预约演示
更新于：2026-02-26
Flavoxate Hydrochloride
盐酸黄酮哌酯
更新于：2026-02-26
概要
基本信息
药物类型 小分子化药 |
别名 2-(1-piperidinyl)ethyl 3-methyl-4-oxo-2-phenyl-4H-chromene-8-carboxylate、2-piperidinoethyl 3-methyl-4-oxo-2-phenyl-4H-1-benzopyran-8-carboxylate、2-piperidinoethyl 3-methylflavone-8-carboxylate + [20] |
靶点 |
作用方式 抑制剂 |
作用机制 ORAI1抑制剂(钙离子释放激活钙通道蛋白-1抑制剂) |
治疗领域 |
权益机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
登录后查看时间轴
结构/序列
分子式C24H26ClNO4 |
InChIKeyXOEVKNFZUQEERE-UHFFFAOYSA-N |
CAS号3717-88-2 |
关联
5
项与 盐酸黄酮哌酯 相关的临床试验CTRI/2024/09/073950
Effect of oral flavoxate on postoperative catheter related bladder dysfunction in adult males undergoing transurethral resection of bladder tumors- A randomized controlled trial vs solifenacin and placebo - Nil
CTRI/2020/04/024700
Single dose oral bioavailability pilot study of two test formulations ofFlavoxate XR Tablet 600 mg, once a day (T1) and Flavoxate XR Tablet800 mg, once a day (T2) and reference formulation of Flavoxate Tablet200 mg, thrice a day (R) in healthy adult male subjects under fastingconditions.
JPRN-UMIN000009999
Clinical evaluation of add-on administration of flavoxate hydrochloride in nocturia patients resistant to an anticholinergic agent - Clinical evaluation of add-on administration of flavoxate hydrochloride in nocturia patients
100 项与 盐酸黄酮哌酯 相关的临床结果
登录后查看更多信息
100 项与 盐酸黄酮哌酯 相关的转化医学
登录后查看更多信息
100 项与 盐酸黄酮哌酯 相关的专利（医药）
登录后查看更多信息
264
项与 盐酸黄酮哌酯 相关的文献（医药）2026-01-01KOREAN JOURNAL OF PHYSIOLOGY & PHARMACOLOGY
Exploring the selective inhibitory effects of Flavoxate and its analogues on two chloride channels and neuronal action potentials
Article
作者: Zhang, Xuan ; Zhang, Yuanyuan ; Liu, Junjiang ; Zhou, Anmin ; Zhang, Gaohua ; Cui, Yan ; Zhao, Yingtong ; Wang, Jiping ; Yang, Jixia ; Li, Honglin ; Song, Yaxin ; Li, Yunxia
Volume-regulated anion channels (VRACs) and TMEM16A calciumactivated chloride channels (CaCCs) are distinct but share some features and can co-immunoprecipitate. Currently, there are no specific inhibitors for these channels exist. Our prior research showed Flavoxate inhibits VRAC currents in HEK293 cells under hypotonic conditions. MFCA (3-methylflavone-8-carboxylic acid, a primary active metabolite of Flavoxate) and 3-methylflavone are two structural analogues of Flavoxate. To further elucidate the specific inhibitory effects of the three flavonoids on VRACs and TMEM16A/CaCCs, the current study used patch-clamp techniques to explore their effects on the two chloride channels. Additionally, we investigated the effects of the three flavonoids on action potential (AP) firing in small dorsal root ganglion (DRG) neurons utilizing the current-clamp technique. Our findings indicate that the inhibition rates of 30 μM Flavoxate, MFCA, and 3-methylflavone on VRAC currents approximately were 78%, 46%, and 35%, with corresponding half-maximal concentration (IC50) values of 1.8 μM, 18.5 μM, and 37.2 μM, respectively. In contrast, the inhibition rates of these compounds on TMEM16A/CaCC currents approximately were 14%, 15%, and 24%, with IC50 values of 32.8 μM, 28.3 μM, and 26.5 μM, respectively. These results suggest that Flavoxate is highly efficient and selective for VRAC inhibition, with the 8-substituent on its flavonoid core being crucial for this selectivity. All three flavonoids strongly inhibit AP firing, indicating that their core structure contributes to analgesic effects. In summary, Flavoxate is a selective VRAC inhibitor and a potential neuropathic pain inhibitor by suppressing AP firing in small DRG neurons.
2025-11-27CHEMICAL RECORD
Harnessing Chromone as a Versatile Scaffold for Emerging Biological Applications: Recent Advances and Medicinal Insights
Review
作者: Dutta, Debashis ; Gogoi, Neelutpal ; Kaishap, Partha Pratim ; Laskar, Boonam ; Dey, Tapan
Chromones, characterized by a benzo‐annulated
γ
‐pyrone core, represent a privileged scaffold, offering a diverse pharmacological spectrum. Clinically approved drugs such as disodium cromoglycate and flavoxate underscore their therapeutic significance. Recent advancements in synthetic strategies have facilitated the development of novel chromone derivatives with improved bioactivity, selectively modulating key molecular targets implicated in cancer, inflammation, diabetes, infectious diseases, and neurodegenerative disorders. Furthermore, their emerging utility as imaging probes and regulators of pharmacologically relevant targets, such as pyridoxal phosphatase (PDXP), highlights their expanding role in modern drug discovery. This review provides a comprehensive overview of recent progress in the identification of bioactive chromone‐based natural products and synthetic analogs, emphasizing their therapeutic potential. Additionally, critical innovations in recent synthetic methodologies and targeted therapeutic applications are discussed, reinforcing chromones as a sustainable and multifunctional framework for next‐generation drug development.
2025-10-28BIOLOGICAL & PHARMACEUTICAL BULLETIN
Evaluation of the Potential Inhibitory Effects of Medications for Detrusor Overactivity on Platelet-Activating Factor (PAF)-Induced Mechanical Activity in Guinea Pig Bladder Smooth Muscle
Article
This study aimed to determine whether currently available medications for detrusor overactivity (DO) can inhibit the platelet-activating factor (PAF)-induced increase in the mechanical activity of the urinary bladder smooth muscle (UBSM) in guinea pigs. Ten clinically used DO drugs-oxybutynin, tolterodine, fesoterodine, propiverine, propantheline, solifenacin, imidafenacin, flavoxate, urapidil, and clenbuterol-were tested at a concentration of 10 μM, exceeding typical therapeutic plasma levels. Among these, oxybutynin exerted the most pronounced inhibitory effect, reducing the PAF (1 μM)-induced increase in basal tone by approximately 60%. Furthermore, oxybutynin (10 μM) also decreased 60 mM KCl-induced contractions by a similar extent and nearly abolished acetylcholine (ACh, 10 μM)-induced contractions. These findings suggest that oxybutynin suppresses PAF-induced UBSM hyperactivity through a mechanism distinct from its anticholinergic effect, likely mediated by blockade of voltage-dependent Ca2+ channels (VDCCs).
1
项与 盐酸黄酮哌酯 相关的新闻（医药）
100 项与 盐酸黄酮哌酯 相关的药物交易
登录后查看更多信息
研发状态
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 |
|---|---|---|---|
| 尿道疾病 | 中国 | 1995-01-01 | |
| 慢性前列腺炎 | 日本 | 1978-08-01 | |
| 膀胱炎 | 日本 | 1978-08-01 | |
| 尿频 | 日本 | 1978-08-01 | |
| 排尿困难 | 美国 | 1970-01-15 | |
| 疼痛 | 美国 | 1970-01-15 | |
| 膀胱过度活动症 | 美国 | 1970-01-15 | |
| 尿失禁 | 美国 | 1970-01-15 | |
| 急迫性尿失禁 | 美国 | 1970-01-15 |
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
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
生物医药百科问答
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
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