Delving into the Latest Updates on Trifluoperazine Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

10-[3-(4-methyl-1-piperazinyl)propyl]-2-(trifluoromethyl)-10H-phenothiazine, Trifluoperazine, Trifluoperazine hydrochloride (JAN/USP)

+ [10]

Target

DRDs

Action

antagonists

Mechanism

DRDs antagonists(Dopamine receptors antagonists)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication

Anxiety DisordersDepressive DisorderSchizophrenia

Inactive Indication-

Originator Organization

GSK Plc

Active Organization

Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.

Inactive Organization

GlaxoSmithKline, Inc.

Drug Highest PhaseApproved

First Approval Date

United States (16 Apr 1959),

Anxiety Disorders

Regulation-

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Structure/Sequence

Molecular FormulaC21H24F3N3S

InChIKeyZEWQUBUPAILYHI-UHFFFAOYSA-N

CAS Registry117-89-5

View All Structures (2)

The antimicrobial effectiveness of five phenothiazine derivatives, namely A, B, C, D and E, was examined against three Gram-pos. and three Gram-neg. bacteria, as well as seven fungal species.Anal. of the gathered data revealed that all derivatives exhibited strong antibacterial properties.However, their performance as antifungal agents were comparatively less effective which may be attributed to cell structure of fungi.Notably, in several instances, the activity of the phenothiazine derivatives surpassed that of the reference drug penicillin 10.Furthermore, mol. docking studies provided addnl. evidence of the ability of these four derivatives to bind with the target enzyme PBP2a.The docking scores obtained ranged from -11.27 to -15.90 Kcal/mol.According to pharmacokinetics and ADME study, all phenothiazine derivatives A-E, as well as Penicillin 10, have a bioavailability higher than zero, ranging between 0.17 and 0.55.Phenothiazine derivative A is similar to the reference drug penicillin 10, indicating that it is the most bioactive.

01 Feb 2025·Talanta

Highly sensitive electrochemical determination of agomelatine in biological samples based on Cu nanoparticles/Schiff base network1 modified glassy carbon electrode: DFT and experimental studies

Article

Author: Afkhami, Abbas ; Ajdari, Beheshteh ; Madrakian, Tayyebeh ; Jalali Sarvestani, Mohammad Reza

In this study, a nanocomposite of copper nanoparticles incorporated into a covalent organic framework (Cu@SNW1) was synthesized and characterized by various approaches such as scanning electron microscopy, cyclic voltammetry, X-ray diffraction, electrochemical impedance spectroscopy, and energy dispersive X-ray spectroscopy. The interaction between the nanocomposite and agomelatine (AGM) was investigated through density functional theory computations. The results indicated that the nanocomposite displays electrocatalytic properties towards AGM and their interactions are both experimentally and thermodynamically viable. The synthesized nanocomposite was employed as an electrocatalytic modifier for the highly selective and sensitive square wave anodic stripping voltammetric detection of AGM. Experimental parameters including; pH, deposition time, modifier concentration, and deposition potential were fine-tuned using the Box-Behnken experimental design strategy. Under the optimal conditions, a linear correlation was established between the anodic peak current of AGM and its concentration across two linear ranges, 0.007-1.00 μmol L^-1 and 1.00-6.50 μmol L^-1. The method demonstrated a limit of detection of 0.002 μmol L^-1 under the optimized parameters. Furthermore, the proposed method exhibited high sensitivity and selectivity in determining AGM in urine, serum, and saliva samples.

01 Feb 2025·Glia

A bottom‐up approach identifies the antipsychotic and antineoplastic trifluoperazine and the ribose derivative deoxytubercidin as novel microglial phagocytosis inhibitors

Article

Author: Rodriguez‐Iglesias, Noelia ; Cañas‐Zabala, Lorena ; Patsch, Christoph ; Valero, Jorge ; Paris, Iñaki ; Zhang, Jitao David ; Gutbier, Simon ; Sierra, Amanda ; Carretero, Alejandro ; Hatje, Klas ; Britschgi, Markus

AbstractPhagocytosis is an indispensable function of microglia, the brain professional phagocytes. Microglia is particularly efficient phagocytosing cells that undergo programmed cell death (apoptosis) in physiological conditions. However, mounting evidence suggests microglial phagocytosis dysfunction in multiple brain disorders. These observations prompted us to search for phagocytosis modulators (enhancers or inhibitors) with therapeutic potential. We used a bottom‐up strategy that consisted on the identification of phagocytosis modulators using phenotypic high throughput screenings (HTSs) in cell culture and validation in organotypic cultures and in vivo. We performed two complementary HTS campagnes: at Achucarro, we used primary cultures of mouse microglia and compounds of the Prestwick Chemical Library; at Roche, we used human iPSC derived macrophage‐like cells and a proprietary chemo‐genomic library with 2200 compounds with known mechanism‐of‐action. Next, we validated the more robust compounds using hippocampal organotypic cultures and identified two phagocytosis inhibitors: trifluoperazine, a dopaminergic and adrenergic antagonist used as an antipsychotic and antineoplastic; and deoxytubercidin, a ribose derivative. Finally, we tested whether these compounds were able to modulate phagocytosis of apoptotic newborn cells in the adult hippocampal neurogenic niche in vivo by administering them into the mouse hippocampus using osmotic minipumps. We confirmed that both trifluoperazine and deoxytubercidin have anti‐phagocytic activity in vivo, and validated our bottom‐up strategy to identify novel phagocytosis modulators. These results show that chemical libraries with annotated mechanism of action are an starting point for the pharmacological modulation of microglia in drug discovery projects aiming at the therapeutic manipulation of phagocytosis in brain diseases.

100 Deals associated with Trifluoperazine Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D00799	Trifluoperazine Hydrochloride	N05AB06	DB00831

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Anxiety Disorders	China	Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.	01 Jan 1995
Depressive Disorder	China	Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.	01 Jan 1995
Schizophrenia	China	Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.	01 Jan 1995

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03966053 (DBA, CTgov)	Phase 1/2	Diamond-Blackfan Anemia 1	2	Trifluoperazine	fxonzrfhwq(jyznaxyiyh) = hkcimnjnjt wvjnynwpzn (lpclyehxfh, qzfshwwqks - ftdkiqjrtt) View more	-	14 Dec 2022
ASCO2012	Not Applicable	-	-	Trifluoperazine	jrpyzpwsng(steqetyipl) = hshlujbecm rolbcalcfc (wpkhhrbvgh )	-	20 May 2012
ASCO2012	Not Applicable	-	-	trifluoperazine (Ionizing radiation)	jrpyzpwsng(steqetyipl) = uldosjstnb rolbcalcfc (wpkhhrbvgh )	-	20 May 2012