Delving into the Latest Updates on Pyragrel Sodium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

TSF

Target

TXA2 synthase

Mechanism

TXA2 synthase inhibitors(Thromboxane A2 synthase inhibitors)

Therapeutic Areas

Nervous System DiseasesCardiovascular Diseases

Active Indication

Acute Ischemic StrokeThrombotic cerebral infarctionBrain Infarction

Inactive Indication-

Originator Organization

Hefei medical and Pharmaceutical Co., Ltd.

Active Organization

Hefei medical and Pharmaceutical Co., Ltd.

Inactive Organization-

Drug Highest PhasePhase 3

First Approval Date-

RegulationSpecial Review Project (CN)

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Structure/Sequence

Molecular FormulaC18H20N2O4

InChIKeyGKIIUOKTDCNMFK-SOFGYWHQSA-N

CAS Registry1018438-91-9

View All Structures (2)

Sarcopenic obesity, encompassing both muscle wasting and obesity, is relevant across individuals. Toona sinensis (TS) has been shown to regulate glucose and lipid metabolisms. However, the efficacy and mechanisms of TS fruit (TSF) in sarcopenic obesity are unclear. This study investigated impacts of TSF extract on skeletal muscle atrophy in C57BL/6 mice fed a high-fat diet (HFD). After 25 weeks of TSF pre-treatment and supplementation, it reversed loss of skeletal muscle mass and grip strength in HFD-fed mice, independent of body weight changes. TSF treatment notably increased the phosphorylation of Akt, mTOR, and P70S6K, while suppressing nuclear localization of NFκB, FoxO1a, and transcription of atrogin-1, MuRF-1, and myostatin expression in HFD-fed muscle. Additionally, TSF influenced autophagic flux and mitochondria quality control, emphasizing its role in balancing protein synthesis and degradation. In conclusion, TSF alleviates HFD-induced sarcopenia via protein turnover, autophagic flux and mitochondria quality control, highlighting its potential therapeutic value for sarcopenic obesity.Graphical abstractSupplementary InformationThe online version contains supplementary material available at 10.1007/s10068-024-01610-3.

24 Dec 2024·ACS Nano

On-Site Self-Penetrating Nanomedicine Enabling Dual-Priming Drug Activation and Inside-Out Thrombus Ablation

Article

Author: He, Zhonggui ; Wu, Haonan ; Luo, Cong ; Wang, Yuequan ; Zhang, Shenwu ; Wang, Jing ; Sun, Jin ; Zhang, Hongyuan

Main conventional antithrombotic therapies often suffer from unsatisfactory treatment outcomes and the risk of undesirable tissue hemorrhage. Deep clot penetration, on-demand drug activation, and release within the clots remain significant challenges. While past efforts to develop nanomedicines and prodrugs have improved safety at the expense of therapeutic effects. Herein, we develop a self-piercing and self-activating nanoassembly composed of an oxidation-sensitive prodrug (TGL-S-Fmoc, TSF) of ticagrelor (TGL) and IR808 (a photothermal/photodynamic dual-effect photosensitizer). TSF readily coassembles with IR808 into a carrier-free hybrid nanomedicine. Upon laser irradiation, IR808 enables photothermal thrombolysis and deep clot penetration of TSF while also synergistically facilitating prodrug activation triggered by IR808-generated singlet oxygen (¹O₂) and the endogenous hydrogen peroxide within the clots. Following fibrin-targeting modification, the nanoassembly achieves self-indicating thrombus-targeted accumulation, self-piercing deep clot penetration, dual-priming prodrug activation, and inside-out thrombus ablation with favorable safety in vivo. This study advances the clinical translation of antithrombotic prodrugs and nanomedicines.

01 Dec 2024·International Journal of Eating Disorders

A Psychophysiological Investigation of Mechanisms Underlying “Feeling Fat” in Women With and Without Binge Eating

Article

Author: Wilson, Samantha ; Mehak, Adrienne ; Racine, Sarah E.

ABSTRACTObjective“Feeling fat”, the somatic experience of being overweight not fully explained by objective body weight, is considered to be an eating pathology maintenance factor. The traditional clinical understanding of “feeling fat” is based on the body displacement hypothesis, which suggests that negative emotions are projected onto the body and experienced as “feeling fat” in lieu of adaptive emotion regulation. A more recent theory suggests that “feeling fat” occurs in response to thought‐shape fusion (TSF), a cognitive distortion in response to the imagined consumption of perceived fattening food. The present experimental study compared the roles of these two proposed mechanisms of “feeling fat” using self‐report and psychophysiological measures.MethodEighty‐two women (41 with binge eating, 41 control participants) self‐reported “feeling fat” and had their heart rate variability (HRV), a physiological index of emotion regulation, measured before and after imagined inductions. Participants imagined either a personalized negative affective experience or consuming a preferred, so‐called ‘fattening’ food.ResultsThe TSF induction increased self‐reports of “feeling fat” among participants with binge eating but not among control women. The negative affect induction did not increase self‐reported “feeling fat” in either group. HRV did not significantly change in response to either induction for either group.DiscussionTSF may be a more potent precursor to “feeling fat” than negative affect for individuals with binge eating. This may suggest new treatment directions, such as cognitive defusion from TSF when patients experience “feeling fat.” The utility of HRV in monitoring “feeling fat” is questionable.

100 Deals associated with Pyragrel Sodium

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acute Ischemic Stroke	Phase 3	CN	Hefei medical and Pharmaceutical Co., Ltd.	04 Aug 2023
Thrombotic cerebral infarction	Phase 3	CN	Hefei medical and Pharmaceutical Co., Ltd.	04 Aug 2023
Brain Infarction	Phase 2	CN	Hefei medical and Pharmaceutical Co., Ltd.	16 Jul 2018