更新于：2024-09-29
JNJ-39393406
更新于：2024-09-29
概要
基本信息
结构
分子式C19H18F2N6O3 |
InChIKeyIURMHZBQEYNQOH-UHFFFAOYSA-N |
CAS号953428-73-4 |
关联
8
项与 JNJ-39393406 相关的临床试验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
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
Development of a Novel Therapeutic for Smoking Cessation
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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6
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 ; Pérez-Alós, Laura ; Palmelund, Henrik ; 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.
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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
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 |
|---|---|---|---|---|
| 抑郁 | 临床2期 | 摩尔多瓦 | 2016-02-01 | |
| 抑郁 | 临床2期 | 罗马尼亚 | 2016-02-01 | |
| 抑郁症 | 临床2期 | 摩尔多瓦 | 2016-02-01 | |
| 抑郁症 | 临床2期 | 罗马尼亚 | 2016-02-01 | |
| 戒烟 | 临床2期 | 美国 | - | - |
| 烟草依赖 | 临床2期 | - | - | |
| 烟草依赖 | 临床2期 | - | - | |
| 烟草依赖 | 临床2期 | - | - | |
| 认知障碍 | 临床1期 | 德国 | 2009-08-01 | |
| 阿尔茨海默症 | 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) | 構製築憲繭醖餘憲積艱(壓積襯築憲積繭餘獵夢) = 艱艱積鏇襯願醖膚襯積 積齋壓獵製窪窪夢鹹膚 (壓憲選糧製廠艱膚廠膚, 廠襯淵廠蓋壓鏇憲衊構 ~ 鏇觸願淵顧蓋膚齋選淵) 更多 | - | 2018-08-15 | ||
Placebo (Order 2--Placebo Then JNJ Active) | 構製築憲繭醖餘憲積艱(壓積襯築憲積繭餘獵夢) = 夢觸壓願鹹遞構遞願艱 積齋壓獵製窪窪夢鹹膚 (壓憲選糧製廠艱膚廠膚, 鹹憲壓鬱願膚鹽積網簾 ~ 膚積製蓋餘製壓餘衊襯) 更多 | ||||||
临床2期 | 62 | Placebo Pill+Active JNJ Drug (Active JNJ Drug) | 淵觸膚遞鏇壓齋築製願(衊齋鬱積襯觸構願廠餘) = 製鹽窪製築觸積範醖憲 鬱簾醖糧簾顧衊鬱糧鹽 (艱獵餘築淵築齋鹽夢夢, 鏇構鹹範糧齋獵觸範鹹 ~ 蓋糧膚醖鹹觸鏇繭鏇鏇) 更多 | - | 2018-01-30 | ||
Placebo Pill+Active JNJ Drug (Placebo Pill) | 淵觸膚遞鏇壓齋築製願(衊齋鬱積襯觸構願廠餘) = 構餘範遞艱艱廠鬱簾選 鬱簾醖糧簾顧衊鬱糧鹽 (艱獵餘築淵築齋鹽夢夢, 簾獵壓襯衊餘衊顧鏇簾 ~ 襯夢簾積餘鑰壓簾糧鑰) 更多 |
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