更新于：2024-06-29
Quinidine Gluconate
奎尼丁葡萄糖酸盐
更新于：2024-06-29
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) |
治疗领域 |
在研适应症- |
非在研适应症 |
原研机构 |
在研机构- |
最高研发阶段撤市 |
首次获批日期 美国 (1950-07-12), |
最高研发阶段(中国)- |
特殊审评- |
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结构
分子式C26H36N2O9 |
InChIKeyXHKUDCCTVQUHJQ-LCYSNFERSA-N |
CAS号7054-25-3 |
关联
17
项与 奎尼丁葡萄糖酸盐 相关的临床试验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
Quinidine Versus Verapamil in Short-coupled Idiopathic Ventricular Fibrillation: an Open-label, Randomized Crossover Pilot Trial
Quinidine versus verapamil in short-coupled idiopathic ventricular fibrillation: An open label, randomized crossover pilot trial - QUEEN-IVF
100 项与 奎尼丁葡萄糖酸盐 相关的临床结果
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100 项与 奎尼丁葡萄糖酸盐 相关的转化医学
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100 项与 奎尼丁葡萄糖酸盐 相关的专利（医药）
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6,950
项与 奎尼丁葡萄糖酸盐 相关的文献（医药）2024-02-01Journal of chromatography. A
Chiral zwitterionic stationary phases based on Cinchona alkaloids and dipeptides – design, synthesis and application in chiral separation
Article
作者: Tůma, Jiří ; Asnin, Leonid ; Kohout, Michal ; Kuncová, Anežka ; Schug, Kevin ; Svoboda, Jiří
Chiral resolution of polar organic compounds such as amino acids and peptides represents an important chromatographic task due to increasing significance of natural species, which play important signaling and regulatory roles in the living organisms. Despite the number of available chiral stationary phases, this task remains challenging, since not many of the commercially available systems are capable to resolve non-derivatized zwitterionic species. In this study, we present a target-oriented design of a new class of chiral selectors. Pursuing the goal to separate amino acids, and especially short peptides, we have combined Cinchona alkaloids - quinine and quinidine - with three different biogenic dipeptides. We have synthesized six different chiral stationary phases, with selector loading of ∼200 μmol g-1, and tested their chiral recognition capabilities for acidic, basic and zwitterionic analytes using various mobile phases. We have observed that all chiral stationary phases retain the chiral anion exchange capability known for commercially available Cinchona-based columns leading to baseline or partial resolution of six out of ten analytes. The performance in chiral resolution of basic analytes is not optimum due to the weak cation exchange character of the peptidic residue. However, we report on encouraging results in the chiral resolution of short peptides, for which, depending on their structure, we see the chiral resolution of up to three stereoisomers (from four possible) in a preliminary screening.
2024-02-01Drug metabolism and disposition: the biological fate of chemicals
Utilizing a Dual Human Transporter MDCKII-MDR1-BCRP Cell Line to Assess Efflux at the Blood Brain Barrier
Article
作者: Harlfinger, Stephanie ; Li, Wei ; Sproat, Graham G ; Gozalpour, Elnaz ; Li, Danxi ; O'Neill, Daniel J ; Colclough, Nicola ; Du, Hongwen ; Chen, Kan ; McGinnity, Dermot F ; Tucker, James W ; Yan, Yumei ; Alluri, Ravindra V
To facilitate the design of drugs readily able to cross the blood brain barrier (BBB), a Madin-Darby canine kidney (MDCK) cell line was established that over expresses both P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP), the main human efflux transporters of the BBB. Proteomics analyses indicate BCRP is expressed at a higher level than Pgp in this cell line. This cell line shows good activity for both transporters [BCRP substrate dantrolene efflux ratio (ER) 16.3 ± 0.9, Pgp substrate quinidine ER 27.5 ± 1.2], and use of selective transporter inhibitors enables an assessment of the relative contributions to overall ERs. The MDCKII-MDR1-BCRP ER negatively correlates with rat unbound brain/unbound plasma ratio, Kpuu Highly brain penetrant compounds with rat Kpuu ≥ 0.3 show ERs ≤ 2 in the MDCKII-MDR1-BCRP assay while compounds predominantly excluded from the brain, Kpuu ≤ 0.05, demonstrate ERs ≥ 20. A subset of compounds with MDCKII-MDR1-BCRP ER < 2 and rat Kpuu < 0.3 were shown to be substrates of rat Pgp using a rat transfected cell line, MDCKII-rMdr1a. These compounds also showed ERs > 2 in the human National Institutes of Health (NIH) MDCKI-MDR1 (high Pgp expression) cell line, which suggests that they are weak human Pgp substrates. Characterization of 37 drugs targeting the central nervous system in the MDCKII-MDR1-BCRP efflux assay show 36 have ERs < 2. In drug discovery, use of the MDCKII-MDR1-BCRP in parallel with the NIH MDCKI-MDR1 cell line is useful for identification of compounds with high brain penetration. SIGNIFICANCE STATEMENT: A single cell line that includes both the major human efflux transporters of the blood brain barrier (MDCKII-MDR1-BCRP) has been established facilitating the rapid identification of efflux substrates and enabling the design of brain penetrant molecules. Efflux ratios using this cell line demonstrate a clear relationship with brain penetration as defined by rat brain Kpuu.
2024-02-01Homeopathy : the journal of the Faculty of Homeopathy
Antiviral Activity of Cinchona officinalis, a Homeopathic Medicine, against COVID-19
Article
作者: Dhaked, Devendra Kumar ; Velayutham, Ravichandiran ; Das, Pamelika ; Singh, Subhas ; Yellurkar, Manoj Limbraj ; Thomas, Austin Jose ; Singh, Lalith ; Arumugam, Somasundaram ; Manoharan, Raja ; Vadivel, Kumaravel ; Prasanna, Vani Sai
Abstract:
Background Coronavirus disease 2019 (COVID-19) is a potentially fatal disease caused by the novel severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Several studies have shown that hydroxychloroquine (HCQ) significantly inhibits SARS-CoV-2 infections in vitro.
Objective Since the phytoconstituents of Cinchona officinalis (CO) are similar to those of HCQ, the objective of this study was to test the antiviral potential of different homeopathic formulations of CO.
Methods An analysis of the molecular composition of CO was carried out using ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry, followed by a detailed docking study. The constituents of CO were docked against various targets of SARS-CoV-2, and the binding potential of the phytoconstituents was compared and quantified. The ligand with the lowest Glide docking score is considered to have the best binding affinity. The cytotoxicity of several homeopathic formulations, including CO mother tincture (CO-MT), was also checked on VeroE6 cells. A known antiviral, remdesivir, was used as a positive control for the in vitro assays to evaluate the effects of CO-MT against SARS-CoV-2-infected VeroE6 cells.
Results Molecular docking studies showed that constituents of CO exhibited binding potential to various targets of SARS-CoV-2, including Mpro, PLpro, RdRp, nucleocapsid protein, ACE2 (in host) and spike protein. Quinoline, one of the constituents of CO, can potentially bind the spike protein of SARS-CoV-2. Quinic acid showed better binding capabilities with Mpro, PLpro RdRp, nucleocapsid protein and ACE2 (allosteric site) than other constituents. Quinidine exhibited better binding to ACE2. Compared to HCQ, other phytoconstituents of CO had the equivalent potential to bind the RNA-dependent RNA polymerase, nucleocapsid protein, Mpro, PLpro and spike protein of SARS-CoV-2. In vitro assays showed that homeopathic CO-MT was not cytotoxic and that CO-MT and remdesivir respectively caused 89% and 99% inhibition of SARS-CoV-2 infection in VeroE6 cells.
Conclusion Based on this in silico and in vitro evidence, we propose CO-MT as a promising antiviral medicine candidate for treating COVID-19. In vivo investigation is required to clarify the therapeutic potential of CO-MT in COVID-19.
12
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
2024-02-13
100 项与 奎尼丁葡萄糖酸盐 相关的药物交易
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研发状态
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 |
|---|---|---|---|
| 心律失常 | 美国 | 1950-07-12 |
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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
N/A | - | 糧齋鏇餘夢餘鑰憲糧網(蓋襯製鏇築繭醖窪夢壓): HR = 0.74 (95% CI, 0.22 ~ 2.48), P-Value = 0.62 | - | 2019-09-03 | |||
quinidine | |||||||
N/A | KCNT1 gene mutation | 1 | 積蓋範遞壓遞鑰顧構繭(壓糧鑰醖鏇壓遞鑰獵簾) = 衊壓積築鬱鹹廠繭憲積 築夢膚糧積構襯鹹鑰構 (鏇鹽艱鹹醖簾獵製範淵 ) | 积极 | 2018-10-05 | ||
N/A | - | - | 選鏇繭獵鑰餘遞廠餘簾(築糧襯築鑰鹹鬱築繭膚) = 夢鑰願鬱觸築網鑰網積 鏇衊膚獵餘構網繭網艱 (觸獵窪觸選獵夢鏇鏇簾, ± 12.4) | - | 2002-06-12 |
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