预约演示
更新于：2025-09-18
Bumetanide
布美他尼
更新于：2025-09-18
概要
基本信息
药物类型 小分子化药 |
别名 3-(aminosulfonyl)-5-(butylamino)-4-phenoxybenzoic acid、3-butylamino-4-(phenoxy)-5-sulfamoylbenzoic acid、3-butylamino-4-phenoxy-5-sulfamoyl-benzoic acid + [22] |
作用方式 抑制剂 |
作用机制 NKCC1抑制剂(溶质载体家族12成员2抑制剂)、NKCC2抑制剂(钠钾氯协同转运蛋白-2抑制剂)、SLC12A4抑制剂(solute carrier family 12 member 4 inhibitors) |
在研适应症 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 日本 (1976-04-08), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C17H20N2O5S |
InChIKeyMAEIEVLCKWDQJH-UHFFFAOYSA-N |
CAS号28395-03-1 |
关联
50
项与 布美他尼 相关的临床试验NCT06941415
Bumetanide vs. Furosemide for Adults Hospitalized With Cirrhosis: the BUFF Trial
NCT07005414
Efficacy of Bumetanide in Children With Autism Spectrum Disorder Guided by Peripheral Blood Biomarkers and Machine Learning Models: A Randomized Controlled Trial
CTR20251712
布美他尼片在健康研究参与者中的单剂量、随机、开放、交叉、两制剂、两周期餐后人体生物等效性试验
100 项与 布美他尼 相关的临床结果
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100 项与 布美他尼 相关的转化医学
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100 项与 布美他尼 相关的专利（医药）
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3,491
项与 布美他尼 相关的文献（医药）2025-11-01NEUROCHEMISTRY INTERNATIONAL
Imbalance of NKCC1/KCC2 contributes to the pathogenesis of primary focal hyperhidrosis
Article
作者: Yu, Feng-Qiang ; Lin, Nan-Long ; Zheng, Ru-Jie ; Li, Xu ; Zhang, Meng-Long ; Qiu, Rui-Qin ; Lin, Jian-Bo
BACKGROUND:
Primary focal hyperhidrosis (PFH) is characterized by excessive sweating in localized regions, significantly impacting patients' quality of life. The imbalance between sodium-potassium-chloride cotransporter 1 (NKCC1) and potassium-chloride cotransporter 2 (KCC2) disrupts chloride ion homeostasis, potentially contributing to the pathogenesis of PFH.
METHODS:
Sweat gland tissues from 76 healthy controls and 76 PFH patients were collected. Expression levels of NKCC1 and KCC2 were assessed using quantitative real-time PCR and Western blotting. Primary sweat gland cells isolated from PFH patients (PFH-SG) and controls (NPFH-SG) were subjected to NKCC1 knockdown via lentiviral shRNA transfection. A hyperhidrosis mouse model was induced by intraperitoneal injection of pilocarpine hydrochloride, and mice were pretreated with the NKCC1 inhibitor bumetanide for one week. Sweat secretion, serum acetylcholine, and chloride ion concentrations were measured. Expression levels of aquaporin 5 (AQP5), brain-derived neurotrophic factor (BDNF), and neuregulin-1 (NRG-1) proteins were analyzed.
RESULTS:
PFH tissues showed significantly elevated NKCC1 and decreased KCC2 expression compared to controls, correlating with lower sweat chloride levels. NKCC1 knockdown in PFH-SG cells reduced elevated AQP5 expression. In vivo, bumetanide treatment markedly reduced sweat secretion, lowered serum acetylcholine, and restored chloride ion concentrations in hyperhidrosis mice. Furthermore, bumetanide treatment significantly decreased expressions of BDNF and NRG-1 in sympathetic ganglia axons, indicating attenuation of sympathetic hyperactivity associated with hyperhidrosis. NKCC1/KCC2 imbalance contributes significantly to PFH pathology.
CONCLUSIONS:
Bumetanide effectively improves this imbalance, reducing excessive sweating and modulating related neurotransmitter signaling, offering potential therapeutic avenues for PFH.
2025-07-01Current drug discovery technologies
Potential Role of Benzoic Acid and its Synthetic Derivatives to Alleviate Cancer: An Up-to-Date Review
Review
作者: Singh, Mhaveer ; Kaushik, Niranjan ; Koya Kamal, Yoonus Kunju Thajuddin ; Mishra, Amrita ; Mishra, Arun K. ; Singh, Harpreet ; Kumar, Arvind
Unregulated cell division is one of the main causes of cancer. These cancerous cells negatively
impact nearby healthy cells. Cancer can occur anywhere in the body. Normal cell division
occurs when cells grow, reproduce, and divide as the body needs. As a normal cascade of cell growth
and division, when the cells get damaged, they undergo death, and normal cells develop. However,
sometimes, this process is not followed, and abnormal or damaged cells start to grow and multiply
several times more than normal. This particular process may form the basis of cancer. There is a
research gap in terms of identifying personalized synthetic anticancer therapy, which may be based
on individual patient characteristics with an aim to optimize treatment efficacy and minimize adverse
effects. While searching for new bioactive compounds, it has been observed that organic molecules
with benzoic acid (BA) moiety possess significant anticancer potential. Several works of literature
reported the use of BA from natural or synthetic sources to synthesize bioactive chemicals. It has
been observed that several natural products also contain BA moiety, and the presence of this moiety
is considered responsible for several important biological activities. Therefore, in order to chemically
synthesize a wide variety of potent biologically active compounds, benzoic acid as a basic moiety in
the form of a scaffold can be employed. Other synthetic compounds with BA scaffolds include furosemide,
tetracaine, and bumetanide. The current article aims to focus on past and present work done
on BA derivatives and to emphasize the molecular pathways involved in cancer treatment. The future
prospects for research in this area are encouraging as researchers are striving to advance synthetic
BA derivatives. This could possibly contribute to more efficient treatments and better results for cancer
patients.
2025-06-10Current Neuropharmacology
Mendelian Randomization Uncovers Potential Repurposable Medications for Neuropsychiatric Disorders
Article
作者: Li, Tingyu ; Liu, Shanling ; Gao, Linbo ; Xiao, Xiao ; Zhang, Lin ; Wang, Qiang
Background::
The growing prevalence of neuropsychiatric disorders is becoming a major
health challenge. Traditional pharmacotherapies face limitations, making drug repurposing a valuable
strategy. However, high-throughput screening approaches for these conditions are scarce.
Methods::
This study leveraged exposure data from the UK Biobank Neale Lab (N = 361,141) and
outcome data from the FinnGen database (N = approximately 410,000) to employ Mendelian Randomization
(MR) analyses and identify potential drug repurposing candidates for neuropsychiatric
disorders. Sensitivity, Linkage Disequilibrium Score Correlation (LDSC), and Bayesian Colocalization
(COLOC) analyses were conducted to ensure the robustness and reliability of our findings.
Results::
Using the IVW method, seven medications with negative causal associations with neuropsychiatric
disorders were identified. Pregabalin, bumetanide, and prednisolone were associated with
reduced anxiety (beta = -7.28, p = 4.00e-03; beta = -2.24, p = 6.00e-03; beta = -1.74, p = 2.84e-03).
Vitamin B1 preparations showed an inverse association with dementia (beta = -2.47, p = 1.51e-03),
Creon E/C granules with epilepsy (beta = -4.99, p = 3.91e-03), Pentasa SR 250 mg with multiple
sclerosis (beta = -3.95, p = 3.83e-03), and zolmitriptan with stroke excluding subarachnoid hemorrhage
(beta = -1.61, p = 6.00e-03). Sensitivity analyses confirmed these findings, whereas the LDSC
and COLOC analyses provided additional support.
Conclusion::
MR-based drug repurposing is a promising approach for the treatment of neuropsychiatric
disorders. Further validation is necessary to effectively integrate these medications into clinical
practice.
100 项与 布美他尼 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 |
|---|---|---|---|
| 心源性水肿 | 美国 | 2025-09-12 | |
| 肝腹水症 | 美国 | 2025-09-12 | |
| 由肾脏疾病引起的水肿 | 美国 | 2025-09-12 | |
| 心脏衰竭 | 加拿大 | 1993-12-31 | |
| 急性肾损伤 | 中国 | 1982-01-01 | |
| 药物中毒 | 中国 | 1982-01-01 | |
| 高钙血症 | 中国 | 1982-01-01 | |
| 高钾血症 | 中国 | 1982-01-01 | |
| 高血压 | 中国 | 1982-01-01 | |
| 低钠血症 | 中国 | 1982-01-01 | |
| 水肿 | 日本 | 1976-04-08 |
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 |
|---|---|---|---|---|
| 自闭症谱系障碍 | 临床3期 | 巴西 | 2018-09-24 | |
| 自闭症谱系障碍 | 临床3期 | 巴西 | 2018-09-24 | |
| 自闭症谱系障碍 | 临床3期 | 法国 | 2018-09-24 | |
| 自闭症谱系障碍 | 临床3期 | 法国 | 2018-09-24 | |
| 自闭症谱系障碍 | 临床3期 | 德国 | 2018-09-24 | |
| 自闭症谱系障碍 | 临床3期 | 德国 | 2018-09-24 | |
| 自闭症谱系障碍 | 临床3期 | 匈牙利 | 2018-09-24 | |
| 自闭症谱系障碍 | 临床3期 | 匈牙利 | 2018-09-24 | |
| 自闭症谱系障碍 | 临床3期 | 意大利 | 2018-09-24 | |
| 自闭症谱系障碍 | 临床3期 | 意大利 | 2018-09-24 |
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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3期 | 211 | (BUMETANIDE (S95008) Followed by Open-Label S95008) | 鹽膚膚製膚齋壓憲範觸 = 鏇獵構淵鏇鬱淵觸鬱製 衊簾築鑰糧鬱鹹膚廠壓 (鏇積構憲簾繭願鏇憲範, 壓鑰糧鑰構範鹽鏇獵鏇 ~ 鬱範鬱構糧鏇選餘壓鏇) 更多 | - | 2023-06-05 | ||
PLACEBO for week 0 - 26+S95008 (PLACEBO Followed by Open-Label S95008) | 鹽膚膚製膚齋壓憲範觸 = 壓鏇糧憲獵鬱簾襯範築 衊簾築鑰糧鬱鹹膚廠壓 (鏇積構憲簾繭願鏇憲範, 積憲淵鏇網淵築夢鬱夢 ~ 遞觸廠願憲艱憲製製蓋) 更多 | ||||||
临床2期 | 34 | 遞蓋積艱簾鏇獵憲餘膚(膚淵築製壓廠簾鬱獵範) = 艱淵願夢鏇窪艱網襯製 鬱襯鏇繭艱鹹夢積壓積 (積築淵齋鏇糧獵淵獵遞 ) 更多 | - | 2022-09-20 | |||
Bumetanide plus placebo | 遞蓋積艱簾鏇獵憲餘膚(膚淵築製壓廠簾鬱獵範) = 蓋願構網鬱簾顧膚壓觸 鬱襯鏇繭艱鹹夢積壓積 (積築淵齋鏇糧獵淵獵遞 ) 更多 | ||||||
临床2期 | 34 | (Placebo) | 蓋衊網鬱艱夢糧選繭壓(膚鏇獵襯餘鏇構壓襯廠) = 構鬱願艱鏇襯願遞餘憲 鏇顧簾襯糧齋願構衊選 (蓋鏇積鑰醖糧憲淵選繭, 1.78) 更多 | - | 2020-03-10 | ||
(Treatment Grup) | 蓋衊網鬱艱夢糧選繭壓(膚鏇獵襯餘鏇構壓襯廠) = 餘獵餘鹹願糧繭壓齋觸 鏇顧簾襯糧齋願構衊選 (蓋鏇積鑰醖糧憲淵選繭, 3.29) 更多 |
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