Delving into the Latest Updates on Thiethylperazine Malate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Thiethylperazine malate (JAN), Torecan

Target

D1 receptor x D2 receptor x D4 receptor

Mechanism

D1 receptor antagonists(Dopamine D1 receptor antagonists), D2 receptor antagonists(Dopamine D2 receptor antagonists), D4 receptor antagonists(Dopamine D4 receptor antagonists)

Therapeutic Areas

Other Diseases

Active Indication-

Inactive Indication

Nausea and vomiting

Originator Organization

Novartis Pharma AG

Active Organization-

Inactive Organization

Novartis Pharmaceuticals Corp.

Drug Highest PhaseWithdrawn

First Approval Date

US (18 Jul 1961),

Nausea and vomiting

Regulation-

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Structure

Molecular FormulaC30H41N3O10S2

InChIKeyGTHHLZDYRHLACN-UHFFFAOYSA-N

CAS Registry52239-63-1

View All Structures (2)

AbstractAlzheimer’s disease (AD) is spreading its root disproportionately among the worldwide population. Many genes have been identified as the hallmarks of AD. Based upon the knowledge, many clinical trials have been designed and conducted. Attempts have been made to alleviate the pathology associated with AD by targeting the molecular products of these genes. Irrespective of the understanding on the genetic component of AD, many clinical trials have failed and imposed greater challenges on the path of drug discovery. Therefore, this review aims to identify research and review articles to pinpoint the limitations of drug candidates (thiethylperazine, CT1812, crenezumab, CNP520, and lecanemab), which are under or withdrawn from clinical trials. Thorough analysis of the cross-talk pathways led to the identification of many confounding factors, which could interfere with the success of clinical trials with drug candidates such as thiethylperazine, CT1812, crenezumab, and CNP520. Though these drug candidates were enrolled in clinical trials, yet literature review shows many limitations. These limitations raise many questions on the rationale behind the enrollments of these drug candidates in clinical trials. A meticulous prior assessment of the outcome of clinical studies may stop risky clinical trials at their inceptions. This may save time, money, and resources.

01 Nov 2023·Microchimica Acta

Electrochemical determination of thiethylperazine using semi-graphitized carbon nanofibers-MnO nanocomposite

Article

Author: Smajdor, Joanna ; Marzec, Mateusz ; Piech, Robert ; Paczosa-Bator, Beata ; Zambrzycki, Marcel

AbstractA new voltammetric method is proposed for high sensitive thiethylperazine (THP) determination, using a glassy carbon electrode modified with semi-graphitized carbon nanofibers/MnO nanocomposite (eCNF/MnO/GC). To the best of our knowledge, this is the first electrochemical assay of THP determination, and the first use of the eCNF/MnO as the electrode modifier. The proposed method using eCNF/MnO/GC is characterized by high repeatability and sensitivity of measurements, with the linearity of THP in the range from 0.05 to 2.2 µmol L−1. The lowest detection limit achieved on the eCNF/MnO/GC electrode for 30 s of preconcentration was 6.3 nmol L−1 THP in 0.05 mol L−1 acetate buffer of pH 5.6. The proposed method was successfully applied to highly sensitive THP determination in complex matrices, such as tablets and plasma with good recovery (98–103%). The RSD value obtained for THP measurement at a concentration of 0.1 µmol L−1 was 1.3%. Amperometric measurements of THP under the flow injection conditions were also performed to indicate the possibility of its fast and accurate determination (103% and 95% for unmodified and modified electrode, respectively), with the duration of single analysis of approx. 30 s.Graphical Abstract

01 Feb 2020·Environment InternationalQ1 · ENVIRONMENTAL SCIENCE & ECOLOGY

Micro–level evaluation of organic compounds transformation in anaerobic digestion under feast and famine conditions assisted by iron–based materials – Revealing the true mechanism of AD enhancement

Q1 · ENVIRONMENTAL SCIENCE & ECOLOGY

ArticleOA

Author: Zhou, Yan ; Yan, Wangwang ; Qian, Tingting ; Soh, Yan Ni Annie

Conductive materials have been applied to assist syntrophic metabolism in anaerobic digestion. However, their role in the transformation of organic compounds, particularly recalcitrant compounds, has not been revealed. In this study, iron-based materials - magnetite nanoparticles and Fe²⁺- were employed to explore their effects on the transformation of different organic matters in anaerobic system. Prompted methane production rates and quantity in iron-based materials groups were found due to the improved solubilization of organic particles, enhanced degradation of recalcitrant compounds, and maintained microbial activity under substrate-limited conditions. Specifically, the proportion of the reducing functional groups (C-C/H or CC) and O/C ratio were always significantly lower in iron-based materials supplemented groups (Fe groups) compared to Control group, despite hydrolysis was greatly enhanced in Fe groups. The greater dehydrogenation oxidation was confirmed in the presence of iron-based materials. The remaining humic-like substances (HS), a typical type of recalcitrant compound, was about 2.5 times higher in Control group (221.2 ± 5.3 mg/L-C) compared to Fe groups after 30 days degradation. By tracking the aromaticity of HS and individual compounds at molecular level, this study reveals that iron-based materials were more effective in stimulating the degradation of aliphatic moieties than the aromatic moieties of recalcitrant compounds. When readily biodegradable substrates were limited, Fe groups continued methane generation by using recalcitrant compounds (e.g. thiethylperazine and fluvoxamino acid) as carbon source, and the microbial activity was maintained according to higher relative abundance of protonated nitrogen and continuous methanogenesis activity at starvation phase.

100 Deals associated with Thiethylperazine Malate

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