Delving into the Latest Updates on Acenta Discovery, Inc. with Synapse

概览

疾病领域	数量

神经系统疾病	1

排名前五的药物类型	数量

小分子化药	2

排名前五的靶点	数量

nAChRα4&β2(神经性乙酰胆碱受体蛋白α4/β2复合体)	1
Monoamine transporter subfamily	1

关联

2

项与 Acenta Discovery, Inc. 相关的药物

nAChRα4&β2 agonists(Acenta Discovery, Inc.)

靶点

nAChRα4&β2

作用机制

nAChRα4&β2激动剂

在研机构

Acenta Discovery, Inc.

原研机构

Acenta Discovery, Inc.

在研适应症

戒烟

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期-

Nocaine/modafinil hybrid ligands(Acenta Discovery, Inc.)

靶点

Monoamine transporter subfamily

作用机制

Monoamine transporter subfamily inhibitors

在研机构

Acenta Discovery, Inc.

原研机构

Acenta Discovery, Inc.

在研适应症

抑郁症 [+1]

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期-

100 项与 Acenta Discovery, Inc. 相关的临床结果

登录后查看更多信息

0 项与 Acenta Discovery, Inc. 相关的专利（医药）

登录后查看更多信息

2

项与 Acenta Discovery, Inc. 相关的文献（医药）

Drugs of the Future4区 · 医学

Norepinephine transporter inhibitors and their therapeutic potential

4区 · 医学

Article

作者: Zhou, Jia

The norepinephrine transporter (NET) is located in the plasma membrane of noradrenergic neurons, where it functions to take up synaptically released norepinephrine (NE). The NET thus serves as the primary mechanism for the inactivation of noradrenergic signaling. Some potent and selective or mixed NET inhibitors (e.g., reboxetine and atomoxetine) have been successfully developed to treat a variety of mental disorders such as depression and attention deficit hyperactivity disorder (ADHD). However, to date, only a very limited number of NET-selective inhibitors are available. New potent and selective NET inhibitors may find application in the treatment of mental disorders or in PET imaging, and may enhance our basic understanding of these illnesses. In the present review, both previously reported and newly designed NET inhibitors, as well as their therapeutic and imaging potential, will be discussed. Two types of molecules, the conformationally constrained tropanes and the piperidine-based nocaine/modafinil hybrid ligands, represent new leads and provide good opportunities for discovering novel potent and selective NET inhibitors that are useful as therapies and imaging agents for the NET.

Development of nocaine/modafinil hybrid monoamine transporter inhibitors as superior antidepressants: From compound library establishment to in vivo evaluation

作者: McGonigle, Paul ; Johnson, Kenneth M. ; Giberson, Kelly M. ; Zhou, Jia ; Caldarone, Barbara J. ; Kozikowski, Alan P.

A compound library of piperidine-based nocaine/modafinil hybrid ligands has been established by rational design, synthesis and pharmacol. investigation in pursuit of the next generation of antidepressants with fewer side effects but faster onset of action.Inhibition data of reuptake at monoamine transporters (DAT, SERT, and NET) demonstrate that some of these compounds display high potency with a single, dual or triple selectivity "spectrum".The in vivo data indicate that some of them are more active in tail suspension tests than desipramine.Based upon Lipinski′s "rule of five" and positron emission tomog. (PET) imaging studies, this class of compounds has drug-like phys. properties with a suitable capability to penetrate the blood-brain barrier.Furthermore, these compounds display only weak or even extremely weak muscarinic receptor binding affinity, indicating that as potential antidepressants, they may overcome certain side effects that are of concern with other antidepressants, which are thought to be mediated by their anticholinergic properties.A systematic in vivo assessment of the therapeutic potential of selected compounds from this library and a comparison of the activity of the most promising compounds in a battery of behavioral models are being carried out using the proprietary SmartCubeTM technol. to identify the best drug candidate(s) for advancement to pre-development characterization in preparation for an IND submission.

100 项与 Acenta Discovery, Inc. 相关的药物交易

登录后查看更多信息

100 项与 Acenta Discovery, Inc. 相关的转化医学

登录后查看更多信息

组织架构

使用我们的机构树数据加速您的研究。

登录

或

查看完整样例数据

管线布局

2024年11月16日管线快照

管线布局中药物为当前组织机构及其子机构作为药物机构进行统计，早期临床1期并入临床1期，临床1/2期并入临床2期，临床2/3期并入临床3期

临床前

2

登录后查看更多信息

当前项目

药物(靶点)	适应症	全球最高研发状态

nAChRα4&β2 agonists(Acenta Discovery, Inc.) ( nAChRα4&β2 )	戒烟更多	临床前
Nocaine/modafinil hybrid ligands(Acenta Discovery, Inc.) ( Monoamine transporter subfamily )	抑郁症更多	临床前