Delving into the Latest Updates on Pidazone with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target-

Action

inhibitors

Mechanism

Neuritis inhibitors

Therapeutic Areas

Nervous System DiseasesCardiovascular Diseases

Active Indication

Alzheimer DiseaseStroke

Inactive Indication

Cognition DisordersMemory DisordersMild dementia+ [1]

Originator Organization

Chinese Academy of Sciences

Active Organization

Gibh

Inactive Organization

Guangdong South China New Drug Creation Center

Drug Highest PhasePhase 1

First Approval Date-

RegulationSpecial Review Project (China)

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Structure/Sequence

Molecular FormulaC20H20N6O

InChIKeyZTJHTEHADIHZJS-UHFFFAOYSA-N

CAS Registry1252608-59-5

This single-center, randomized, placebo-controlled, double-blind, dose-increasing study was designed to evaluate the safety, tolerability, and pharmacokinetics of multiple successive dosing in healthy Chinese adult subjects.In this study, 20 healthy adult subjects were enrolled in a multi-dose study in the 30mg and 40mg groups.

Start Date26 May 2020

Sponsor / Collaborator

Xiangya Hospital Central South University

CTR20200977

/ CompletedPhase 1

哌哒甲酮片在中国成人健康受试者中多次给药的安全性、耐受性及药代动力学研究

[Translation] Safety, tolerability and pharmacokinetics of pyridamole tablets after repeated administration in healthy Chinese adult subjects

主要目的：评估中国成人健康受试者空腹条件下多次连续服用哌哒甲酮片后的安全性、耐受性;次要目的：评估中国成人健康受试者空腹条件下多次连续服用哌哒甲酮片后的药代动力学特性。

[Translation]

The primary objective is to evaluate the safety and tolerability of multiple continuous administration of pyridamole tablets in healthy Chinese adult subjects under fasting conditions; the secondary objective is to evaluate the pharmacokinetic properties of pyridamole tablets in healthy Chinese adult subjects under fasting conditions.

Start Date26 May 2020

Sponsor / Collaborator

Guangdong South China New Drug Creation Center

[+1]

CTR20191869

/ CompletedPhase 1

评估高脂饮食对哌哒甲酮片在中国健康成人受试者中药代动力学影响研究

[Translation] A study to evaluate the effect of a high-fat diet on the pharmacokinetics of pyridamole tablets in healthy Chinese adults

主要目的：评估高脂饮食对中国健康成人受试者单剂量服用哌哒甲酮片药代动力学特征的影响;次要目的：评估高脂饮食对中国健康成人受试者单剂量服用哌哒甲酮片的安全性的影响。

[Translation]

The primary objective was to evaluate the effect of a high-fat diet on the pharmacokinetic characteristics of a single dose of pyridamole tablets in healthy Chinese adult subjects. The secondary objective was to evaluate the effect of a high-fat diet on the safety of a single dose of pyridamole tablets in healthy Chinese adult subjects.

Start Date18 Sep 2019

Sponsor / Collaborator

Guangdong South China New Drug Creation Center

[+1]

100 Clinical Results associated with Pidazone

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100 Translational Medicine associated with Pidazone

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100 Patents (Medical) associated with Pidazone

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18

Literatures (Medical) associated with Pidazone

01 Jan 2025·Bioorganic & Medicinal Chemistry

Synthesis and biological evaluation of lappaconitine analogues as potential anti-neuroinflammatory agents by side chain modification and scaffold hopping strategy

Article

Author: Xing, Feng ; Li, Yu-Zhu ; Su, Hong-Yi ; Zhong, He-Yang ; Chen, Lin ; Zhang, Yin-Yong ; Zhou, Xian-Li

Neuroinflammation mediated by microglia is widely recognized as a key pathophysiological mechanism in neurodegenerative diseases. Lappaconitine (LA) is a natural C₁₈-diterpenoid alkaloid isolated from Aconitum sinomontanum Nakai, and previous study showed that LA and its derivatives inhibited lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW264.7 cells. However, the anti-neuroinflammatory effects of LA and its derivatives on microglia are still not clear. Here, LA analogues were designed and synthesized, and the anti-neuroinflammatory activity of the synthesized compounds was screened using LPS-induced overexpression of NO in BV-2 microglia. The screening results showed that compound 10 displayed the highest ability to inhibit NO production (IC₅₀ = 9.98 ± 1.6 µM). Mechanistic investigations revealed that compound 10 attenuated LPS-activated neuroinflammation through suppression of TLR4/MyD88/NF-κB pathway in BV-2 microglia. Acute toxicity assays showed that compound 10 (LD₅₀ = 508.1 mg/kg) was safer relative to LA (LD₅₀ = 30.6 mg/kg). Collectively, our findings show that compound 10 could have potential as anti-neuroinflammatory agents.

01 Sep 2024·Biomedicine & Pharmacotherapy

AD16 attenuates neuroinflammation induced by cerebral ischemia through down-regulating astrocytes A1 polarization

Article

Author: Huang, Cheng ; Huang, Zhihua ; Zhao, Guojian ; Luo, Zhengwei ; Tang, Xiaolu ; Liu, Gaigai ; Yu, Zining ; Feng, Zhong-Ping ; Sun, Hong-Shuo ; Yuan, Zhidong ; Su, Guangjun ; Zhang, Limei

A1 polarization of astrocytes mediated prolonged inflammation contributing to brain injury in ischemic stroke. We have previously shown that AD16 protects against neonatal hypoxic-ischemic brain damage in vivo and oxygen-glucose deprivation in vitro. More recently, AD16 has demonstrated safety, tolerability, and favorable pharmacokinetics in a randomized controlled phase I trial. In this study, we utilized a rat model of transient middle cerebral artery occlusion (tMCAO) to explore whether the anti-inflammatory compound AD16 protects against ischemic brain injury by regulating A1 polarization and its underlying mechanisms. Our results showed that AD16 treatment significantly reduced the brain infarcted volume and improved neurological function in tMCAO rats. GO analysis results show that differential genes among the Sham, tMCAO and AD16 treatment groups are involved in the regulation of cytokine and inflammatory response. KEGG enrichment pathways analysis mainly enriched in cytokine-cytokine receptor interaction, viral protein interaction with cytokine-cytokine receptor, TNF, chemokine, NF-κB and IL-17 signaling pathway. Furthermore, AD16 treatment decreased the permeability of the blood-brain barrier and suppressed neuroinflammation. AD16 treatment also significantly reduced the polarization of A1 and inhibited NF-κB and JAK2/STAT3 signaling pathways. This study demonstrates that AD16 protects against brain injury in ischemic stroke by reducing A1 polarization to suppress neuroinflammation through downregulating NF-κB and JAK2/STAT3 signaling. Our findings uncover a potential molecular mechanism for AD16 and suggest that AD16 holds promising therapeutic potential against cerebral ischemia.

01 Aug 2022·Neuroscience BulletinQ2 · MEDICINE

AD-16 Protects Against Hypoxic-Ischemic Brain Injury by Inhibiting Neuroinflammation

Q2 · MEDICINE

Article

Author: Feng, Zhong-Ping ; Wan, Jiangfan ; Luo, Zhengwei ; Hu, Wenhui ; Chen, Nai-Hong ; Huang, Zhihua ; Ovcjak, Andrea ; Sun, Hong-Shuo

Neuroinflammation is a key contributor to the pathogenic cascades induced by hypoxic-ischemic (HI) insult in the neonatal brain. AD-16 is a novel anti-inflammatory compound, recently found to exert potent inhibition of the lipopolysaccharide-induced production of pro-inflammatory and neurotoxic mediators. In this study, we evaluated the effect of AD-16 on primary astrocytes and neurons under oxygen-glucose deprivation (OGD) in vitro and in mice with neonatal HI brain injury in vivo. We demonstrated that AD-16 protected against OGD-induced astrocytic and neuronal cell injury. Single dose post-treatment with AD-16 (1 mg/kg) improved the neurobehavioral outcome and reduced the infarct volume with a therapeutic window of up to 6 h. Chronic administration reduced the mortality rate and preserved whole-brain morphology following neonatal HI. The in vitro and in vivo effects suggest that AD-16 offers promising therapeutic efficacy in attenuating the progression of HI brain injury and protecting against the associated mortality and morbidity.

100 Deals associated with Pidazone

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Alzheimer Disease	Discovery	China	Guangdong South China New Drug Creation Center	30 Jan 2019
Cognition Disorders	Discovery	China	Gibh	28 Jan 2019
Cognition Disorders	Discovery	China	Guangdong South China New Drug Creation Center	28 Jan 2019
Memory Disorders	Discovery	China	Gibh	28 Jan 2019
Memory Disorders	Discovery	China	Guangdong South China New Drug Creation Center	28 Jan 2019
Mild dementia	Discovery	China	Gibh	28 Jan 2019
Mild dementia	Discovery	China	Guangdong South China New Drug Creation Center	28 Jan 2019
Moderate dementia	Discovery	China	Guangdong South China New Drug Creation Center	28 Jan 2019
Moderate dementia	Discovery	China	Gibh	28 Jan 2019
Stroke	Discovery	China	Gibh	23 Nov 2017