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In the late s Solvay Pharmaceuticals discontinued
2023-08-25
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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The AChR is composed of five homologous
2023-08-25
The AChR is composed of five homologous, membrane-spanning subunits. AChRs containing two α, one β, one δ and one γ subunit (AChRγ) predominate during embryonic development and mice lacking AChRγ die at birth (Takahashi et al., 2002). After birth, the AChRγs are replaced during the first 2 postnatal
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Until now five muscarinic receptor M genes have
2023-08-25
Until now, five muscarinic receptor (M1-5) genes have been cloned, but, M1-3 receptors are functionally recognized in the lungs. Smooth muscle contraction is mainly mediated by M3. M2 may also participate in the contraction via Gi protein which leads to a decrease in cAMP. On the other hand, M2 is l
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hydroxydopamine OHDA is a selective catecholaminergic
2023-08-25
6-hydroxydopamine (6-OHDA) is a selective catecholaminergic neurotoxin mainly used to generate lesions in the nigrostriatal pathway in rats (Ungerstedt, 1968). The most common use of 6-OHDA is via unilateral injection into the rat medial forebrain bundle (MFB). DA depletion, nigral DA cell loss, and
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S63845 Introduction Lipoxygenases LOXs are key enzymes that
2023-08-25
Introduction Lipoxygenases (LOXs) are key enzymes that catalyze the polyunsaturated fatty acids (PUFAs) such as arachidic S63845 (AA), linoleic acid (LA) and others unsaturated fatty acids (Brash, 1999). LOXs are expressed in immune, neural, epithelial, tumor cells and other cells (Claesson, 2009)
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The enzyme Arginase ARG plays a
2023-08-25
The enzyme Arginase 1 (ARG1) plays a role in the hepatic urea cycle by hydrolyzing L-arginine to L-ornithine and urea [13]. In the context of macrophages and MDSCs, ARG1 expression redirects L-arginine metabolism to abolish cytotoxic nitric oxide production [14], suppress T-cell function [15], [16],
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Different antioxidants were described as useful
2023-08-25
Different antioxidants were described as useful biomarkers in monitoring response to treatment in human and veterinary medicine [33,65,66]. In the same line, Thiol and TAC also proved to be useful biomarkers in monitoring the post-ovariohysterectomy period in queens with pyometra, since antioxidants
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Plant tissues were thought to be natural sources
2023-08-25
Plant tissues were thought to be natural sources containing different types of antioxidant compounds (tocopherols, ascorbic acid, carotenoids, and phenolic compounds). As a general classification, antioxidants were grouped as vitamins (ascorbic acid, tocopherols), carotenoids (condensed tannins, xan
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br Experimental section br Abbreviations
2023-08-25
Experimental section Abbreviations PSA, puromycin–sensitive aminopeptidase; APN, aminopeptidase N; AML, acute myeloid Leukemia; ALL, acute lymphoblastic leukemia; AADR, amino Fmoc-Lys(Dnp)-OH deprivation response; PAN, puromycin aminonucleoside; DCC, dicyclohexyl carbodiimide; NHS, N–hydroxy
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A unique finding in this study is that LO
2023-08-25
A unique finding in this study is that 12/15-LO influences CREB phosphorylation in the murine brain. While previous reports have found that knockout of 5-lipoxygenase, a related enzyme that also uses arachidonic Fmoc-Val-OH for substrate, can regulate CREB phosphoryation in the context of Alzheimer
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Spectroscopic techniques are powerful biophysical tools
2023-08-25
Spectroscopic techniques are powerful biophysical tools used in the study of biomolecular structures, including those of proteins. UV–Vis nm to lb spectroscopy makes use of absorption property of the protein peptide backbone at around 218 nm, and aromatic amino acid residues primarily at around 280
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To investigate further the clinical and
2023-08-24
To investigate further the clinical and mutational spectrum associated with -related dyskinesia, we here performed a screen in a large series of patients affected with an unexplained hyperkinetic movement disorder, resulting in the identification of 2 pediatric patients presenting with a novel pheno
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Endogenous adenosine systems have largely
2023-08-24
Endogenous adenosine systems have largely been implicated in drug actions by the demonstration that caffeine (non-selective A1R and A2AR antagonist) (see Section The issue of caffeine), in doses up to 7.5–10mg/kg, inhibits antinociception, and when this occurs, it Adenosine is generally also seen w
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br Conclusions and clinical relevance Astrogliosis and an in
2023-08-24
Conclusions and clinical relevance Astrogliosis and an increase in ADK is a pathologcial hallmark of epilepsy. The consequence of increased ADK in the epileptic heat shock protein inhibitors is a decrease in the ambient adenosine tone and A1R activity. As a result, systemic administration of A1R
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Our analysis demonstrated that ADA
2023-08-24
Our analysis demonstrated that ADA is a transpicuous and rapid test with high sensitivity and specificity for diagnosis of TBM decidedly. The summary sensitivity and specificity were 0.89 and 0.91 respectively, indicating a sufficient level for overall diagnostic accuracy. The modality of SROC curve
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