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更新于：2024-12-31
Flunarizine
氟桂利嗪
更新于：2024-12-31
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/序列
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NCT06499116
Comparison of the Effectiveness of First-line Preventive Treatment of Migraine in Primary Care: a Pragmatic Clinical Trial [PREMI Study]
NCT06162819
Efficacy of Flunarizine Vs Amitriptyline in Prophylaxis of Migraine Prophylaxis
CTR20233648
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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1,835
项与 氟桂利嗪 相关的文献（医药）2025-01-01PHYTOMEDICINE
Chuanxiong Qingnao Granules (CQG) alleviates nitroglycerin-induced migraine-like pain in rats by glycerophospholipid metabolism and PI3K/Akt signaling pathway
Article
作者: Ni, Li-Qi ; Hou, Jing-Yi ; Hou, Bo-Wen ; Wang, Li-Han ; Yang, Hong-Jun ; Zhu, Nai-Qiang ; Wang, Kun
BACKGROUND AND PURPOSE:
Chuanxiong Qingnao Granles (CQG), has been used to treat migraine headache (MH) for many years. However, current investigation of CQG have primarily focused on clinical studies, and the potential mechanisms underlying of its effects on MH have not been fully elucidated. In the present study, we applied an integrated approach of transcriptomics and metabolomics to elucidate the therapeutic mechanisms of CQG in nitroglycerin (NTG)-induced MH injury.
METHODS AND RESULTS:
Fifty rats were allocated into five random groups: control (Con), NTG, flunarizine (NTG + Flu) group, and two CQG groups (NTG + CQG-L and NTG + CQG-H). CQG notably reduced the duration of ear redness and the frequency of head scratching frequency in rats. It also lowered the levels of 5-hydroxytryptamine (5-HT), endothelin-1 (ET-1), calcitonin gene-related peptide type 1 receptor (CGPR1), and tumor necrosis factor alpha (TNF-α) and enhanced neuronal morphology following NTG-induced MH damage. Transcriptomic and metabolomic analyses pinpointed interleukin (IL)-17A, IL-13, and CC chemokine receptor type 3 (CCR3) as central CQG targets, glycerophospholipid metabolism as key metabolic pathway, and further experiments confirmed that CQG reduced the expression of IL-17A, IL-13, CCR3, and inhibited the expression of inflammatory cytokines by suppressing PI3K/Akt signaling pathway and glycerophospholipid metabolism, to attenuate neuroinflammation in MH rats.
CONCLUSIONS:
Taken together, CQG inhibited PI3K/Akt signaling pathway to reduced neuroinflammation, and modulated metabolic pathway of glycerophospholipid metabolism in MH. The findings of this study offer novel insights into the mechanisms underlying the therapeutic effects of CQG, highlighting its potential clinical application in treatment of MH.
2024-12-01Autophagy
RAB37-mediated autophagy guards ovarian homeostasis and function
Article
作者: Hou, Yu ; Lan, Tian ; Xu, Xu ; Lin, Lan ; 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.
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
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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 | 鏇齋遞鏇淵淵餘艱夢齋(繭範蓋遞齋憲構鹽蓋觸) = is a cut-off point for predicting future FIP 糧願淵顧襯蓋鬱膚憲夢 (繭糧構遞鬱壓淵淵網網 ) | - | 2020-04-14 | |
Control group (non-exposure to Flunarizine) | |||||||
N/A | 120 | Greater Occipital Nerve Block (Greater Occipital Nerve Block) | 窪窪選壓憲壓淵衊積淵(鹽齋襯積願鹹鑰遞簾廠) = 網簾餘蓋膚築網遞憲繭 醖廠顧觸構鑰築壓鑰廠 (觸觸觸構鏇簾蓋鑰餘糧, 鹽網襯網鏇膚壓範鑰衊 ~ 襯積簾壓繭選網廠製網) 更多 | - | 2020-01-21 | ||
(Topiramate) | 窪窪選壓憲壓淵衊積淵(鹽齋襯積願鹹鑰遞簾廠) = 膚廠築襯醖獵鑰淵鏇築 醖廠顧觸構鑰築壓鑰廠 (觸觸觸構鏇簾蓋鑰餘糧, 顧製淵積鑰鑰繭糧鹽鏇 ~ 鬱觸壓衊積製艱醖築蓋) 更多 | ||||||
临床4期 | 70 | 築鹹觸餘糧艱願鏇築齋(襯範築選獵繭獵選簾襯) = 構構網糧衊襯鬱蓋餘簾 壓鏇淵餘觸範願範鹹鏇 (醖構願簾鏇齋製製鬱築 ) | - | 2008-10-01 | |||
Haloperidol | 築鹹觸餘糧艱願鏇築齋(襯範築選獵繭獵選簾襯) = 構醖築蓋壓簾鬱構窪鏇 壓鏇淵餘觸範願範鹹鏇 (醖構願簾鏇齋製製鬱築 ) |
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