更新于：2024-12-25
Trifluoperazine Hydrochloride
盐酸三氟拉嗪
更新于：2024-12-25
概要
基本信息
原研机构 |
在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (1959-04-16), |
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C21H26Cl2F3N3S |
InChIKeyBXDAOUXDMHXPDI-UHFFFAOYSA-N |
CAS号440-17-5 |
关联
7
项与 盐酸三氟拉嗪 相关的临床试验Evaluation of Trifluoperazine Effectiveness in Treatment Process, Survival rate and Cure rate of COVID-19 Patients
Evaluation of the Effect of Trifluoperazin in Treatment of Patients with Confirmed 2019 Novel Coronavirus(COVID- 19): An Open-Label Randomized Clinical Trial
Prescriber Based, Active Post Marketing Surveillance Study (PMS) to Generate the Safety & Efficacy Data of Chlordiazepoxide and Trifluoperazine In the Treatment of Chronic Anxiety & Insomnia in Actual Field Conditions of Use
100 项与 盐酸三氟拉嗪 相关的临床结果
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100 项与 盐酸三氟拉嗪 相关的转化医学
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100 项与 盐酸三氟拉嗪 相关的专利（医药）
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4,292
项与 盐酸三氟拉嗪 相关的文献（医药）2025-02-01GLIA
A bottom‐up approach identifies the antipsychotic and antineoplastic trifluoperazine and the ribose derivative deoxytubercidin as novel microglial phagocytosis inhibitors
Article
作者: Sierra, Amanda ; Rodriguez‐Iglesias, Noelia ; Cañas‐Zabala, Lorena ; Zhang, Jitao David ; Gutbier, Simon ; Valero, Jorge ; Hatje, Klas ; Patsch, Christoph ; Carretero, Alejandro ; Paris, Iñaki ; Britschgi, Markus
Abstract:
Phagocytosis is an indispensable function of microglia, the brain professional phagocytes. Microglia is particularly efficient phagocytosing cells that undergo programmed cell death (apoptosis) in physiological conditions. However, mounting evidence suggests microglial phagocytosis dysfunction in multiple brain disorders. These observations prompted us to search for phagocytosis modulators (enhancers or inhibitors) with therapeutic potential. We used a bottom‐up strategy that consisted on the identification of phagocytosis modulators using phenotypic high throughput screenings (HTSs) in cell culture and validation in organotypic cultures and in vivo. We performed two complementary HTS campagnes: at Achucarro, we used primary cultures of mouse microglia and compounds of the Prestwick Chemical Library; at Roche, we used human iPSC derived macrophage‐like cells and a proprietary chemo‐genomic library with 2200 compounds with known mechanism‐of‐action. Next, we validated the more robust compounds using hippocampal organotypic cultures and identified two phagocytosis inhibitors: trifluoperazine, a dopaminergic and adrenergic antagonist used as an antipsychotic and antineoplastic; and deoxytubercidin, a ribose derivative. Finally, we tested whether these compounds were able to modulate phagocytosis of apoptotic newborn cells in the adult hippocampal neurogenic niche in vivo by administering them into the mouse hippocampus using osmotic minipumps. We confirmed that both trifluoperazine and deoxytubercidin have anti‐phagocytic activity in vivo, and validated our bottom‐up strategy to identify novel phagocytosis modulators. These results show that chemical libraries with annotated mechanism of action are an starting point for the pharmacological modulation of microglia in drug discovery projects aiming at the therapeutic manipulation of phagocytosis in brain diseases.
2024-12-01JOURNAL OF PLANT PHYSIOLOGY
Crosstalk of methylglyoxal and calcium signaling in maize (Zea mays L.) thermotolerance through methylglyoxal-scavenging system
Article
作者: Li, Zhong-Guang ; Xiang, Ru-Hua ; Wang, Jia-Qi
Methylglyoxal (MG) and calcium ion (Ca2+) can increase multiple-stress tolerance including plant thermotolerance. However, whether crosstalk of MG and Ca2+ exists in the formation of maize thermotolerance and underlying mechanism still remain elusive. In this paper, maize seedlings were irrigated with MG and calcium chloride alone or in combination, and then exposed to heat stress (HS). The results manifested that, compared with the survival percentage (SP, 45.3%) of the control seedlings, the SP of MG and Ca2+ alone or in combination was increased to 72.4%, 74.2%, and 83.4% under HS conditions, indicating that Ca2+ and MG alone or in combination could upraise seedling thermotolerance. Also, the MG-upraised SP was separately weakened to 42.2%, 40.3%, 52.1%, and 39.4% by Ca2+ chelator (ethylene glycol tetraacetic acid, EGTA), plasma membrane Ca2+ channel blocker (lanthanum chloride, LaCl3), intracellular Ca2+ channel blocker (neomycin, NEC), and calmodulin (CaM) antagonist (trifluoperazine, TFP). However, significant effect of MG scavengers N-acetylcysteine (NAC) and aminoguanidine (AG) on Ca2+-induced thermotolerance was not observed. Similarly, an endogenous Ca2+ level in seedlings was increased by exogenous MG under non-HS and HS conditions, while exogenous Ca2+ had no significant effect on endogenous MG. These data implied that Ca2+ signaling, at least partly, mediated MG-upraised thermotolerance in maize seedlings. Moreover, the activity and gene expression of glyoxalase system (glyoxalase I, glyoxalase II, and glyoxalase III) and non-glyoxalase system (MG reductase, aldehyde reductase, aldo-keto reductase, and lactate dehydrogenase) were up-regulated to a certain extent by Ca2+ and MG alone in seedlings under non-HS and HS conditions. The up-regulated MG-scavenging system by MG was enhanced by Ca2+, while impaired by EGTA, LaCl3, NEC, or TFP. These data suggest that the crosstalk of MG and Ca2+ signaling in maize thermotolerance through MG-scavenging system. These findings provided a theoretical basis for breeding climate-resilient maize crop and developing smart agriculture.
2024-12-01REPRODUCTIVE TOXICOLOGY
Trifluoperazine effect on human sperm: The accumulation of reactive oxygen species and the decrease in the mitochondrial membrane potential
Article
作者: Luo, Tao ; Zheng, Liping ; Cheng, Cheng ; Wang, Houpeng ; Ding, Jing ; Chen, Ying ; Qian, Ruirui
A strong link between antipsychotic drug use and reduced human sperm quality has been reported. Trifluoperazine (TFP), a commonly used antipsychotic, is now being explored for anticancer applications. Although there are hints that TFP might affect the male reproductive system, its impact on human sperm quality remains uncertain. Using a human sperm and TFP in vitro coculture system, we examined the effect of TFP (12.5, 25, 50 and 100 μM) on human sperm function and physiological parameters. The results showed that 50 μM and 100 μM TFP induced the accumulation of reactive oxygen species (ROS) and a decrease in the mitochondrial membrane potential (MMP) of human sperm, leading to decreased sperm viability, while 25 μM TFP inhibited only the penetration ability, total sperm motility, and progressive motility. Although 12.5 μM and 25 μM TFP increased [Ca2+]i in human sperm, they did not affect capacitation or the acrosome reaction. These results may be explained by the observation that 12.5 μM and 25 μM TFP did not increase tyrosine phosphorylation in human sperm, although TFP increased [Ca2+]i in a time-course traces similar to that of progesterone. Our results indicated that TFP could cause male reproductive toxicity by inducing the accumulation of ROS and a decrease in the MMP in human sperm.
1
项与 盐酸三氟拉嗪 相关的新闻（医药）2024-09-20
·药闻康策
100 项与 盐酸三氟拉嗪 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 |
|---|---|---|---|
| 抑郁症 | 中国 | 1995-01-01 | |
| 精神分裂症 | 中国 | 1995-01-01 | |
| 焦虑症 | 美国 | 1959-04-16 |
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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 | 2 | 鏇鬱製壓繭糧醖蓋艱壓(構衊顧鬱糧窪範築衊餘) = 獵築網繭蓋簾鏇鹹築膚 鏇範簾夢鑰壓衊鏇積鹹 (膚製廠製餘構積艱製衊, 廠鏇獵醖壓襯廠遞築鏇 ~ 壓憲蓋鏇鹽蓋餘壓願積) 更多 | - | 2022-12-14 | |||
N/A | - | - | 顧簾壓選鹹選觸淵醖積(鹽憲積蓋淵夢繭窪觸鬱) = 積鏇遞齋鬱選醖鬱簾遞 鹹製鏇艱壓簾網簾艱鬱 (憲觸廠衊顧鏇壓艱願鏇 ) | - | 2012-05-20 | ||
(Ionizing radiation) | 顧簾壓選鹹選觸淵醖積(鹽憲積蓋淵夢繭窪觸鬱) = 觸觸構淵鏇網鬱蓋範獵 鹹製鏇艱壓簾網簾艱鬱 (憲觸廠衊顧鏇壓艱願鏇 ) |
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