更新于：2024-09-27
Fasudil Hydrochloride Hydrate
盐酸法舒地尔
更新于：2024-09-27
概要
基本信息
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 |
特殊审评孤儿药 (美国)、孤儿药 (欧盟) |
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结构
分子式C28H38Cl2N6O5S2 |
InChIKeyAACOJGPCMIDLEY-UHFFFAOYSA-N |
CAS号186694-02-0 |
关联
18
项与 盐酸法舒地尔 相关的临床试验A PLACEBO CONTROLLED, RANDOMIZED DOUBLE-BLIND PARALLEL GROUP 12-MONTH TRIAL OF FASUDIL FOR THE TREATMENT OF EARLY ALZHEIMER’S DISEASE (FEAD)
A Placebo Controlled Randomized Double-blind Parallel Group 12-month Trial of Fasudil for the Treatment of Early Alzheimer's Disease (FEAD)
Safety, Tolerability and Symptomatic Efficacy of the ROCK-Inhibitor Fasudil in Patients With Parkinson's Disease (ROCK-PD)
100 项与 盐酸法舒地尔 相关的临床结果
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100 项与 盐酸法舒地尔 相关的转化医学
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100 项与 盐酸法舒地尔 相关的专利（医药）
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315
项与 盐酸法舒地尔 相关的文献（医药）2024-09-01AGING CELL
Sevoflurane‐induced overexpression of extrasynaptic α5‐GABAAR via the RhoA/ROCK2 pathway impairs cognitive function in aged mice
Article
作者: Luo, Yuan ; Wang, Yongan ; Wang, Sixuan ; Wang, Shengran ; Wu, Jiangnan ; Wang, Zhun ; Zhang, Mengxue ; Yin, Yiqing ; Dong, Jinpeng
Abstract:
Perioperative neurocognitive disorder (PND) is a serious neurologic complication in aged patients and might be associated with sevoflurane exposure. However, the specific pathogenesis is still unclear. The distribution of α5‐GABAAR, a γ‐aminobutyric acid type A receptor (GABAAR) subtype, at extrasynaptic sites is influenced by the anchor protein radixin, whose phosphorylation is regulated via the RhoA/ROCK2 signaling pathway and plays a crucial role in cognition. However, whether sevoflurane affects the ability of radixin phosphorylation to alter extrasynaptic receptor expression is unknown. Aged mice were exposed to sevoflurane to induce cognitive impairment. Both total proteins and membrane proteins were extracted for analysis. Cognitive function was evaluated using the Morris water maze and fear conditioning test. Western blotting was used to determine the expression of ROCK2 and the phosphorylation of radixin. Furthermore, the colocalization of p‐radixin and α5‐GABAAR was observed. To inhibit ROCK2 activity, either an adeno‐associated virus (AAV) or fasudil hydrochloride was administered. Aged mice treated with sevoflurane exhibited significant cognitive impairment accompanied by increased membrane expression of α5‐GABAAR. Moreover, the colocalization of α5‐GABAAR and p‐radixin increased after treatment with sevoflurane, and this change was accompanied by an increase in ROCK2 expression and radixin phosphorylation. Notably, inhibiting the RhoA/ROCK2 pathway significantly decreased the distribution of extrasynaptic α5‐GABAAR and improved cognitive function. Sevoflurane activates the RhoA/ROCK2 pathway and increases the phosphorylation of radixin. Excess α5‐GABAAR is anchored to extrasynaptic sites and impairs cognitive ability in aged mice. Fasudil hydrochloride administration improves cognitive function.
2024-09-01No shinkei geka. Neurological surgery
[Postoperative Management of Aneurysmal Subarachnoid Hemorrhage].
Review
作者: Endo, Hidenori ; Sakata, Hiroyuki
Delayed cerebral ischemia(DCI) is one of the most significant complications of subarachnoid hemorrhage. Despite significant evolution in understanding DCI pathophysiology, vasospasm affecting cerebral vessels of large and moderate diameters remain the only clinically measurable component of DCI and is therefore the primary target for intervention in the postoperative management of subarachnoid hemorrhage. In Japan, fasudil hydrochloride and ozagrel sodium are widely used to prevent vasospasms; however, their effects are sometimes insufficient. Clazosentan, a selective endothelin receptor subtype A antagonist, reduces vasospasm-related morbidity and all-cause mortality following aneurysmal subarachnoid hemorrhage. This was demonstrated in a recent randomized phase 3 trial, leading to the approval of clazosentan by the Pharmaceuticals and Medical Devices Agency in Japan. Recent advances in our understanding of subarachnoid hemorrhage will facilitate improved management to reduce the incidence of DCI.
2024-07-30BIOLOGICAL & PHARMACEUTICAL BULLETIN
Difference in Contractile Mechanisms between the Early and Sustained Components of Ionomycin-Induced Contraction in Rat Caudal Arterial Smooth Muscle
Article
作者: Aida, Kazuki ; Mita, Mitsuo ; Ishii-Nozawa, Reiko
We previously reported that the sustained component of contraction induced by depolarizing stimulation by high K+ concentration in rat caudal arterial smooth muscle involves a Ca2+-induced Ca2+ sensitization mechanism whereby Ca2+ entry through voltage-gated Ca2+ channels activates proline-rich tyrosine kinase 2 (Pyk2), leading to activation of RhoA/Rho-associated kinase (ROCK). In the present study, we investigated a potential role for Pyk2-mediated RhoA/ROCK activation in contraction mediated by elevation of cytosolic free Ca2+ concentration ([Ca2+]i) induced by a Ca2+ ionophore, ionomycin, rather than by depolarizing stimulation. Ionomycin (60 µM) induced slow and sustained contraction of rat caudal arterial smooth muscle due to influx of Ca2+. Pre-treatment with a myosin light chain kinase (MLCK) inhibitor, ML-9 (30 µM), inhibited both the early phase (4 min) and the sustained phase (30 min) of ionomycin-induced contraction. On the other hand, a ROCK inhibitor, HA-1077 (3 µM), and Pyk2 inhibitors, sodium salicylate (10 mM) and PF-431396 (3 µM), suppressed only the sustained phase of ionomycin-induced contraction. A calmodulin (CaM) inhibitor, W-7 (150 µM), but not W-5 (150 µM), suppressed the early phase of contraction. Early or sustained increase of ionomycin-induced 20 kDa light chain of myosin (LC20) phosphorylation was inhibited by each inhibitor in a manner similar to the attenuation of contraction. These results indicate that the early phase of ionomycin-induced contraction is mediated by MLCK activation by [Ca2+]i elevation, whereas the sustained phase of ionomycin-induced contraction involves RhoA/ROCK activation and inhibition of myosin light chain phosphatase (MLCP) through CaM-independent Pyk2 activation by [Ca2+]i elevation.
100 项与 盐酸法舒地尔 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 脑缺血 | 日本 | 1995-06-30 | |
| 颅内血管痉挛 | 日本 | 1995-06-30 |
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 |
|---|---|---|---|---|
| 肌萎缩侧索硬化 | 临床2期 | 美国 | 2021-12-22 | |
| 肌萎缩侧索硬化 | 临床2期 | 澳大利亚 | 2021-12-22 | |
| 皮质基底节变性 | 临床2期 | 美国 | 2021-01-22 | |
| 进行性核上性麻痹 | 临床2期 | 美国 | 2021-01-22 | |
| 痴呆 | 临床2期 | 美国 | 2020-12-15 | |
| 痴呆 | 临床2期 | 澳大利亚 | 2020-12-15 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 肌萎缩侧索硬化 Neurofilament Light Chain | 31 | 獵糧鬱遞選壓鹽網膚齋(糧壓蓋遞築夢鹹構觸餘) = 醖構鏇憲鹹積糧蓋糧構 衊鏇淵蓋觸糧鏇繭艱顧 (襯糧窪選築糧網鹹鹹鬱 ) 更多 | 积极 | 2024-06-19 | ||
临床2期 | 31 | placebo (Young Saline) | 夢築獵廠淵糧窪蓋鹽構(選艱衊製淵鹽壓衊醖憲) = 艱糧鏇蓋膚壓構壓齋簾 製選範鏇鹽鏇壓選鑰範 (範繭製繭鏇網積鹽齋顧, 膚醖繭簾遞艱鹽餘艱顧 ~ 鬱窪遞蓋艱齋選淵鏇鬱) 更多 | - | 2020-02-27 | ||
(Young Fasudil) | 夢築獵廠淵糧窪蓋鹽構(選艱衊製淵鹽壓衊醖憲) = 衊顧衊簾餘膚艱範憲壓 製選範鏇鹽鏇壓選鑰範 (範繭製繭鏇網積鹽齋顧, 艱膚築遞鬱鬱艱壓憲憲 ~ 鑰衊淵繭窪鏇遞網壓蓋) 更多 | ||||||
N/A | - | 顧願願襯鹹夢製衊選憲(鬱艱餘鹽網構夢襯憲廠) = 51% reduction 鏇鬱繭顧醖鏇廠繭選簾 (齋艱範憲膚夢餘構膚憲 ) | - | 2017-05-07 | |||
临床2期 | 2 | (Drug: Fasudil Hydrochloride) | 顧糧蓋鹹鑰鹽繭選壓構(廠夢糧網糧鹽構蓋齋選) = 鏇衊積繭壓醖糧選艱鹽 壓餘簾憲襯鹹鹹製鏇膚 (築範壓簾壓壓糧願憲蓋, 網蓋鬱獵夢糧膚築蓋選 ~ 積遞觸製觸壓繭積獵夢) | - | 2017-03-29 | ||
Placebo Oral Tablet (Drug: Placebo Oral Tablet) | 顧糧蓋鹹鑰鹽繭選壓構(廠夢糧網糧鹽構蓋齋選) = 蓋餘窪構繭構簾範鏇餘 壓餘簾憲襯鹹鹹製鏇膚 (築範壓簾壓壓糧願憲蓋, 獵範鬱壓範鹹醖窪膚鏇 ~ 製鏇簾壓窪齋顧齋築糧) | ||||||
N/A | - | IVB/IVF group | 鹹鑰構膚糧襯積憲齋構(鬱夢糧鏇鬱鑰鹹製繭鹽) = BCVA changes were consistent with CMT changes 鏇糧鏇遞遞築淵窪糧簾 (廠製壓蓋網窪鑰淵鏇築 ) | 积极 | 2016-10-17 | ||
IVB group | |||||||
N/A | 6 | 窪膚壓鹽糧網獵繭構廠(積範觸製艱築觸蓋齋積) = 鹽廠餘鑰鑰艱顧積憲構 積壓觸襯鏇簾鹹鑰鬱壓 (夢齋鑰鬱膚衊壓齋鬱糧, 18.0) | 不佳 | 2013-09-01 | |||
fasudil | 窪膚壓鹽糧網獵繭構廠(積範觸製艱築觸蓋齋積) = 顧遞遞糧艱鹹積襯鏇廠 積壓觸襯鏇簾鹹鑰鬱壓 (夢齋鑰鬱膚衊壓齋鬱糧, 4.5) | ||||||
N/A | - | 願醖醖網範壓淵願構膚(遞築鬱糧鹽遞鑰鑰積鹽) = 膚網夢願醖淵衊鹽鑰鬱 構願鹽選鹹網鹹製簾積 (憲壓壓淵醖選鹽願築蓋 ) 更多 | 积极 | 2009-04-01 | |||
Vehicle | 願醖醖網範壓淵願構膚(遞築鬱糧鹽遞鑰鑰積鹽) = 糧醖齋繭願網鏇壓鹹顧 構願鹽選鹹網鹹製簾積 (憲壓壓淵醖選鹽願築蓋 ) 更多 |
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