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更新于：2025-11-01
JNJ-39393406
更新于：2025-11-01
概要
基本信息
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结构/序列
分子式C19H18F2N6O3 |
InChIKeyIURMHZBQEYNQOH-UHFFFAOYSA-N |
CAS号953428-73-4 |
关联
7
项与 JNJ-39393406 相关的临床试验NCT02677207
The Effects of JNJ-39393406 on Psychometric Performance and Residual Depressive Symptoms in 80 Patients With Unipolar or Bipolar Depression: a Phase II Exploratory add-on Double Blind Placebo Controlled 2 Week Trial
NCT02217527
Development of a Novel Therapeutic for Smoking Cessation
NCT02230384
The Development of of A Novel Therapeutic to Aid Tobacco Smoking Cessation in Persons With Schizophrenia or Schizoaffective Disorder
100 项与 JNJ-39393406 相关的临床结果
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100 项与 JNJ-39393406 相关的转化医学
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100 项与 JNJ-39393406 相关的专利（医药）
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7
项与 JNJ-39393406 相关的文献（医药）2021-10-01European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology3区 · 医学
The effects of JNJ-39393406 a positive allosteric nicotine modulator on mood and cognition in patients with unipolar depression: A double-blind, add-on, placebo-controlled trial
3区 · 医学
Article
作者: Carla Canuso ; Linda Levi ; Igor Nastas ; Lisa Ford ; Jinyoung Park ; John M. Davis ; Michael Davidson ; Mark Weiser ; Stefanie Rassnick
Nicotinic agonists have been shown to improve cognition and mood, but this improvement is inconsistent and short-lived, possibly due to receptor desensitization. Positive Allosteric Modulators (PAMs) of the nicotinic alpha-7 nicotinic-acetyl-choline receptor (a7nAChR) are hypothesized to change the configuration of the nicotinic receptor and delay desensitization, potentially increasing the duration of the activation of the receptor, and improving clinical efficacy. This was a randomized controlled trial (RCT) adding JNJ-39393406 9 (a PAM of the a7nAChR) (n=35) or placebo (n=36) to treatment as usual for two weeks in 71 patients with unipolar depression. Mixed models for repeated measures analyses were performed Primary outcome measures were the Brief Assessment of Cognition in Schizophrenia (BACS) composite and the Montgomery-Asperg Depression Rating Scale (MADRS) scores. The drug was well tolerated, however mixed models for repeated measures comparing JNJ-39393406 to placebo showed no significant difference for MADRS total score (p=0.78), BACS composite score (p=0.34), or any of the secondary outcome measures. There was no significant difference in adverse events between the study groups (p=0.44). In conclusion, this study's findings do not support the hypothesis that a positive nicotinic receptor modulator can improve cognitive or depressive symptomatology in patients with unipolar depression.
2020-01-01International journal of pharmaceutics2区 · 医学
Comparison of induction methods for supersaturation: pH shift versus solvent shift
2区 · 医学
Article
作者: Rades, Thomas ; Müllertz, Anette ; Palmelund, Henrik ; Pérez-Alós, Laura ; Bavnhøj, Christoffer ; Plum, Jakob
In order to investigate the supersaturation propensity of drugs in a simple and small-scale setup, induction of supersaturation is often performed via solvent shift. For weak bases, a potentially more biorelevant induction method would be a pH shift, as it is often hypothesized that the induction method will impact the supersaturation and precipitation. However, this has not been investigated systematically in a pharmaceutical context. This study investigates the impact of the induction method of supersaturation for nine basic drugs, A0619, A2853, albendazole, cinnarizine, dipyridamole, intraconazole, JNJ39393406, ketoconazole, and posaconazole, on four parameters: highest apparent degree of supersaturation, induction time, precipitation rate and solid form of the precipitate, using a novel standardized small-scale supersaturation and precipitation method. For eight of the nine drugs, the same highest apparent degree of supersaturation was obtained with both induction methods. For the induction time, precipitation rate and the solid form of the precipitate, no systematic differences between the induction methods were detected, however individual drugs did show differences. The study shows that, if a drug is sufficiently soluble at low pH, the solvent shift and pH shift induction methods of supersaturation yield comparable results.
2019-12-01Stem cell research4区 · 医学
Alpha7 nicotinic acetylcholine receptors and neural network synaptic transmission in human induced pluripotent stem cell-derived neurons
4区 · 医学
ArticleOA
作者: Larsen, Hjalte M ; Hyttel, Poul ; Stummann, Tina C ; Hansen, Susanne K ; Mikkelsen, Jens D
The α7 nicotinic acetylcholine receptor has been extensively researched as a target for treatment of cognitive impairment in Alzheimer's disease and schizophrenia. Investigation of the α7 receptor is commonly performed in animals but it is critical to increase the biologically relevance of the model systems to fully capture the physiological role of the α7 receptor in humans. For example most humans, in contrast to animals, express the hybrid gene CHRFAM7A, the product of which modulates α7 receptor activity. In the present study, we used human induced pluripotent stem cell (hiPSC) derived neurons to establish a humanized α7 model. We established a cryobank of neural stem cells (NSCs) that could reproducibly be matured into neurons expressing neuronal markers and CHRNA7 and CHRFAM7A. The neurons responded to NMDA, GABA, and acetylcholine and exhibited synchronized spontaneous calcium oscillations. Gene expression studies and application of a range of α7 positive allosteric modulators (PNU-120595, TQS, JNJ-39393406 and AF58801) together with the α7 agonist PNU-282987 during measurement of intracellular calcium levels demonstrated the presence of functional α7 receptors in matured hiPSC-derived neuronal cultures. Pharmacological α7 activation also resulted in intracellular signaling as measured by ERK 1/2 phosphorylation and c-Fos protein expression. Moreover, PNU-120596 increased the frequency of the spontaneous calcium oscillations demonstrating implication of α7 receptors in human synaptic networks activity. Overall, we show that hiPSC derived neurons are an advanced in vitro model for studying human α7 receptor pharmacology and the involvement of this receptor in cellular processes as intracellular signaling and synaptic transmission.
1
项与 JNJ-39393406 相关的新闻（医药）2024-09-12
临床2期快速通道临床1期并购
100 项与 JNJ-39393406 相关的药物交易
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外链
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 重度抑郁症 | 临床2期 | 美国 | 2016-02-01 | |
| 重度抑郁症 | 临床2期 | 罗马尼亚 | 2016-02-01 | |
| 分裂情感性障碍 | 临床2期 | 美国 | 2014-09-01 | |
| 精神分裂症 | 临床2期 | 美国 | 2014-09-01 | |
| 尼古丁成瘾 | 临床2期 | 美国 | 2014-09-01 | |
| 烟草依赖 | 临床2期 | - | - | |
| 烟草依赖 | 临床2期 | - | - | |
| 烟草依赖 | 临床2期 | - | - | |
| 阿尔茨海默症 | 临床1期 | 德国 | 2009-08-01 | |
| 认知障碍 | 临床1期 | 德国 | 2009-08-01 |
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临床结果
临床结果
适应症
分期
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临床2期 | 36 | placebo (Order 1--JNJ Active Then Plac) | 願衊淵廠顧願鬱築願簾(衊繭顧願壓淵顧襯淵遞) = 餘構膚構鹽鹽顧餘衊壓 艱襯窪鏇醖蓋顧膚繭簾 (鹹製壓遞鏇醖蓋鬱襯鬱, 1.3) 更多 | - | 2018-08-15 | ||
Placebo (Order 2--Placebo Then JNJ Active) | 願衊淵廠顧願鬱築願簾(衊繭顧願壓淵顧襯淵遞) = 網鹹襯壓餘網範簾憲廠 艱襯窪鏇醖蓋顧膚繭簾 (鹹製壓遞鏇醖蓋鬱襯鬱, 0.6) 更多 | ||||||
临床2期 | 62 | Placebo Pill+Active JNJ Drug (Active JNJ Drug) | 鬱廠製願鹽鑰鏇簾糧顧(齋製夢膚選範鬱艱廠積) = 繭醖範襯膚艱繭製膚艱 糧獵憲簾願齋蓋艱餘鬱 (選齋艱願構獵鹹鏇夢壓, 0.151) 更多 | - | 2018-01-30 | ||
Placebo Pill+Active JNJ Drug (Placebo Pill) | 鬱廠製願鹽鑰鏇簾糧顧(齋製夢膚選範鬱艱廠積) = 淵夢鹽鏇鑰願築範鏇鑰 糧獵憲簾願齋蓋艱餘鬱 (選齋艱願構獵鹹鏇夢壓, 0.173) 更多 |
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