Delving into the Latest Updates on Mimopezil with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

DEBIO-9902 SR implants, N-(2-Hydroxy-3-methoxy-5-chlorobenzylidene)huperzine A, N-(5-chloro-2-hydroxy-3-methoxy-benzylidene)-huperzine A

+ [10]

Target

AChE x NMDA receptor

Mechanism

AChE inhibitors(Acetylcholinesterase inhibitors), NMDA receptor antagonists(Glutamate [NMDA] receptor antagonists)

Therapeutic Areas

Nervous System Diseases

Active Indication-

Inactive Indication

Alzheimer Disease

Originator Organization

Shanghai Institute of Materia Medica Chinese Academy of Sci

Active Organization-

Inactive Organization

Debiopharm International SA

Shanghai Institute of Materia Medica Chinese Academy of Sci

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC23H23ClN2O3

InChIKeyUYRWZANUXPUEPQ-OWNLDCJBSA-N

CAS Registry180694-97-7

Alzheimer's disease is characterised by memory loss and difficulties with thinking. These problems may be due to a deficiency in a brain chemical called acetylcholine. Acetylcholine helps transmit messages between nerve cells. Acetylcholine is degraded by an enzyme called "acetylcholinesterase". ZT-1 is a new drug derived from a plant extract already used in China for memory disorders, which blocks the action of the enzyme and restores adequate levels of acetylcholine.
This study will test the safety and efficacy of ZT-1 in the treatment of patients with Alzheimer's disease.
BRAINz stands for Better Recollection for Alzheimer's patients with the Implant of ZT-1.

Start Date01 Feb 2007

Sponsor / Collaborator

Debiopharm International SA

EUCTR2004-002941-11-GB / Not yet recruitingPhase 2

A multicentre, 3-month, randomised, double blind, placebo and active controlled study on the tolerability and efficacy of ZT-1 for the symptomatic treatment of mild to moderate Alzheimer’s Disease

Start Date06 Dec 2004

Sponsor / Collaborator

Debiopharm International SA

100 Clinical Results associated with Mimopezil

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100 Translational Medicine associated with Mimopezil

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100 Patents (Medical) associated with Mimopezil

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17

Literatures (Medical) associated with Mimopezil

01 Jan 2023·Neurochemistry International

Efficacy of novel SPAK inhibitor ZT-1a derivatives (1c, 1d, 1g & 1h) on improving post-stroke neurological outcome and brain lesion in mice

Article

Author: Zhang, Jinwei ; Molyneaux, Bradley J ; Patel, Shivani M ; Oft, Helena ; Foley, Lesley M ; Zhang, Ting ; Sun, Dandan ; Deng, Xianming ; Bhuiyan, Mohammad Iqbal H ; Fischer, Sydney ; Hitchens, T Kevin

SPAK inhibitor ZT-1a was previously shown to be neuroprotective in murine ischemic stroke models. In this study, we further examined the efficacy of four ZT-1a derivatives (ZT-1c, -1d, -1g and -1h) on reducing stroke-induced sensorimotor function impairment and brain lesions. Vehicle control (Veh) or ZT-1 derivatives were administered via osmotic pump to adult C57BL/6J mice during 3-21 h post-stroke. Neurological behavior of these mice was assessed at days 1, 3, 5, and 7 post-stroke and MRI T2WI and DTI analysis was subsequently conducted in ex vivo brains. Veh-treated stroke mice displayed sensorimotor function deficits compared to Sham mice. In contrast, mice receiving ZT-1a derivatives displayed significantly lower neurological deficits at days 3-7 post-stroke (p < 0.05), with ZT-1a, ZT-1c and ZT-1d showing greater impact than ZT-1h and ZT-1g. ZT-1a treatment was the most effective in reducing brain lesion volume on T2WI and in preserving NeuN + neurons (p < 0.01), followed by ZT-1d > -1c > -1g > -1h. The Veh-treated stroke mice displayed white matter tissue injury, reflected by reduced fractional anisotropy (FA) or axial diffusivity (AD) values in external capsule, internal capsule and hippocampus. In contrast, only ZT-1a-as well as ZT-1c-treated stroke mice exhibited significantly higher FA and AD values. These findings demonstrate that post-stroke administration of SPAK inhibitor ZT-1a and its derivatives (ZT-1c and ZT-1d) is effective in protecting gray and white matter tissues in ischemic brains, showing a potential for ischemic stroke therapy development.

01 Dec 2019·Poultry ScienceQ2 · AGRICULTURAL & FORESTRY SCIENCE

Antioxidant activities and protective effects of duck embryo peptides against H2 O2-induced oxidative damage in HepG2 cells

Q2 · AGRICULTURAL & FORESTRY SCIENCE

ArticleOA

Author: Liang, Guizhao ; Xie, Huadong ; Bu, Lijun ; He, Ying

Previous work showed that peptides from duck eggs incubated for 15 D presented high total antioxidant activities. Here, this work explore the antioxidant activities of different segments, ZT1 (≤3 KD), ZT2 (≤10 KD), and ZT3 (≤30 KD), derived from duck embryo peptides and their protective effects against H2O2-induced oxidative damage in HepG2 cells. Peptides present no cytotoxicity to HepG2 cells. Moreover, ZT1 exhibits a higher ability to scavenge several radicals as well as stronger inhibition of H2O2-induced oxidative stress than ZT2 and ZT3. The activities of catalase and glutathione peroxidase as well as total superoxide dismutase increase in a concentration-dependent manner. Peptides are isolated from ZT1 and then subjected to LC-MS/MS to identify their sequences, followed by functional annotation, bioinformatics prediction, and hot-spot motif recognition. As a result, 413 potential functional peptides are identified, with some compounds exhibiting more than 1 function. This work will help for exploring bioactive substances in duck embryo eggs and enhance the utilization value of duck or other poultry eggs.

01 Oct 2019·European Journal of Medicinal ChemistryQ1 · MEDICINE

A hemicyanine derivative for near-infrared imaging of β-amyloid plaques in Alzheimer's disease

Q1 · MEDICINE

Article

Author: Jin-Hua Zhao ; Xiao-Bing Wang ; Cheng Wang ; Si-Qiang Fang ; Cun-Jian Shi ; Ling-Yi Kong ; Fu-Cheng Yin ; Hua-Li Yang ; Yan-Wei Tang ; Lai-Liang Qu ; Heng Luo

The formation of amyloid-β (Aβ) plaques in the brain is one of the main pathological features of Alzheimer's disease (AD). The imaging probes, capable of detecting Aβ deposition, are important tools for early diagnosis of AD. In this article, we designed, synthesized and evaluated a cyanine-based near-infrared fluorescence (NIRF) probe ZT-1 for the detection of Aβ deposits in the brain. The probe had excellent fluorescent properties with an emission maximum above 720 nm upon binding to Aβ aggregates with affinity of 445.0 nM (K_d). Furthermore, ZT-1 exhibited good biostability, photostability, and binding selectivity toward Aβ_1-42 aggregates by in vitro fluorescence staining experiments. In vivo NIRF imaging result also revealed that our probe could efficiently differentiate transgenic and wild-type mice. All these studies indicated that ZT-1 is a promising fluorescent probe for Aβ plaques in the AD brains.

100 Deals associated with Mimopezil

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB05520

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Alzheimer Disease	Phase 2	-	Shanghai Institute of Materia Medica Chinese Academy of Sci	-
Alzheimer Disease	Phase 2	EU	Debiopharm International SA	-
Alzheimer Disease	Phase 2	CA	Debiopharm International SA	-
Alzheimer Disease	Phase 2	GB	Debiopharm International SA	-
Alzheimer Disease	Phase 2	AU	Debiopharm International SA	-