更新于：2024-06-21
Levodopa/Benserazide Hydrochloride
多巴丝肼
更新于：2024-06-21
概要
基本信息
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (1979-08-27), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C19H26N4O9 |
InChIKeyQFLMOYQNYBDXMT-ZCMDIHMWSA-N |
CAS号37270-69-2 |
关联
72
项与 多巴丝肼 相关的临床试验Clinical study of Madopar in the treatment of early stage steroid-induced osteonecrosis of the femoral head
嘉亨（珠海横琴）医药科技有限公司研制的多巴丝肼片与持证商为上海罗氏制药有限公司的多巴丝肼片（商品名：美多芭®）在中国健康受试者中进行的随机、开放、单剂量、两序列、四周期、交叉、空腹及餐后状态下的生物等效性研究
上海理想制药有限公司研制的多巴丝肼片与持证商为上海罗氏制药有限公司的多巴丝肼片（商品名：美多芭®）在中国健康受试者中进行的随机、开放、单剂量、两序列、四周期、交叉、空腹及餐后状态下的生物等效性研究
100 项与 多巴丝肼 相关的临床结果
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100 项与 多巴丝肼 相关的转化医学
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100 项与 多巴丝肼 相关的专利（医药）
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461
项与 多巴丝肼 相关的文献（医药）2024-02-11Journal of biomolecular structure & dynamics
Biophysical insights on the interaction of anticoagulant drug dicoumarol with calf thymus-DNA: deciphering the binding mode and binding force with thermodynamics
Article
作者: Saranya, Jagadeesan ; Bodapati, Anna Tanuja Safala ; Sahoo, Bijaya Ketan ; Madku, Shravya Rao ; Lavanya, K ; Reddy, Ragaiahgari Srinivas
The biological activity of drugs is exhibited due to their interactions with bio-receptors. Dicoumarol (DIC) is a natural hydroxycoumarin and a well-known anticoagulant. DNA is the genetic material and one of the targets of numerous drugs. The interaction of DIC with calf-thymus DNA (ct-DNA) has been studied using different biophysical techniques and docking studies. The binding constant in the order of 103 to 104 M-1 was observed from spectroscopic studies. Thermodynamic studies at 4 different temperatures revealed the spontaneity of the interaction with the entropy-driven process. Marker displacement studies with competitive markers of intercalators (ethidium bromide) and groove binders (Hoechst 33258) confirmed the groove-binding nature of DIC in DNA. The groove-binding mode of DIC was complemented by different studies like viscosity measurements, DNA melting, and the effect of KI on the binding. A minor perturbation in the DNA viscosity and no significant change in the DNA melting temperature (Tm) after binding with DIC further confirms the groove binding mode. The effect of KI on the DIC and DIC-DNA system suggested the absence of DIC intercalation. The absence of significant electrostatic force was revealed from the ionic-strength effect study. Binding-induced conformational variation in ct-DNA was absent in circular dichroism studies. Molecular docking studies suggested the position of DIC within the minor groove of ct-DNA, covering three base pairs long. The outcome of this report may help in understanding the pharmacodynamics and pharmacokinetics of dicoumarol analogs and related molecules.Communicated by Ramaswamy H. Sarma.
2024-01-01The Science of the total environment
Bioaccumulation of pharmaceuticals and stimulants in macrobenthic food web in the European Arctic as determined using stable isotope approach
Article
作者: Caban, Magda ; Mordec, Marlena ; Balazy, Piotr ; Wielogórska, Ewa ; Øverjordet, Ida Beathe ; Lepoint, Gilles ; Chełchowski, Maciej ; Sokołowski, Adam ; Włodarska-Kowalczuk, Maria
Although pharmaceuticals are increasingly detected in abiotic matrices in the Arctic, the accumulation of drugs in the resident biota and trophic transfer have not been yet examined. This study investigated the behaviour of several pharmaceuticals in the rocky-bottom, macrobenthic food web in the coastal zone of Isfjorden (western Spitsbergen) using stable isotope analyses (SIA) coupled with liquid chromatography-mass spectrometry (LC-MS/MS). Across 16 macroalgal and invertebrate species the highest average concentration was measured for ciprofloxacin (CIP) (on average 60.3 ng g-1 dw) followed by paracetamol (PCT) (51.3 ng g-1 dw) and nicotine (NIC) (37.8 ng g-1 dw). The biomagnification potential was assessed for six target compounds of 13 analytes detected that were quantified with a frequency > 50 % in biological samples. The trophic magnification factor (TMF) ranged between 0.3 and 2.8, and was significant for NIC and CIP. TMF < 1.0 for NIC (0.3; confidence interval, CI 0.1-0.5) indicated that the compound does not accumulate with trophic position. The dilution of pharmaceutical residues in the food web may result from limited intake with dietary route, poor assimilation efficiency and high biotransformation rates in benthic invertebrates. TMF for CIP (2.8, CI 1.2-6.4) suggests trophic magnification, a phenomenon observed previously for several antibiotics in freshwater food webs. Trophic transfer therefore plays a role in controlling concentration of CIP in the Arctic benthic communities and should be considered in environmental risk assessment. Biomagnification potential of diclofenac (DIC; 0.9, CI 0.5-1.7), carbamazepine (CBZ; 0.4, CI 0.1-2.1), caffeine (CAF; 0.9, CI 0.5-1.9) and PCT (1.3, CI 0.7-2.7) was not evident due to large 95 % confidence of their TMFs. This study provides the first evidence of drug bioaccumulation in the Arctic food web and indicates that behaviour of pharmaceuticals varies among target compounds.
2023-12-01Biochemical and biophysical research communications
Evaluating the protective effect of metformin against diclofenac-induced oxidative stress and hepatic damage: In vitro and in vivo studies
Article
作者: Heidari, Mahmoud-Reza ; Jafari, Elham ; Rahimi, Hamid-Reza ; Mandegary, Ali ; Aminzadeh, Azadeh ; Darijani, Mohammad Hossein ; Karami-Mohajeri, Somayyeh
Diclofenac (DIC) is one of the most commonly prescribed non-steroidal anti-inflammatory drugs and has been shown to cause oxidative stress and liver injury. The current study investigated protective effects of metformin against DIC-induced hepatic toxicity in both in vitro and in vivo models. For the in vitro study, HepG2 cells were exposed to DIC in the presence or absence of metformin. The effect of metformin on cell viability was evaluated by MTT assay. Oxidative stress parameters (malondialdehyde (MDA), total thiol molecules (TTM), and total antioxidant capacity (TAC)) were assessed. For the in vivo study, thirty-six male Wistar rats were randomly divided into 6 groups. These groups were normal saline, metformin (200 mg/kg), DIC (50 mg/kg/day), DIC + metformin (50, 100, and 200 mg/kg/day). Histopathological studies and serum levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), lactate dehydrogenase (LDH), albumin, direct and total bilirubin were measured. Also, oxidative stress parameters were assessed in liver tissue. Furthermore, expression of glutathione peroxidase (GPX)-1, -3, and -4, catalase (CAT), superoxide dismutase (SOD)-1, and -3 was examined using the real-time PCR method in hepatic tissue. In the in vitro study, metformin significantly prevented DIC-induced loss in cell viability in HepG2 cells. Metformin markedly reduced DIC-induced elevation of MDA levels and increased the TAC and TTM levels. In the in vivo study, metformin significantly prevented DIC-induced changes in hematological and histological markers. Administration of metformin significantly improved oxidative stress parameters in liver tissue. In addition, metformin increased the expression of antioxidant enzymes. Our results suggest that metformin exerts a significant protective effect against DIC-induced hepatic toxicity.
100 项与 多巴丝肼 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
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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 |
|---|---|---|---|
| 帕金森病 | 日本 | 1979-08-27 | |
| 帕金森病 | 日本 | 1979-08-27 | |
| 帕金森病 | 日本 | 1979-08-27 |
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临床结果
临床结果
适应症
分期
评价
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临床1/2期 | 41 | 襯襯顧壓齋糧鹽廠夢糧(夢繭築網顧餘憲蓋遞衊) = 齋窪顧餘獵衊蓋壓夢窪 遞齋獵憲鹽獵製憲鑰簾 (艱顧選壓鑰選壓餘艱廠, 積餘獵憲獵蓋醖觸艱壓 ~ 淵淵網廠鏇鹹膚顧衊簾) | - | 2023-03-03 | |||
临床2期 | 58 | 廠憲蓋築鑰糧遞鹽簾繭(鑰憲觸鏇餘壓積網觸選) = 憲繭廠繭餘網淵醖襯觸 構蓋壓壓獵淵簾顧願鑰 (鬱艱餘窪衊蓋餘廠餘範, 獵願鏇夢壓艱壓艱製製 ~ 顧窪鏇膚襯廠淵網觸廠) 更多 | - | 2020-02-28 | |||
廠憲蓋築鑰糧遞鹽簾繭(鑰憲觸鏇餘壓積網觸選) = 願淵窪鹹網糧鏇鹽顧餘 構蓋壓壓獵淵簾顧願鑰 (鬱艱餘窪衊蓋餘廠餘範, 鏇齋鹹觸鏇餘選衊製願 ~ 廠壓遞築構繭艱鬱網糧) 更多 | |||||||
临床2期 | 38 | Recombinant Interferon Alfa-2b+Dacarbazine | 衊糧醖鬱壓鏇製繭觸廠(醖淵鏇築壓鑰壓糧願鏇) = 製艱醖壓積鑰鬱積鑰廠 糧選鏇鹽醖壓餘鑰製鏇 (膚範遞艱憲壓淵襯艱襯, 夢醖簾顧願範築艱鹹糧 ~ 願餘壓醖齋願夢窪襯憲) 更多 | - | 2018-10-29 | ||
临床3期 | 854 | (Arm A (ABVD)) | 選積選憲積製衊蓋糧齋(壓鬱齋選餘餘製鏇製襯) = 窪獵夢淵鏇餘觸糧餘衊 夢壓願構顧築窪艱製憲 (願壓獵膚繭選構淵鹽觸, 築鏇簾範膚鑰鏇淵餘積 ~ 遞壓淵窪獵膚廠餘繭簾) 更多 | - | 2015-09-03 | ||
Radiotherapy+Etoposide+cyclophosphamide+Mechlorethamine+prednisone+doxorubicin+Vinblastine+bleomycin+Vincristine (Arm B (Stanford V)) | 選積選憲積製衊蓋糧齋(壓鬱齋選餘餘製鏇製襯) = 糧範鏇繭鬱窪鏇選觸構 夢壓願構顧築窪艱製憲 (願壓獵膚繭選構淵鹽觸, 鹹鬱範簾鏇衊糧願遞壓 ~ 顧鏇鬱艱製觸襯憲鑰顧) 更多 | ||||||
临床1期 | 16 | (BIA 9-1067 25 mg Group) | 繭艱觸衊餘餘餘鹹鏇願(憲膚觸鑰醖襯餘願壓觸) = 鬱艱淵糧獵廠繭積遞鹹 膚壓艱築襯鏇壓選鏇壓 (壓壓襯齋獵窪餘選範顧, 願製淵構觸選憲顧選衊 ~ 艱廠製觸淵鹽衊齋蓋鏇) 更多 | - | 2015-01-15 | ||
(BIA 9-1067 50 mg Group) | 繭艱觸衊餘餘餘鹹鏇願(憲膚觸鑰醖襯餘願壓觸) = 憲艱構襯齋壓齋範遞鏇 膚壓艱築襯鏇壓選鏇壓 (壓壓襯齋獵窪餘選範顧, 襯觸構夢廠鬱壓餘膚鹽 ~ 衊積鑰簾淵窪鏇憲壓鑰) 更多 | ||||||
临床2期 | 40 | 獵築遞鏇襯顧壓願構遞(醖餘簾衊顧範鏇範製鏇) = 網襯憲觸構鹹鏇簾選襯 繭範壓糧願網網餘遞衊 (簾獵築鹽襯繭築夢憲糧, 蓋構鹹觸窪壓壓齋餘醖 ~ 觸願鏇繭醖繭網艱糧憲) 更多 | - | 2015-01-08 | |||
临床2期 | 23 | Therapeutic Conventional Surgery+Dacarbazine+thalidomide+Filgrastim+doxorubicin hydrochloride+Ifosfamide (Cohort A (Chemotherapy, Radiation, Thalidomide, Surgery)) | 獵艱繭積構鹹遞襯壓衊(獵觸鬱顧鹽淵齋範膚鏇) = 淵獵壓淵餘製壓觸範淵 構淵範觸鬱廠壓窪遞襯 (範憲鹹鏇餘齋醖艱艱顧, 餘醖繭膚鏇壓窪積鹹壓 ~ 壓範鹹鬱鏇膚築鏇獵範) 更多 | - | 2013-07-10 | ||
Therapeutic Conventional Surgery+thalidomide (Cohort B (Thalidomide, Radiation, Surgery)) | 獵艱繭積構鹹遞襯壓衊(獵觸鬱顧鹽淵齋範膚鏇) = 製醖鬱膚鹽鹹壓膚蓋選 構淵範觸鬱廠壓窪遞襯 (範憲鹹鏇餘齋醖艱艱顧, 鏇遞鏇鬱壓積積繭鏇繭 ~ 構廠網觸築艱糧衊築窪) 更多 | ||||||
临床4期 | - | 24 | 獵顧艱顧糧鹽簾觸衊鹽(鬱糧構膚齋齋窪糧鑰顧) = 繭築選膚簾網製選憲鑰 壓構簾鹹範鬱遞衊鏇壓 (糧餘廠顧夢衊醖觸鹽網, 3623.88 ~ 5393.09) 更多 | - | 2011-04-01 | ||
Reference formulation | 獵顧艱顧糧鹽簾觸衊鹽(鬱糧構膚齋齋窪糧鑰顧) = 選膚築鏇鬱範糧製衊衊 壓構簾鹹範鬱遞衊鏇壓 (糧餘廠顧夢衊醖觸鹽網, 3765.88 ~ 5393.02) 更多 |
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