Delving into the Latest Updates on Etilefrine Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Etilefrine, Etilefrine hydrochloride (JP17), 塩酸エチレフリン

+ [6]

Target

ADRA1 x β1-adrenergic receptor

Action

agonists, antagonists

Mechanism

ADRA1 agonists(Adrenergic receptor alpha-1 agonists), β1-adrenergic receptor antagonists(Beta-1 adrenergic receptor antagonists)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Hypotension

Inactive Indication-

Originator Organization

Sanofi

Active Organization

Sanofi KK

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (03 Dec 1960),

Hypotension

RegulationOrphan Drug (European Union)

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Structure/Sequence

Molecular FormulaC10H16ClNO2

InChIKeyKTNROWWHOBZQGK-UHFFFAOYSA-N

CAS Registry943-17-9

View All Structures (2)

This work aimed to evaluate and compare the impact of adding hypertonic saline solution (HSS) infusion and/or etilefrine to oral diuretics therapy on clinical outcomes, renal and systemic hemodynamics, metabolic and inflammatory pathways by estimating the changes in selected biological markers in cirrhotic patients with ascites. Also, the trial aims to assess the safety and tolerability of such treatment regimens.

Start Date30 Nov 2017

Sponsor / Collaborator

Tanta University

JPRN-UMIN000016234

/ RecruitingNot ApplicableIIT

The effect of ephedrine and etilefrine on systolic pressure variation and pulse pressure variation - The effect of ephedrine and etilefrine on systolic pressure variation and pulse pressure variation

Start Date16 Jan 2015

Sponsor / Collaborator-

100 Clinical Results associated with Etilefrine Hydrochloride

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100 Translational Medicine associated with Etilefrine Hydrochloride

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100 Patents (Medical) associated with Etilefrine Hydrochloride

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719

Literatures (Medical) associated with Etilefrine Hydrochloride

06 Nov 2024·Journal of Agricultural and Food Chemistry

Biocontrol Ability of Strain Bacillus amyloliquefaciens SQ-2 against Table Grape Rot Caused by Aspergillus tubingensis

Article

Author: Li, Suran ; Dai, Shuangshuang ; Huang, Lei ; Ying, Ming ; Cui, Yumeng

Bacillus amyloliquefaciens strain SQ-2, isolated from a cured product, has been demonstrated to exhibit a highly efficacious performance against phytopathogens, including Stemphylium solani, Fusarium moniliforme, Fusarium graminearum, and Aspergillus tubingensis. In particular, with regard to A. tubingensis, which causes summer bunch rot, SQ-2 has been observed to suppress the mycelial growth of all tested grape cultivars by over 40%. Especially on Kyoho grapes, it has the highest inhibition rate of 53%. Scanning electron microscopy (SEM) confirms that SQ-2 is an effective agent for suppressing the mycelia proliferation, differentiation, and spore formation of A. tubingensis. Furthermore, an LC/MS analysis revealed that SQ-2 produces two principal lipopeptides, namely, bacillibactin and surfactin, in addition to a polyketide, bacillaene. Further analysis through gas chromatography-mass spectrometry (GC/MS) identified 41 distinct volatile organic compounds secreted by SQ-2. Transcriptomic analysis indicated that exposure to the metabolite of SQ-2 induced substantial gene expression alterations in A. tubingensis. These data suggest that B. amyloliquefaciens strain SQ-2 exhibits promising crop protection potential of inhibiting plant pathogens through the secretion of bacillibactin, surfactin, bacillaene, and VOCs.

01 Nov 2024·Journal of Biological Chemistry

Comprehensive characterization of the OCT1 phenylalanine-244-alanine substitution reveals highly substrate-dependent effects on transporter function

Article

Author: Schröder, Sophie ; Brockmöller, Jürgen ; Gebauer, Lukas ; Jensen, Ole ; Wittern, Carla Isabel

Organic cation transporters (OCTs) can transport structurally highly diverse substrates. The molecular basis of this extensive polyspecificity has been further elucidated by cryo-EM. Apparently, in addition to negatively charged amino acids, aromatic residues may contribute to substrate binding and substrate selectivity. In this study, we provide a comprehensive characterization of phenylalanine 244 in OCT1 function. We analyzed the uptake of 144 OCT1 substrates for the phenylalanine 244 to alanine substitution compared to WTOCT1. This substitution had highly substrate-specific effects ranging from transport reduced to 10% of WT activity up to 8-fold increased transport rates. Four percent of substrates showed strongly increased uptake (>200% of WT) whereas 39% showed strongly reduced transport (<50% of WT). Particularly with larger, more hydrophobic, and more aromatic substrates, the Phe244Ala substitution resulted in higher transport rates and lower inhibition of the transporter. In contrast, substrates with a lower molecular weight and less aromatic rings showed generally decreased uptake rates. A comparison of our data to available transport kinetic data demonstrates that generally, high-affinity low-capacity substrates show increased uptake by the Phe244Ala substitution, whereas low-affinity high-capacity substrates are characterized by reduced transport rates. Altogether, our study provides the first comprehensive characterization of the functional role of an aromatic amino acid within the substrate translocation pathway of OCT1. The pleiotropic function further highlights that phenylalanine 244 interacts in a highly specific manner with OCT1 substrates and inhibitors.

01 Nov 2024·Energy Conversion and Management

Understanding the relationship between catalytic pyrolysis conditions and hydrogen production by aqueous phase reforming of the water-soluble fractions of bio-oils

Author: Justicia, Jessica ; Gilarranz, Miguel A. ; Fermoso, Javier ; Moreno, Ines ; Baeza, Jose A. ; Baeza, José A. ; Heras, Francisco ; Calvo, Luisa ; Moreno, Inés ; Justicia, Jéssica

The valorization to H2 of real aqueous fractions of bio-oil (AFBs) from catalytic pyrolysis of woodchips was carried out by aqueous phase reforming (APR).Notable gas yield (23 mmol/gTOCo) and H₂ concentration (46 mol%) were achieved, with values among the best published for the APR of real biorefinery streams.The reforming of AFBs was favored by a high concentration of levoglucosan and low proportion of acids and ketones, with acetone and acetic acid being the most refractory compounds to APR.Relationships between the pyrolysis conditions and the H2 production obtained by APR were assessed, with more favorable results when the pyrolysis was carried out under the most severe conditions of those studied, i.e. 0.30 catalyst/biomass ratio and 500°C in the catalytic step.H₂ production increased to 32 mmol/gTOCo when 0.04 wt% formic acid was added to the reaction medium, showing that this strategy can overcome the low reforming ability of some AFB components.The Pt catalyst showed good stability after 3 consecutive reaction cycles, displaying only a slight decrease in TOC conversion and CCgas, but a moderate decrease in H2 production and gas concentrationThe loss of activity was ascribed to cumulative adsorption of high mol. weight compounds and oligomers on the catalyst surface.

100 Deals associated with Etilefrine Hydrochloride

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