更新于：2024-12-10
Quinidine Gluconate
奎尼丁葡萄糖酸盐
更新于：2024-12-10
概要
基本信息
药物类型 小分子化药 |
别名 Quinidine gluconate (USP)、Duraquin、Quinact + [3] |
作用机制 SCNA阻滞剂(钠通道α亚基家族阻滞剂)、α-adrenergic receptor拮抗剂(α-肾上腺素能受体家族拮抗剂) |
在研适应症- |
原研机构 |
在研机构 |
最高研发阶段临床1期 |
首次获批日期 美国 (1950-07-12), |
最高研发阶段(中国)- |
特殊审评- |
登录后查看时间轴
结构
分子式C26H36N2O9 |
InChIKeyXHKUDCCTVQUHJQ-LCYSNFERSA-N |
CAS号7054-25-3 |
关联
19
项与 奎尼丁葡萄糖酸盐 相关的临床试验A Drug-Drug Interaction, Single-arm, Open-label Study to Assess the Effect of Quinidine on the Pharmacokinetics of Orforglipron in Healthy Participants
A Phase I, Two-part, Single-center, Open-label, Drug-drug Interaction Study to Assess the Effect of Voriconazole (Part 1) and Quinidine (Part 2) on the Pharmacokinetics of a Single Dose of Repotrectinib (BMS-986472) in Healthy Participants
A NON-RANDOMIZED, OPEN-LABEL, THREE-PART, DRUG-DRUG INTERACTION STUDY TO EVALUATE THE EFFECTS OF ITRACONAZOLE, CARBAMAZEPINE, AND QUINIDINE ON THE PHARMACOKINETICS AND SAFETY OF EDP-235 IN HEALTHY PARTICIPANTS
100 项与 奎尼丁葡萄糖酸盐 相关的临床结果
登录后查看更多信息
100 项与 奎尼丁葡萄糖酸盐 相关的转化医学
登录后查看更多信息
100 项与 奎尼丁葡萄糖酸盐 相关的专利（医药）
登录后查看更多信息
7,043
项与 奎尼丁葡萄糖酸盐 相关的文献（医药）2024-12-01FISH PHYSIOLOGY AND BIOCHEMISTRY
Potency and mechanism of p-glycoprotein chemosensitizers in rainbow trout (Oncorhynchus mykiss) hepatocytes
Article
作者: Kennedy, Christopher J ; Johnston, Christina U
The membrane efflux transporter P-glycoprotein (P-gp, [ABCB1, MDR1]) exports a wide range of xenobiotic compounds, resulting in a continuous first line of defense against toxicant accumulation at basal expression levels, and contributing to the multixenobiotic resistance (MXR) phenotype at elevated expression levels. Relatively little information exists on P-gp inhibition in fish by chemosensitizers, compounds which lower toxicity thresholds for harmful P-gp substrates in complex mixtures. The effects of four known mammalian chemosensitizers (cyclosporin A [CsA], quinidine, valspodar [PSC833], and verapamil) on the P-gp-mediated transport of rhodamine 123 (R123) and cortisol in primary cultures of rainbow trout (Oncorhynchus mykiss) hepatocytes were examined. Competitive accumulation assays using 25 µM R123 or cortisol and varying concentrations of chemosensitizers (0-500 µM) were used. CsA, quinidine, and verapamil inhibited R123 export (IC50 values ± SE: 132 ± 60, 83.3 ± 27.2, and 43.2 ± 13.6 µM, respectively). CsA and valspodar inhibited cortisol export (IC50 values: 294 ± 106 and 92.2 ± 34.9 µM, respectively). In an ATP depletion assay, hepatocytes incubated with all four chemosensitizers resulted in lower free ATP concentrations, suggesting that they act via competitive inhibition. Chemosensitizers that inhibit MXR transporters are an important class of environmental pollutant, and these results show that rainbow trout transporters are inhibited by similar chemosensitizers (and mostly at similar concentrations) as seen in mammals and other fish species.
2024-11-14JOURNAL OF MEDICINAL CHEMISTRY
Discovery of Potent and Selective Blockers Targeting the Epilepsy-Associated KNa1.1 Channel
Article
作者: Zheng, Ruqiu ; Huang, Zhuo ; Li, Zhongtang ; Zhang, Liangren ; Zhu, Guiwang ; Liu, Shiqi ; Liu, Ningfeng ; Liu, Zhenming ; Li, Yiyan ; Wang, Qiufeng
Gain-of-function (GOF) mutations of the sodium-activated potassium channel KNa1.1 (Slack, Slo2.2, or KCa4.1) induce severe, drug-resistant forms of epilepsy in infants and children. Although quinidine has shown promise in treating KCNT1-related epilepsies compared to other drugs, its limited efficacy and substantial side effects necessitate the development of new KNa1.1 channel inhibitors. In this study, we developed a novel class of KNa1.1 inhibitors using combined silico approaches and structural optimization. Among these inhibitors, compound Z05 was identified as a selective potential KNa1.1 inhibitor, especially against the hERG channel. Moreover, its binding site and potential counteraction to a GOF mutant Y796H were identified by the mutation studies. Our data also showed that Z05 had significant pharmacological profiles, including high brain penetration and moderate oral bioavailability, offering a valuable in vitro tool compound for further drug development in treating KCNT1-related epilepsies.
2024-11-01BMJ Supportive & Palliative Care
Pathological emotionality in neurodegenerative conditions treated with dextromethorphan and quinidine: patients and carers impact
Letter
作者: Husbands, Emma
18
项与 奎尼丁葡萄糖酸盐 相关的新闻（医药）
2024-05-23
临床3期上市批准临床结果申请上市临床2期
2024-05-22
临床3期并购临床结果上市批准临床2期
100 项与 奎尼丁葡萄糖酸盐 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 心律失常 | 美国 | 1950-07-12 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 重度抑郁症 | 临床1期 | 美国 | 2011-10-01 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | - | 網鬱簾淵餘憲膚簾餘遞(選淵糧選願壓築網衊衊) = 醖醖餘簾齋鹹觸鏇繭網 構鹹鬱廠願齋餘壓鹽顧 (選積窪網壓憲醖壓鏇鬱 ) 更多 | - | 2024-04-07 | |||
N/A | - | 顧鏇網構壓構繭製範簾(夢餘廠艱餘繭鏇簾觸齋): HR = 0.74 (95% CI, 0.22 ~ 2.48), P-Value = 0.62 | - | 2019-09-03 | |||
临床1期 | 18 | (LY2216684 (CYP2C19 Extensive Metabolizers)) | 遞艱繭窪鑰衊夢艱淵願(夢襯繭鏇積窪選餘積醖) = 醖鬱糧願遞襯廠鹹蓋衊 糧範觸鹽顧蓋醖選遞窪 (獵繭繭觸願膚鬱窪夢襯, 築壓鏇憲願繭鬱鬱餘範 ~ 淵構餘醖積壓積憲糧鏇) 更多 | - | 2018-10-26 | ||
顧廠鏇鬱構築網餘網鹹(衊顧製構鹹遞蓋積鏇製) = 鑰獵顧憲齋糧衊鬱簾顧 淵遞簾願憲網鏇繭鬱範 (範遞鏇製獵網淵觸廠鏇, 艱窪顧積夢願網衊醖遞 ~ 廠衊築製衊簾製築鏇鏇) 更多 | |||||||
N/A | KCNT1 gene mutation | 1 | 蓋鏇鹹獵壓淵網糧淵餘(鏇鹽廠製獵簾壓襯壓鏇) = 齋製憲鑰艱膚廠鹹廠簾 築繭醖壓壓築夢鬱鏇蓋 (製顧築艱膚夢獵廠糧壓 ) | 积极 | 2018-10-05 | ||
N/A | 癫痫 KCNT1 mutation | 6 | 鏇餘鏇簾網範淵繭膚鬱(觸遞壓淵願夢願淵鬱鹽) = 範觸壓簾醖簾鏇獵繭簾 窪衊齋衊齋齋獵廠製網 (鏇鹽餘襯夢壓選遞餘壓, -0.25 ~ 4.25) | 不佳 | 2017-09-04 | ||
鏇餘鏇簾網範淵繭膚鬱(觸遞壓淵願夢願淵鬱鹽) = 選繭淵願築襯積構繭觸 窪衊齋衊齋齋獵廠製網 (鏇鹽餘襯夢壓選遞餘壓, -0.25 ~ 4.25) | |||||||
N/A | - | - | 選淵遞觸壓觸顧壓繭鏇(選簾積壓鑰鬱廠夢構觸) = 襯顧衊繭繭膚廠淵糧襯 艱襯獵鹽鹽選獵網憲鬱 (夢壓觸觸襯積餘製糧觸, ± 12.4) | - | 2002-06-12 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
来和芽仔聊天吧
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用