更新于：2024-12-06
Bevantolol Hydrochloride
盐酸贝凡洛尔
更新于：2024-12-06
概要
基本信息
药物类型 小分子化药 |
别名 (±)-bevantolol、1-((2-(3,4-dimethoxyphenyl)ethyl)amino)-3-(3-methylphenoxy)-2-propanol、1-(3,4-dimethoxyphenethylamino)-3-(m-tolyloxy)-2-propanol + [17] |
作用机制 ADRA1拮抗剂(肾上腺素能受体α-1家族拮抗剂)、Cav2.2阻滞剂(N-型电压门控性钙通道α-1B亚基阻滞剂)、VMAT2抑制剂(突触囊泡单胺转运体抑制剂) |
非在研适应症- |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (1995-03-31), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构
分子式C20H28ClNO4 |
InChIKeyFJTKCFSPYUMXJB-UHFFFAOYSA-N |
CAS号42864-78-8 |
关联
2
项与 盐酸贝凡洛尔 相关的临床试验Phase IIb, Randomized, Double-blind, Placebo-controlled Study in Parallel Groups Assessing the Efficacy and Safety of Two Doses of SOM3355 in Patients Suffering From Huntington's Disease With Choreic Movements
Phase IIa, Double-blind, Randomized, Placebo-controlled Study of the Efficacy and Safety of SOM3355 in Huntington's Disease (HD) Patients With Chorea Movements.
100 项与 盐酸贝凡洛尔 相关的临床结果
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100 项与 盐酸贝凡洛尔 相关的转化医学
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100 项与 盐酸贝凡洛尔 相关的专利（医药）
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243
项与 盐酸贝凡洛尔 相关的文献（医药）2024-09-01Asian Pacific journal of cancer prevention : APJCP
In-vivo Toxicity Evaluation of 3-(2-(3,4 dimethoxyphenyl)-2 oxoethylidene) Indolin-2-one (RAJI) in Zebrafish and Mice Model
Article
作者: Pandurangan, Ashok Kumar ; Sivaprakasam, Prathibha ; Chandrabose, Karthikeyan
OBJECTIVE:
Breast cancer is a global health concern, with millions of cases reported annually worldwide, making it the most common cancer among women. In India, the incidence of breast cancer has been steadily rising, reflecting a growing public health challenge and hence in the development of new drug moieties. Toxicity analysis of such novel drug candidates play a critical role in drug development, ensuring the safety and efficacy of potential therapeutics. Animal models, especially mice and zebrafish in the recent days, have been extensively used for toxicity evaluation owing to their physiological and genetic similarities to humans. This study was hence conducted with an aim to assess the toxicity using animal models, particularly mice and zebrafish.
METHODS:
In this study, 3-(2-(3,4-dimethoxyphenyl)-2-oxoethylidene)indolin-2-one (RAJI) - a chemically synthesised novel drug, was assessed for its toxicological potential in both zebrafish and mice models highlighting its survival, hatching, locomotor, neuromotor, behavioural abnormalities in zebrafish model and haematological and biochemical abnormalities in mice model.
RESULTS:
The results obtained emphasise that no significant damages were seen in both zebrafish (survival, hatching, locomotor, neuromotor, behavioural abnormalities) and mice (body weight, haematological and biochemical abnormalities) models when administered in low doses.
CONCLUSION:
All results obtained signifies that RAJI poses no harmful effects in the model organisms until administered in higher concentrations, thereby emphasising the fact that RAJI is a safe drug.
2023-01-01Anti-cancer agents in medicinal chemistry
Design, Synthesis, Docking Studies, Enzyme Inhibitory and Antiplatelet Aggregation Activities of New 1,3-Diphenyl-3-(Phenylthio)Propan-1-One Derivatives as Selective COX-2 Inhibitors
Article
作者: Bayanati, Maryam ; Daraei, Bahram ; Zarghi, Afshin
Background::
Cancer is the second leading cause of death worldwide after heart disease. A vast number of studies indicated that selective cyclooxygenase-2 (COX-2) inhibitors could be chemopreventive against different types of cancer because the expression of COX-2 is increased. Therefore, to develop new therapeutics for cancer, the design and synthesis of new COX-2 inhibitors with few side effects seem attractive as anti-cancer agents.
Objective::
Some of the well-known drugs that have been widely used for some time have been removed from the market due to the cardiac side effects they cause, so there is a need to introduce a scaffold that can inhibit COX-2 with high potency and low side effects. This study aimed to introduce a new COX-2 inhibitor structure.
Methods::
A new series of β-aryl-β-mercapto ketones possessing a methylsulfonyl pharmacophore was synthesized and evaluated as selective COX-2 inhibitors. In-vitro COX-1 and COX-2 inhibition effects of these compounds were evaluated, and molecular modeling was examined. Also, the antiplatelet aggregation activity of the synthesized compounds was tested.
Results::
In-vitro COX-1 and COX-2 inhibition assays indicated that almost all newly synthesized compounds showed selectivity for COX-2 with IC50 values in the 0.07-0.22 μM range and COX-2 selectivity indexes in the 170 to 703.7 range. Among the tested compounds 1-(4-(methylsulfonyl)phenyl)-3-phenyl-3-(phenylthio)propan-1-one (4a), 3-(3,4- dimethoxyphenyl)-1-(4-(methylsulfonyl)phenyl)-3-(phenylthio)propan-1-one (4g) and 3-(4-fluorophenyl)-1-(4-(methyl sulfonyl)phenyl)-3-(phenylthio)propan-1-one (4h) were the most potent COX-2 inhibitors and 3-(3,4- dimethoxyphenyl)-1-(4-(methylsulfonyl)phenyl)-3-(phenylthio)propan-1-one had the highest selectivity index for COX-2 enzyme inhibitory activity. The Anti-platelet aggregation activity results indicated that the compound 1-(4- (methylsulfonyl)phenyl)-3-(phenylthio)-3-(p-tolyl)propan-1-one (4b) possesses the strong anti-platelet activity. Our molecular modeling studies also indicated that the methylsulfonyl pharmacophore group is placed into the adjunct pocket in the COX-2 active site and forms hydrogen bond interactions with NH of Arg513 and NH of His90.
Conclusion::
In brief, all designed and synthesized compounds showed moderate to good COX-2 inhibitory effects and showed good anti-platelet activity. Therefore, these compounds have the potential for further research into developing anti-cancer agents.
2022-12-25Sheng li xue bao : [Acta physiologica Sinica]
[β-arrestin2 recruitment by β-adrenergic receptor agonists and antagonists].
Article
作者: Ma, Lan ; Liu, Xing ; Wang, Yi-Ran ; Cheng, De-Qin
A large number of β-adrenergic receptor (β-AR) agonists and antagonists are widely used in the treatment of cardiovascular diseases and other diseases. Nonetheless, it remains unclear whether these commonly used β-AR drugs can activate downstream β- arrestin-biased signaling pathways. The objective of this study was to investigate β-arrestin2 recruitment effects of β-AR agonists and antagonists that were commonly used in clinical practice. We used TANGO (transcriptional activation following arrestin translocation) assay to detect the β-arrestin2 recruitment by β-AR ligands in HEK293 cell line (HTLA cells) stably transfected with tetracycline transactivator protein (tTA) dependent luciferase reporter and β-arrestin2-TEV fusion gene. Upon activation of β-AR by a β-AR ligand, β-arrestin2 was recruited to the C terminus of the receptor, followed by cleavage of the G protein-coupled receptors (GPCRs) fusion protein at the TEV protease-cleavage site. The cleavage resulted in the release of tTA, which, after being transported to the nucleus, activated transcription of the luciferase reporter gene. The results showed that β-AR non-selective agonists epinephrine, noradrenaline and isoprenaline all promoted β-arrestin2 recruitment at β1-AR and β2-AR. β1-AR selective agonists dobutamine and denopamine both promoted β-arrestin2 recruitment at β1-AR. β2-AR selective agonists procaterol and salbutamol promoted β-arrestin2 recruitment at β2-AR. β-AR non-selective antagonists alprenolol and pindolol promoted β-arrestin2 recruitment at β1-AR. β1-AR selective antagonists celiprolol and bevantolol showed β-arrestin2 recruitment at β1-AR. β2-AR selective antagonists butoxamine showed β-arrestin2 recruitment at β1-AR. These results provide some clues for the potential action of β-AR drugs, and lay a foundation for the screening of β-arrestin-biased β-AR ligands.
1
项与 盐酸贝凡洛尔 相关的新闻（医药）2024-09-20
·药闻康策
100 项与 盐酸贝凡洛尔 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 |
|---|---|---|---|
| 心绞痛 | 中国 | 2002-12-11 | |
| 高血压 | 日本 | 1995-03-31 |
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 |
|---|---|---|---|---|
| 亨廷顿舞蹈病 | 临床2期 | 西班牙 | 2018-08-08 |
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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2期 | 32 | 繭願繭鏇鬱製遞鑰蓋鏇(鹽齋鹽築構壓壓簾襯廠) = The most frequent adverse events during SOM3355 administration were mild to moderate 製餘壓壓壓製鹽簾積獵 (網齋鹹餘積簾膚糧積鹽 ) | - | 2022-12-09 | |||
临床2期 | 32 | 壓積醖壓製齋鏇壓鬱簾(築鹹鏇積製淵積齋築遞) = 構糧遞齋齋餘觸網鏇窪 範鬱構簾糧糧範鹹壓遞 (顧鹽窪糧醖鹹壓夢網憲 ) | 积极 | 2021-10-04 | |||
Placebo | - |
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