pharmacological options.
EXPERT OPINION:
Since its recognition as an independent clinical entity is recent, studies concerning its different treatment alternatives are still scarce, and the level of evidence of published studies is generally low. For acute treatment, although available data are conflicting, triptans are usually tried first. Neurostimulating devices can also be considered for acute treatment of vestibular migraine. Regarding the preventive treatment of vestibular migraine, based on the results of two randomized clinical trials and its pharmacological properties, flunarizine should be considered as the first treatment option. Second-line preventive treatments encompass propranolol, topiramate, venlafaxine, and valproic acid. Among non-pharmacological options, vestibular rehabilitation seems to be a sound prophylactic treatment option.
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.
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 | 襯壓醖淵簾齋憲蓋齋積(壓構築鏇壓鹽糧鹹構齋) = is a cut-off point for predicting future FIP 獵齋網獵醖齋憲襯願膚 (齋艱顧積製壓糧構餘遞 ) | - | 2020-04-14 | |
Control group (non-exposure to Flunarizine) | |||||||
N/A | 120 | Greater Occipital Nerve Block (Greater Occipital Nerve Block) | 艱衊鑰繭鏇積窪繭襯淵(網襯窪築簾簾構鹽鹽膚) = 壓網齋積鹽餘範夢憲獵 蓋範鹽糧選鑰衊積顧觸 (鹹窪網顧製繭襯遞糧範, 餘獵醖窪艱醖壓製鹹獵 ~ 築糧膚願廠餘鏇觸網製) 更多 | - | 2020-01-21 | ||
(Topiramate) | 艱衊鑰繭鏇積窪繭襯淵(網襯窪築簾簾構鹽鹽膚) = 選蓋觸範觸膚憲積觸蓋 蓋範鹽糧選鑰衊積顧觸 (鹹窪網顧製繭襯遞糧範, 淵獵壓築壓糧構艱鏇簾 ~ 淵蓋餘鹹醖廠蓋糧衊願) 更多 | ||||||
临床4期 | 70 | 壓網鹽餘齋築鹹窪鑰選(夢醖遞醖鏇觸顧窪鹽壓) = 鏇獵鹽衊壓觸願齋膚淵 夢獵窪夢獵願醖膚鏇憲 (鏇製膚艱襯壓範鹹鑰構 ) | - | 2008-10-01 | |||
Haloperidol | 壓網鹽餘齋築鹹窪鑰選(夢醖遞醖鏇觸顧窪鹽壓) = 鑰膚顧顧選壓夢製衊襯 夢獵窪夢獵願醖膚鏇憲 (鏇製膚艱襯壓範鹹鑰構 ) |
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