Pozanicline Hydrochloride(Pozanicline Hydrochloride) - 药物靶点：CHRNA7 x nAChR α4/β2/α5 x nAChRα3&β4_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Pozanicline、Pozanicline Tartrate

+ [2]

靶点

CHRNA7 x nAChR α4/β2/α5 x nAChRα3&β4

作用方式

激动剂、拮抗剂

作用机制

nAChR α4/β2/α5激动剂(烟碱性胆碱能受体α4/β2/α5复合体激动剂)、α3β4 receptor拮抗剂(神经性乙酰胆碱受体蛋白α3/β4复合体拮抗剂)、α7 receptor激动剂(神经性乙酰胆碱受体蛋白α-7亚基激动剂)

治疗领域

神经系统疾病其他疾病

在研适应症-

非在研适应症

阿尔茨海默症注意缺陷障碍伴多动

原研机构

AbbVie, Inc.

在研机构-

非在研机构

Abbott Laboratories

AbbVie, Inc.

权益机构-

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C11H16N2O

InChIKeyYRVIKLBSVVNSHF-JTQLQIEISA-N

CAS号161417-03-4

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关联

11

项与 Pozanicline Hydrochloride 相关的临床试验

NCT01756053

/ Terminated临床2期IIT

A Pilot Feasibility Study of the Effects of ABT-089 on Smoking Abstinence Symptoms and Reward

This Phase IIa within-subject, cross-over pilot study will evaluate the effects of ABT-089 (an experimental medication not approved by the FDA) when administered as 40mg oral once daily dose for 10 days, compared to placebo, on the following: abstinence-induced cognitive deficits, smoking withdrawal, smoking urges, smoking reward, and a brief, monitored quit attempt (
4 days). The key cognitive domains include: working memory, sustained attention, and response inhibition.

开始日期2013-03-01

申办/合作机构

University of Pennsylvania

NCT00809510

/ Terminated临床2期

A Study of the Long-term Safety of ABT-089 for Subjects With Mild-to-moderate Alzheimer's Disease Who Participated in the M06-876 Study

The purpose of this study is to evaluate the long-term safety and tolerability of ABT-089 in adults with mild-to-moderate Alzheimer's disease.

开始日期2009-01-01

申办/合作机构

Abbott Laboratories

NCT00686933

/ Completed临床2期

The Long-Term Safety and Tolerability of ABT-089 in Adults With Attention Deficit-Hyperactivity Disorder (ADHD): An Open-Label Extension Study for Subjects Completing Study M10-346

The objective of this study is to evaluate the long-term effects and tolerability of ABT-089 in adults with Attention-Deficit/Hyperactivity Disorder (ADHD).

开始日期2008-05-01

申办/合作机构

AbbVie, Inc.

100 项与 Pozanicline Hydrochloride 相关的临床结果

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100 项与 Pozanicline Hydrochloride 相关的转化医学

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100 项与 Pozanicline Hydrochloride 相关的专利（医药）

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62

项与 Pozanicline Hydrochloride 相关的文献（医药）

2025-03-27·Journal of Medicinal Chemistry

The Heterogeneous Kinetic Origins of the Binding Properties of Orthosteric Ligands at Heteromeric Nicotinic Acetylcholine Receptors

Article

作者: Holmgård, David S. G. ; Zhou, Libin ; Kristensen, Jesper L. ; Jensen, Anders A.

A plethora of agonists and competitive antagonists have been developed to explore the therapeutic potential in neuronal nicotinic acetylcholine receptors (nAChRs). Based on equilibrium and kinetic [³H]epibatidine binding studies, we report that the kinetic fingerprints of [³H]epibatidine at five heteromeric αβ nAChRs and of seven classical agonists at α4β2 and α3β4 nAChRs differ substantially. While this diversity depends on both the agonist and receptor subtype, the overall pattern of kinetic determinants emerging from this profiling is complex. The dramatically different binding kinetics displayed by two alkaloids and competitive antagonists, (+)-DHβE and (+)-cocculine, at the α4β2 nAChR further exemplify how dissimilar kinetics can underlie very comparable pharmacological properties exhibited by close structural analogs. Thus, our findings elucidate the heterogeneous kinetic basis for orthosteric ligand binding to αβ nAChRs and emphasize how the binding affinities, selectivity profiles, and structure-activity relationships of these ligands are rooted in their kinetic traits at the receptors.

2024-02-01·Powder Technology

The effects of humidity on the adhesion of pharmaceutical excipients to steel surfaces

作者: Beaudoin, Stephen ; Vogt, Andrew ; Cheah, WeiBin ; Main, Ethan ; Ketterhagen, William ; Jones, Olivia ; Park, Sarah ; Stevenson, Caralyn ; Sura, Isha ; Monroe, Jordan ; Zhang, Richael ; Nobbe, Briana ; Vazquez, Juan Manuel ; Upton, Josephine ; Capece, Maxx ; Roberts, Tyler

The adhesion between powders and surfaces is influenced by their topog.We investigate the relationships between the topog. on stainless steel, the humidity, and the adhesion of three pharmaceutical powders.These relationships are captured within 'effective' work of adhesion parameters tuned using the enhanced centrifuge method (ECM).The parameters describe the effects of the size, shape, humidity, and topog. on the adhesion.The powders' ability to nestle into features on the steel drove the work of adhesion.When the powders absorbed moisture, the balance of moisture-driven deformation and increased mass dictated the powder removal from the surface.The irregularly shaped hypromellose (HPMC) adhered more strongly to the stainless steel at low humidity than at high.The lactose monohydrate and ABT-089 showed the opposite behavior.The HPMC adhered more strongly to the rough steel than to the smooth or untreated steel.The lactose monohydrate and ABT-089 again showed the opposite behavior.

2021-04-01·American Journal of Medical Genetics Part B: Neuropsychiatric Genetics3区 · 医学

Candidate pharmacological treatments for substance use disorder and suicide identified by gene co‐expression network‐based drug repositioning

3区 · 医学

Article

作者: Genis‐Mendoza, Alma Delia ; Díaz‐Otañez, Carlos Enrique ; Flores, Gonzalo ; Nicolini, Humberto ; García‐Dolores, Fernando ; Monroy‐Jaramillo, Nancy ; López Armenta, Mauro ; Walss‐Bass, Consuelo ; Martínez‐Magaña, José Jaime ; Vázquez‐Roque, Rubén Antonio ; Fries, Gabriel Rodrigo ; Cabrera‐Mendoza, Brenda ; Fresno, Cristóbal

AbstractPatients with substance use disorders (SUD) are at high risk to die by suicide. So far, the neurobiology of the suicide‐SUD association has not been elucidated. This study aimed to identify potential pharmacological targets among hub genes from brain gene co‐expression networks of individuals with SUD in a suicidal and non‐suicidal context. Post‐mortem samples from the prefrontal cortex of 79 individuals were analyzed. Individuals were classified into the following groups: suicides with SUD (n = 28), suicides without SUD (n = 23), nonsuicides with SUD (n = 9), nonsuicides without SUD (n = 19). Gene expression profiles were evaluated with the Illumina HumanHT‐12 v4 array. Co‐expression networks were constructed in WGCNA using the differentially expressed genes found in the comparisons: (a) suicides with and without SUD and (b) nonsuicides with and without SUD. Hub genes were selected for drug‐gene interaction testing in the DGIdb database. Among drugs interacting with hub genes in suicides we found MAOA inhibitors and dextromethorphan. In the nonsuicide individuals, we found interactions with eglumegad and antipsychotics (olanzapine, clozapine, loxapine). Modafinil was found to interact with genes in both suicides and nonsuicides. These drugs represent possible candidate treatments for patients with SUD with and without suicidal behavior and their study in each context is encouraged.

100 项与 Pozanicline Hydrochloride 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	Pozanicline Hydrochloride	-	DB05458

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
注意缺陷障碍伴多动	临床2期	美国	Abbott Laboratories	2006-10-01
注意缺陷障碍伴多动	临床2期	美国	Abbott Laboratories	2006-10-01
阿尔茨海默症	临床2期	美国	Abbott Laboratories	2003-07-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01756053 (CTgov)	临床2期	尼古丁依赖	17	ABT-089 (ABT-089)	夢艱獵繭鏇蓋憲製膚廠(蓋醖襯構夢膚鑰鹹獵顧) = 衊壓觸艱淵壓襯願襯遞膚範餘襯鏇網鹽糧遞範 (壓壓網衊鏇艱艱憲獵網, 構觸憲製簾衊願網蓋糧 ~ 艱夢願齋築餘積鹽餘繭) 更多	-	2014-10-29
				Placebo (Placebo)	夢艱獵繭鏇蓋憲製膚廠(蓋醖襯構夢膚鑰鹹獵顧) = 醖夢窪顧壓醖選顧窪築膚範餘襯鏇網鹽糧遞範 (壓壓網衊鏇艱艱憲獵網, 製夢廠膚襯選淵憲觸齋 ~ 廠築觸艱網獵網窪觸顧) 更多
NS59910 (WPC2013)	临床2期	-	-	Nicotine	醖餘夢積觸膚襯淵鹽觸(蓋餘獵網築選繭範鏇蓋) = 積構襯糧積顧選壓繭艱齋壓構製遞構鑰膚衊製 (遞淵淵選範餘簾構憲夢 )	积极	2013-10-01
				Varenicline	醖餘夢積觸膚襯淵鹽觸(蓋餘獵網築選繭範鏇蓋) = 鹽繭齋艱窪襯窪鹽築構齋壓構製遞構鑰膚衊製 (遞淵淵選範餘簾構憲夢 )