Delving into the Latest Updates on Apelin-13 with Synapse

Overview

Basic Info

Drug Type

Synthetic peptide

Synonyms

Target

APLNR

Mechanism

APLNR agonists(Apelin receptor agonists)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Diabetes Mellitus, Type 2

Inactive Indication-

Originator Organization

Le Centre Hospitalier Universitaire de Toulouse

Active Organization

Le Centre Hospitalier Universitaire de Toulouse

Inactive Organization-

Drug Highest PhasePhase 1

First Approval Date-

Regulation-

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Structure

Molecular FormulaC69H111N23O16S

InChIKeyXXCCRHIAIBQDPX-PEWBXTNBSA-N

CAS Registry217082-58-1

Gene Sequence

Sequence Code 9616810

Source: *****

The purpose of this study is to
Determine blood peptide levels and investigate any tissue gradients of apelin in patients with idiopathic pulmonary arterial hypertension and healthy volunteers.
Evaluate the effect of exogenous apelin infusion on exercise performance in healthy volunteers and patients with idiopathic pulmonary arterial hypertension.

Start Date01 Mar 2012

Sponsor / Collaborator

Imperial College London

100 Clinical Results associated with Apelin-13

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100 Translational Medicine associated with Apelin-13

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100 Patents (Medical) associated with Apelin-13

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377

Literatures (Medical) associated with Apelin-13

04 Dec 2024·NeuroReport

The effects of apelin-13 in a mouse model of post-traumatic stress disorder

Article

Author: Meng, Zijun ; Kuai, Jinxia ; Han, Yuqing ; Yang, Xiaofang ; Bao, Haijun ; Zhou, Yang

The objective is to investigate the effects of apelin-13 in models of post-traumatic stress disorder (PTSD). Mature male CD1 mice were subjected to the single prolonged stress method to induce PTSD-related behaviors. These behaviors were then evaluated using the elevated plus maze test, Morris water maze test, and open field test. Hippocampal neural cell death was assessed using propidium iodide labeling. The expression of hippocampal autophagy pathway-associated proteins was determined through immunoblotting analysis, and LC3 levels were also measured via quantitative real-time reverse transcription-PCR. The results demonstrate that administration of apelin-13 suppressed PTSD-induced hippocampal neural cell death and alleviated PTSD-related behaviors in mice. Additionally, PTSD led to an up-regulation of LC3 and FoxO3a, and down-regulation of P62, p-PI3K, p-Akt, and p-FoxO3a in the hippocampus. However, these changes were reversed by apelin-13 treatment. These findings support the hypothesis that apelin-13 prevents the development of PTSD-like behavior and inhibits autophagy of neuronal cells in a mouse model of PTSD. Apelin-13 may hold potential as a therapeutic agent for PTSD in clinical applications.

01 Dec 2024·Molecular Biology Reports

Protective effect of apelin-13 on ventilator-induced acute lung injury

Article

Author: Zhou, Leilei ; Lian, Siyu ; Jiang, Wenqing ; Chen, Zongyu ; He, Shuang ; Zhang, Xianming ; Shen, Yi

BACKGROUNDMechanical Ventilation (MV) is an essential mechanism of life support in the clinic. It may also lead to ventilator-induced acute lung injury (VILI) due to local alveolar overstretching and/or repeated alveolar collapse. However, the pathogenesis of VILI is not completely understood, and its occurrence and development may be related to physiological processes such as the inflammatory response, oxidative stress, and apoptosis. Some studies have found that the the apelin/APJ axis is an endogenous antagonistic mechanism activated during acute respiratory distress syndrome(ARDS), that can counteract the injury response and prevent uncontrolled lung injury. To indicate that apelin-13 plays a protective role in VILI, an animal model of VILI was established in this study to explore whether apelin-13 can alleviate VILI in rats by inhibiting inflammation, apoptosis and oxidative stress.METHODSSD rats were divided into four groups: control, high tidal volume, high tidal volume + normal saline and high tidal volume + apelin-13. After tracheotomy, the rats in control maintained spontaneous breathing, and the other rats were connected to the small animal ventilator for 4 h to establish the rat VILI model. The mRNA expression of apelin was measured by real-time quantitative polymerase chain reaction(qRT-PCR), immunofluorescence and Western blotting(WB) were used to detect the expression level of APJ, and WB was used to detect the expression of the apoptotic proteins Bax and bcl-2. The degree of lung injury was evaluated by pathological staining of lung tissue,W/D ratio, and BALF total protein concentration. The expression of inflammatory factors(IL-1β, IL-6, TNF-α) in alveolar lavage fluid was measured using ELISA. The activities of MPO and cat and the content of MDA, an oxidative product, in lung tissue were measured to evaluate the degree of oxidative stress in the lung.RESULTSAfter treatment with apelin-13, the apelin/APJ axis in the lung tissue of VILI model rats was activated, and the effect was further enhanced. The pathological damage of lung tissue was alleviated, the expression of the antiapoptotic protein Bcl-2 and the proapoptotic protein Bax was reversed, and the levels of the inflammatory cytokines IL-1β, IL-6, TNF-α levels were all decreased. MPO activity and MDA content decreased, while CAT activity increased.CONCLUSIONThe apelin/apj axis is activated in VILI. Overexpression of apelin-13 further plays a protective role in VILI, mainly by including reducing pathological damage, the inflammatory response, apoptosis and antioxidant stress in lung tissue, thus delaying the occurrence and development of VILI.

01 Nov 2024·Neuroscience Letters

Effects of Apelin-13 on auditory system in STZ-induced diabetic rats

Article

Author: Kılınç, Sevtap ; Eylül Aydemir, Berfin ; Arzu Yiğit, Ayşe ; Güneşer, Özgecan ; Ölçüoğlu, Rukiye ; Kilinç, Sevtap

AIMDamage to the auditory pathways is one of the complications of diabetes. The aim of this study was to investigate the potential therapeutic effects of apelin-13 in the auditory pathways of rats with experimentally induced diabetes by examining its effect on auditory brainstem responses, cochlear oxidative stress and inflammatory cytokines.METHODSThirty-two male Wistar albino rats were divided into four groups: sham control, diabetes, apelin and diabetes + apelin. A single dose of 45 mg/kg streptozotocin (STZ) was administered to induce diabetes. The apelin group received 50 µg/kg apelin-13 for seven days intraperitoneally (ip). At the end of the apelin and STZ applications auditory brainstem responses (ABR) was recorded. At the end of the experiment, cochlea was removed and biochemical analyzes were performed.RESULTSIn ABR recordings, the latencies of wave V in diabetic group were observed to be longer than those of the control, with the apelin treatment exhibiting a partial reversal of this situation, particularly at specific frequencies and intensity levels. Apelin treatment leads to a significant increase in total antioxidant status (TAS) and a reduction in total oxidant status (TOS) and oxidative stress index (OSI) in cochlea compared to diabetic groups. The levels of tumor necrosis factor-alpha (TNF-alpha) and interleukin 1-beta (IL-1 beta) in cochlear tissue were found to be significantly reduced in the apelin-treated group compared to the diabetic group.CONCLUSIONApelin-13 may have a protective effect on the auditory system and may be proposed as a potential new therapeutic strategy for the management diabetic auditory impairment.

100 Deals associated with Apelin-13

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	Phase 1	-	Le Centre Hospitalier Universitaire de Toulouse	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


Pubmed \| J Mol Biol	Not Applicable	-	-	Apelin-13	(emrdxxmdjh) = Apelin also increased I(Na) "window" current by up to 600% onczyoexvd (vhchtimyfx )	-	01 Apr 2010
				Apelin-17