更新于：2024-12-25
Fluphenazine Decanoate
癸氟奋乃静
更新于：2024-12-25
概要
基本信息
药物类型 小分子化药 |
别名 1-(2-hydroxyethyl)-4-(3-(trifluoromethyl-10-phenothiazinyl)propyl)-piperazine、10-(3'-(4''-(β-hydroxyethyl)-1''-piperazinyl)-propyl)-3-trifluoromethylphenothiazine、10-(3-(2-hydroxyethyl)piperazinopropyl)-2-(trifluoromethyl)phenothiazine + [19] |
作用机制 D2 receptor拮抗剂(多巴胺D2受体拮抗剂) |
治疗领域 |
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 美国 (1972-06-20) |
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C32H44F3N3O2S |
InChIKeyVIQCGTZFEYDQMR-UHFFFAOYSA-N |
CAS号5002-47-1 |
关联
9
项与 癸氟奋乃静 相关的临床试验A 12-Month Randomized, Open-Label Study of Caregiver Psycho-education and Skills Training in Patients Recently Diagnosed With Schizophrenia, Schizoaffective Disorder, or Schizophreniform Disorder and Receiving Paliperidone Palmitate or Oral Antipsychotic Treatment
Evaluation of the Necessity of Long-term Pharmacological Treatment With Antipsychotics for the Prevention of Relapse in Long-term Stabilized Schizophrenic Patients: a Randomized, Single-blind, Longitudinal Trial
Pharmacovigilance in Gerontopsychiatric Patients
100 项与 癸氟奋乃静 相关的临床结果
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100 项与 癸氟奋乃静 相关的转化医学
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100 项与 癸氟奋乃静 相关的专利（医药）
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1,869
项与 癸氟奋乃静 相关的文献（医药）2023-12-04Molecular pharmaceutics
Bile Is a Selective Elevator for Mucosal Mechanics and Transport
Article
作者: Schubert, Ulrich S ; Schlauersbach, Jonas ; Choudhury, Susobhan ; Endres, Sebastian ; Pöppler, Ann-Christin ; Möllmert, Stephanie ; Möckel, Conrad ; Meinel, Lorenz ; Heinze, Katrin G ; Scherf-Clavel, Oliver ; Hanio, Simon ; Zorn, Theresa ; Höpfel, Andreas I ; Scheller, Lena ; Guck, Jochen ; Bellstedt, Peter ; Keßler, Christoph
Mucus mechanically protects the intestinal epithelium and impacts the absorption of drugs, with a largely unknown role for bile. We explored the impacts of bile on mucosal biomechanics and drug transport within mucus. Bile diffused with square-root-of-time kinetics and interplayed with mucus, leading to transient stiffening captured in Brillouin images and a concentration-dependent change from subdiffusive to Brownian-like diffusion kinetics within the mucus demonstrated by differential dynamic microscopy. Bile-interacting drugs, Fluphenazine and Perphenazine, diffused faster through mucus in the presence of bile, while Metoprolol, a drug with no bile interaction, displayed consistent diffusion. Our findings were corroborated by rat studies, where co-dosing of a bile acid sequestrant substantially reduced the bioavailability of Perphenazine but not Metoprolol. We clustered over 50 drugs based on their interactions with bile and mucin. Drugs that interacted with bile also interacted with mucin but not vice versa. This study detailed the dynamics of mucus biomechanics under bile exposure and linked the ability of a drug to interact with bile to its abbility to interact with mucus.
2023-07-03Journal of biomolecular structure & dynamics
DFT and MD investigations of the biomolecules of phenothiazine derivatives: interactions with gold and water molecules and investigations in search of effective drug for SARS-CoV-2
Article
作者: Yadav, Rohitash ; Mary, Y. Sheena ; Mary, Shyma ; Al-Otaibi, Jamelah S. ; Trivedi, Ravi ; Chakraborty, Brahmananda ; Soman, Sreejit ; Celik, Ismail
Theoretical analyses of two phenothiazine derivatives, 10-[3-(dimethylamino)-2-methylpropyl]phenothiazine-2-carbonitrile (CYM) and 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol (PAZ) are reported using density functional theory (DFT) and molecular dynamics (MD) simulations. Spectroscopic studies, different electronic and chemical parameters are predicted. Red and yellow in electrostatic potential plot is in rings and oxygen atom in PAZ and C≡N and rings in CYM are sensitive to nucleophilic attacks. The blue in hydrogen atoms refer to electrophilic attack in both PAZ and CYM. Stability of the protein-ligand complex formed with these derivatives and angiotensin-converting enzyme 2 (ACE2) was investigated using MD simulation. Radius of gyration of C-alpha atom of 6VW1 displayed the conformational convergence toward a compact structure leading to stable 6VW1-ligand complex which are also in agreement with root mean square fluctuation (RMSF) values. Localized area predicts reactive sites for Au and H2O molecules interaction with these compounds for further practical applications. Charge density is localized on both molecules and also tries to move toward Au-Au dimer and water molecule and such they are expected to contribute to the sensing performance.Communicated by Ramaswamy H. Sarma.
2023-05-25Pharmaceuticals (Basel, Switzerland)
Innate Vascular Failure by Application of Neuroleptics, Amphetamine, and Domperidone Rapidly Induced Severe Occlusion/Occlusion-like Syndromes in Rats and Stable Gastric Pentadecapeptide BPC 157 as Therapy.
Article
作者: Smoday, Ivan Maria ; Brkic, Filip ; Boban Blagaic, Alenka ; Tepes, Marijan ; Vukovic, Vlasta ; Krezic, Ivan ; Kalogjera, Luka ; Drinkovic, Martin ; Popic, Jelena ; Staresinic, Mario ; Sikiric, Suncana ; Gojkovic, Slaven ; Strbe, Sanja ; Seiwerth, Sven ; Zizek, Helena ; Skrtic, Anita ; Sikiric, Predrag ; Barisic, Ivan ; Oroz, Katarina ; Vranes, Hrvoje ; Beketic Oreskovic, Lidija
Even before behavioral disturbances, neuroleptics, amphetamine, and domperidone application rapidly emerged severe occlusion/occlusion-like syndrome, shared innate vascular and multiorgan failure in rats, comparable to occlusion/occlusion-like syndrome described with vessel(s) occlusion or similar noxious procedures application. As therapy, i.e., activation of the collateral pathways, "bypassing key" (activated azygos vein pathway, direct blood flow delivery), the stable gastric pentadecapeptide BPC 157 is a novel solution. Recently, BPC 157 therapy particularly counteracted neuroleptic- or L-NAME-induced catalepsy, lithium intoxication, and schizophrenia positive and negative symptoms (amphetamine/methamphetamine/apomorphine/ketamine). In rats with complete calvariectomy, medication (BPC 157 10 µg/kg, 10 ng/kg ip or ig) was given 5 min after distinctive dopamine agents (mg/kg ip) (haloperidol (5), fluphenazine (5), clozapine (10), risperidone (5), olanzapine (10), quetiapine (10), or aripiprazole (10), domperidone (25), amphetamine (10), and combined amphetamine and haloperidol) and assessed at 15 min thereafter. All neuroleptic-, domperidone-, and amphetamine-induced comparable vascular and multiorgan failure severe syndrome was alleviated with BPC 157 therapy as before major vessel(s) occlusion or other similar noxious procedures. Specifically, all severe lesions in the brain (i.e., immediate swelling, hemorrhage), heart (i.e., congestion, arrhythmias), and lung (i.e., congestion, hemorrhage), as well as congestion in the liver, kidney, and gastrointestinal (stomach) tract, were resolved. Intracranial (superior sagittal sinus), portal, and caval hypertension and aortal hypotension were attenuated or eliminated. BPC 157 therapy almost annihilated arterial and venous thrombosis, peripherally and centrally. Thus, rapidly acting Virchow triad circumstances that occur as dopamine central/peripheral antagonists and agonist essential class-points, fully reversed by BPC 157 therapy, might be overwhelming for both neuroleptics and amphetamine.
100 项与 癸氟奋乃静 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 |
|---|---|---|---|
| 精神分裂症 | 日本 | 1993-01-19 |
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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 | 60 | (Haloperidol - Pathological Gamblers) | 糧觸簾壓餘衊窪製蓋鏇(淵鹹選淵願願築糧繭膚) = 鹽醖鬱顧鬱廠簾醖觸憲 鹽遞衊願鹹膚願衊膚醖 (範範壓簾鑰遞壓夢鬱觸, 鹽鹹願蓋獵鑰膚構窪糧 ~ 膚鏇憲夢淵襯憲繭鬱觸) 更多 | - | 2016-04-25 | ||
(Fluphenazine - Pathological Gamblers) | 糧觸簾壓餘衊窪製蓋鏇(淵鹹選淵願願築糧繭膚) = 鑰簾繭窪鹽蓋積積膚餘 鹽遞衊願鹹膚願衊膚醖 (範範壓簾鑰遞壓夢鬱觸, 醖襯鏇獵積衊鏇觸糧網 ~ 襯築鹽糧鹹簾鹽衊淵衊) 更多 | ||||||
临床2期 | 10 | (Cohort 1, 10 ug/ml Fluphenazine Treated Lesion) | 鏇醖壓艱獵願網鏇獵襯(鑰簾築鬱繭夢範觸艱範) = 鑰積鏇遞鏇鏇範餘襯鹹 壓遞繭夢鹽壓齋艱淵齋 (淵選範夢窪淵襯鹽齋淵, 遞壓繭壓選艱願醖獵餘 ~ 憲鹽淵鏇壓構廠壓顧獵) 更多 | - | 2010-12-22 | ||
Placebo (Cohort 1, Placebo Treated Lesion) | 鏇醖壓艱獵願網鏇獵襯(鑰簾築鬱繭夢範觸艱範) = 遞積簾齋鹹築憲膚廠窪 壓遞繭夢鹽壓齋艱淵齋 (淵選範夢窪淵襯鹽齋淵, 製憲醖鏇齋膚窪製餘製 ~ 鹽鏇願鹽襯夢憲鏇餘醖) 更多 | ||||||
N/A | 27 | 鏇齋鏇餘鏇壓願鹽齋齋(鹹獵觸鬱製衊衊衊觸醖) = improved significantly for quetiapine as compared to fluphenazine and risperidone 鹹製淵淵膚淵廠顧餘製 (憲艱獵鹽襯齋繭壓鬱淵 ) 更多 | - | 2006-04-01 | |||
N/A | - | - | 積鹹糧鹹範遞齋獵鹽遞(糧齋築願網顧選襯艱壓) = 憲衊遞廠餘築窪襯鏇鹽 網網繭繭餘襯願鏇糧網 (夢壓獵繭餘齋選齋衊範 ) | - | 2003-11-08 |
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