Aim: To investigate the antithrombotic effects of morpholine and piperazine ring derivatives and their mechanisms.
Methods: In isolated rat aorta-precontracted with norepinephrine (NE), the vasodilatory effects of compounds with novel structure were investigated. Mice was given kappa-carrageenin i.p. and kept at the temperature of (20-21) degree C.
Results And Conclusion: Active candidate compounds including MOPMC, 2FBMPC, MPTMBC, DMHPPP and PPVP were shown to antagonize thrombosis at the dose of 1 mg.kg-1 through activating the endothelial target for acetylcholine; while the contrasting compounds MAPC, 4C3FBMOC, mTBMPC, MONVP and MPNVP showed no significant effect on the tension of isolated aorta strips or significant antithrombotic effects at the same dose. The antithrombotic mechanism of novel compounds is not relevant to hemostatic systems or functions of platelet aggregation directly, but they can promote endothelial cells to release tissue-type plasminogen activator (t-PA) and inhibit the activity of plasminogen activator inhibitor-1 (PAI-1).
Download full-text PDF |
Source |
|---|
Publication Analysis
Top Keywords
Similar Publications
Comorbid diabetes mellitus (DM) in patients with ischemic heart disease (IHD) is a serious factor that significantly impairs the life prognosis and increases the risk of cardiovascular complications (CVC) as well as the likelihood of death. The residual risk of developing CVC in such patients is largely determined by the high thrombotic status, that is associated with hypercoagulation characteristic of DM. Hypercoagulation causes activation of both platelet and coagulation pathways, which leads to an increased susceptibility to thrombosis.
View Article and Find Full Text PDFComparing adenosine A receptor modulation of cannabinoid CB receptor-mediated inhibition of GABA and glutamate release in rodent striatal nerve terminals.
Eur J Neurosci
January 2025
CNC-Center for Neuroscience and Cell Biology, University of Coimbra, Coimbra, Portugal.
In corticostriatal nerve terminals, glutamate release is stimulated by adenosine via A receptors (ARs) and simultaneously inhibited by endocannabinoids via CB receptors (CBRs). We previously identified presynaptic AR-CBR heterotetrameric complexes in corticostriatal nerve terminals. We now explored the possible functional interaction between ARs and CBRs in purified striatal GABAergic nerve terminals (synaptosomes) and compared these findings with those on the release of glutamate.
View Article and Find Full Text PDFDirect oral anticoagulants or warfarin in patients with left ventricular thrombus after ST-elevation myocardial infarction: a pilot trial and a prespecified meta-analysis of randomised trials.
EuroIntervention
January 2025
Cardiovascular Medicine Division, Brigham and Women's Hospital, Harvard Medical School, Boston, MA, USA.
Background: The role of direct oral anticoagulants (DOACs) in the treatment of left ventricular thrombus (LVT) after ST-elevation myocardial infarction (STEMI) remains uncertain.
Aims: We aimed to compare the effect of rivaroxaban versus warfarin in patients with STEMI complicated by LVT.
Methods: Adult patients with STEMI and two-dimensional transthoracic echocardiography showing LVT were assigned to rivaroxaban (15 mg once daily) or warfarin (international normalised ratio goal of 2.
High-resolution melting analysis for detection of nucleotide mutation markers in the polymerase-acidic (PA) gene of influenza virus that are associated with baloxavir marboxil resistance.
Arch Virol
January 2025
Department Experimental and Clinical Medicine, University of Florence, Florence, Italy.
The I38T substitution in the influenza virus polymerase-acidic (PA) subunit is a resistance marker of concern for treatment with the antiviral baloxavir marboxil (BXM). Thus, monitoring PA/I38T mutations is of clinical importance. Here, we developed three rapid and sensitive assays for the detection and monitoring of the PA/I38T mutation.
View Article and Find Full Text PDFGYY4137 ameliorates blood brain barrier damage by inhibiting autophagy mediated occludin degradation in cardiac arrest and resuscitation.
Sci Rep
January 2025
Department of Anesthesiology, Second Affiliated Hospital of Harbin Medical University, 246 Xuefu Road, Nangang District, Harbin, 150086, Heilongjiang Province, China.
Cardiopulmonary resuscitation (CPR) after cardiac arrest (CA) is an important cause of neurological impairment and leads to considerable morbidity and mortality. The stability of the blood-brain barrier (BBB) is crucial for minimizing secondary neurological damage and improving long-term prognosis. However, the precise mechanisms and regulatory pathways that contribute to BBB dysfunction after CPR remain elusive.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!