8-Benzylaminoxanthine scaffold variations for selective ligands acting on adenosine A2A receptors. Design, synthesis and biological evaluation.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.104033
Abstract: A library of 34 novel compounds based on a xanthine scaffold was explored in biological studies for interaction with adenosine receptors (ARs). Structural modifications of the xanthine core were introduced in the 8-position (benzylamino and… read more here.
Keywords: scaffold variations; variations selective; selective ligands; benzylaminoxanthine scaffold ... See more keywords
Discovery of Pyridone-Substituted Triazolopyrimidine Dual A2A/A1 AR Antagonists for the Treatment of Ischemic Stroke
Sign Up to like & getrecommendations! Published in 2022 at "ACS Medicinal Chemistry Letters"
DOI: 10.1021/acsmedchemlett.1c00599
Abstract: Ischemic stroke is a complex systemic disease characterized by high morbidity, disability, and mortality. The activation of the presynaptic adenosine A2A and A1 receptors modifies a variety of brain insults from excitotoxicity to stroke. Therefore,… read more here.
Keywords: a2a; treatment ischemic; a2a antagonists; dual a2a ... See more keywords
CHANGES OF VASCULAR REACTIVITY TO ADENOSINE A1 AND A2A RECEPTOR AGONISTS AFTER HYPERBARIC OXYGENATION
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Hypertension"
DOI: 10.1097/01.hjh.0000838252.80031.88
Abstract: Objective: Hyperbaric oxygenation (HBO) affects vascular reactivitiy, which plays an important role in the pathophysiology of hypertension and other cardiovascular diseases. New data suggest important effects of HBO on oxidative stress and alteration of production… read more here.
Keywords: hbo; a2a; hyperbaric oxygenation; adenosine a2a ... See more keywords
Neuroprotection in the Striatum of Hypoxic-Ischemic Piglets by Simultaneous Inhibition of Dopamine D1 and Adenosine A2A Receptors
Sign Up to like & getrecommendations! Published in 2022 at "Neonatology"
DOI: 10.1159/000524207
Abstract: Introduction: Striatal neurons of term newborns are highly vulnerable to hypoxia-ischemia (H-I). In a piglet model of H-I, a dopamine D1 receptor antagonist and an adenosine A2A receptor antagonist alone preferentially protect striatonigral and striatopallidal… read more here.
Keywords: receptor antagonist; a2a; dopamine; adenosine a2a ... See more keywords
KD-64—A new selective A2A adenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist—Caffeine does not reduce diet-induced obesity in mice
Sign Up to like & getrecommendations! Published in 2020 at "PLoS ONE"
DOI: 10.1371/journal.pone.0229806
Abstract: The A2 adenosine receptors play an important role, among others, in the regulation of inflammatory process and glucose homeostasis in diabetes and obesity. Thus, the presented project evaluated of influence of the selective antagonist of… read more here.
Keywords: non selective; a2a; antagonist; adenosine ... See more keywords
Probing Substituents in the 1- and 3-Position: Tetrahydropyrazino-Annelated Water-Soluble Xanthine Derivatives as Multi-Target Drugs With Potent Adenosine Receptor Antagonistic Activity
Sign Up to like & getrecommendations! Published in 2018 at "Frontiers in Chemistry"
DOI: 10.3389/fchem.2018.00206
Abstract: Tetrahydropyrazino-annelated theophylline (1,3-dimethylxanthine) derivatives have previously been shown to display increased water-solubility as compared to the parent xanthines due to their basic character. In the present study, we modified this promising scaffold by replacing the… read more here.
Keywords: target drugs; tetrahydropyrazino; tetrahydropyrazino annelated; a2a ... See more keywords
Functional Expression of IP, 5-HT4, D1, A2A, and VIP Receptors in Human Odontoblast Cell Line
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DOI: 10.3390/biom13060879
Abstract: Odontoblasts are involved in sensory generation as sensory receptor cells and in dentin formation. We previously reported that an increase in intracellular cAMP levels by cannabinoid 1 receptor activation induces Ca2+ influx via transient receptor… read more here.
Keywords: vip receptors; camp; a2a; intracellular camp ... See more keywords
Non-Invasive Assessment of Locally Overexpressed Human Adenosine 2A Receptors in the Heart of Transgenic Mice
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms23031025
Abstract: A2A adenosine receptors (A2A-AR) have a cardio-protective function upon ischemia and reperfusion, but on the other hand, their stimulation could lead to arrhythmias. Our aim was to investigate the potential use of the PET radiotracer… read more here.
Keywords: adenosine receptors; heart; non invasive; fluda ... See more keywords
The Pharmacological Potential of Adenosine A2A Receptor Antagonists for Treating Parkinson’s Disease
Sign Up to like & getrecommendations! Published in 2022 at "Molecules"
DOI: 10.3390/molecules27072366
Abstract: The adenosine A2A receptor subtype is recognized as a non-dopaminergic pharmacological target for the treatment of neurodegenerative disorders, notably Parkinson’s disease (PD). The selective A2A receptor antagonist istradefylline is approved in the US and Japan… read more here.
Keywords: adenosine a2a; a2a; parkinson disease; a2a receptor ... See more keywords