甲磺酸胺银内酯B(Dimethylaminoethyl Ginkgolide B Mesylate) - 药物靶点：PAF receptor_在研适应症：缺血性脑血管病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

PAF receptor

作用机制

PAF receptor拮抗剂(血小板活化因子受体拮抗剂)

治疗领域

在研适应症

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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关联

6

项与甲磺酸胺银内酯B 相关的临床试验

CTR20210115 / Recruiting临床1期

甲磺酸胺银内酯B片多次给药在健康成年受试者中的安全性、耐受性和药代动力学/药效学（PK/PD）的Ⅰ期临床研究

1.研究甲磺酸胺银内酯B片多次给药在健康成年受试者中的安全性、耐受性； 2.观察甲磺酸胺银内酯B片多次给药在健康成年受试者中的PK及PD特征，为后期临床研究的剂量选择提供依据。

开始日期2021-03-27

申办/合作机构

南京柯菲平盛辉制药有限公司

[+2]

CTR20210113 / Recruiting临床1期

注射用甲磺酸胺银内酯B单次给药在健康成年受试者中的安全性、耐受性和药代动力学/药效学（PK/PD）的Ⅰ期临床研究

1、研究注射用甲磺酸胺银内酯B单次给药在健康成年受试者中的安全性、耐受性； 2、观察注射用甲磺酸胺银内酯B单次给药在健康成年受试者中的PK及PD特征，为后期临床研究的剂量选择提供依据。

开始日期2021-01-30

申办/合作机构

南京柯菲平盛辉制药有限公司

[+2]

CTR20160610 / Completed临床1期

甲磺酸胺银内酯B片单次及多次给药随机双盲安慰剂对照PK/PD研究以及进食对PK/PD影响研究

评价甲磺酸胺银内酯B片单次及多次给药在健康受试者中的安全性、耐受性、药代动力学和药效动力学特征以及进食对药代动力学和药效动力学特征的影响

开始日期2015-10-01

申办/合作机构

南京柯菲平盛辉制药有限公司

[+2]

100 项与甲磺酸胺银内酯B 相关的临床结果

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100 项与甲磺酸胺银内酯B 相关的转化医学

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100 项与甲磺酸胺银内酯B 相关的专利（医药）

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17

项与甲磺酸胺银内酯B 相关的文献（医药）

2021-12-01·Molecular Neurobiology2区 · 医学

PAF Receptor Inhibition Attenuates Neuronal Pyroptosis in Cerebral Ischemia/Reperfusion Injury

2区 · 医学

Article

作者: Fang, Weirong ; Zhu, Jianping ; Li, Yunman ; Yin, Qiyang ; Zhao, Bo ; Fei, Yuxiang

Ischemic stroke is an inflammation-related disease, during which process activation of NLRP3 inflammasome and subsequent pyroptosis play crucial roles. Platelet-activating factor (PAF) is a potent phospholipid regulator of inflammation which exerts its effect via binding specific PAF receptor (PAFR). However, whether PAFR contributes to pyroptosis during ischemia/reperfusion (I/R) injury remains to be elucidated. To explore the underlying effect of PAFR on ischemic stroke from the perspective of pyroptosis, mice were subjected to middle cerebral artery occlusion/reperfusion (MCAO/R) injury and primary cultures of mice cerebral cortical neurons were exposed to oxygen-glucose deprivation/reoxygenation (OGD/R) injury to mimic I/R in vivo and in vitro, after which indexes associated with pyroptosis were analyzed. Intriguingly, our results indicated that inhibition of PAFR with its inhibitor XQ-1H or PAFR siRNA exerted a neuroprotective effect against I/R injury both in vivo and in vitro. Furthermore, inflammasome activation and pyroptosis after ischemic challenge were attenuated by XQ-1H or PAFR siRNA. Besides, the protection of XQ-1H was abolished by PAF stimulaiton to some extent. Moreover, XQ-1H or PAFR siRNA alleviated the neuronal pyroptosis induced by LPS and nigericin (an NLRP3 activator) in cortical neurons. Taken together, this study firstly demonstrates that PAFR is involved in neuronal pyroptosis after I/R injury, and XQ-1H, a specific PAFR inhibitor, has a promising prospect in attenuating I/R injury from the perspective of anti-pyroptosis.

2021-09-01·Journal of Stroke and Cerebrovascular Diseases4区 · 医学

10-O-(N N-Dimethylaminoethyl)-Ginkgolide B Methane-Sulfonate (XQ-1H) Ameliorates Cerebral Ischemia Via Suppressing Neuronal Apoptosis

4区 · 医学

Article

作者: Li, Yunman ; Fang, Weirong ; Li, Xiang ; Fei, Yuxiang ; Khadankhuu, Bayarmaa

OBJECTIVESThe 10-O-(N N-dimethylaminoethyl)-ginkgolide B methane-sulfonate (XQ-1H) is an effective novel drug for the treatment of ischemic cerebrovascular disease derived from Ginkgolide B, a traditional Chinese medicine, has been widely used in the treatment of cardiovascular and cerebrovascular diseases. However, whether XQ-1H exerts neuroprotective effect via regulating neuronal apoptosis and the underlying mechanism remain to be elucidated.MATERIALS AND METHODSThis study was aimed to investigate the neuroprotective effect of XQ-1H in rats subjected to middle cerebral artery occlusion/reperfusion (MCAO/R) and the oxygen glucose deprivation/reoxygenation (OGD/R) induced neuronal apoptosis on pheochromocytoma (PC-12) cells.RESULTSThe results showed that administration of XQ-1H at different dosage (7.8, 15.6, 31.2 mg/kg) reduced the brain infarct and edema, attenuated the neuro-behavioral dysfunction, and improved cell morphology in brain tissue after MCAO/R in rats. Moreover, incubation with XQ-1H (1 µM, 3 µM, 10 µM, 50 µM, 100 µM) could increase the cell viability, and showed no toxic effect to PC-12 cells. XQ-1H at following 1 µM, 10 µM, 100 µM decreased the lactate dehydrogenase (LDH) activity and suppressed the cell apoptosis in PC-12 cells exposed to OGD/R. In addition, XQ-1H treatment could significantly inhibit caspase-3 activation both in vivo and in vitro, reciprocally modulate the expression of apoptosis related proteins, bcl-2, and bax via activating PI3K/Akt signaling pathway. For mechanism verification, LY294002, the inhibitor of PI3K/Akt pathway was introduced the expressions of bcl-2 and phosphorylated Akt were down-regulated, the expression of bax was up-regulated, indicating that XQ-1H could alleviate the cell apoptosis through activating the PI3K/Akt pathway.CONCLUSIONSOur findings demonstrated that XQ-1H treatment could provide a neuroprotective effect against ischemic stroke induced by cerebral ischemia/reperfusion injury in vivo and in vitro through regulating neuronal survival and inhibiting apoptosis. The findings of the study confirmed that XQ-1H could be develop as a potential drug for treatment of cerebral ischemic stroke.

2021-05-01·Life Sciences3区 · 医学

XQ-1H promotes cerebral angiogenesis via activating PI3K/Akt/GSK3β/β-catenin/VEGF signal in mice exposed to cerebral ischemic injury

3区 · 医学

Article

作者: Li, Yunman ; Fei, Yuxiang ; Fang, Weirong ; Zhu, Jianping ; Zhao, Bo

Stroke still ranks as a most lethal disease worldwide. Angiogenesis during the chronic phase of ischemic stroke can alleviate ischemic injury and attenuate neurological deficit. XQ-1H is a new compound derived from the structure modification of ginkgolide B, which exerts anti-inflammation and neuroprotection against cerebral ischemic injury during the acute or subacute phase. However, whether XQ-1H facilitates angiogenesis and neural functional recovery during the chronic phase remains unclear. This research was designed to explore whether XQ-1H promotes angiogenesis after ischemic stroke and to preliminarily elucidate the mechanism. In vitro, XQ-1H was found to facilitate proliferation, migration and tube formation in bEnd.3 cells. In vivo, XQ-1H raised the CD31 positive microvessel number and increased focal cerebral blood flow in mice exposed to cerebral ischemic injury, and improved the neurological function. Mechanism studies revealed that XQ-1H exerted angiogenesis promoting effect via the PI3K/Akt/GSK3β/β-catenin/VEGF signal pathway, which was reversed by LY294002 (the specific inhibitor of PI3K/Akt). In conclusion, XQ-1H exerts angiogenetic effect both in vivo and in vitro, which is a potential agent against ischemic stroke during chronic phase.

100 项与甲磺酸胺银内酯B 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
缺血性脑血管病	临床1期	中国	南京柯菲平盛辉制药有限公司	2014-11-11
缺血性脑血管病	临床1期	中国	江苏柯菲平医药股份有限公司	2014-11-11
急性缺血性卒中	临床前	中国	江苏柯菲平医药股份有限公司	2012-08-05