Showing 1-30 of 292 results for "R6520"
Elisabeth Wigenstam et al.
Toxicology, 328, 40-47 (2014-12-17)
Chlorine (Cl2) causes tissue damage and a neutrophilic inflammatory response in the airways manifested by pronounced airway hyperreactivity (AHR). The importance of early anti-inflammatory treatment has previously been addressed. In the previous study, both high-dose and low-dose of dexamethasone (DEX)...
Tiina Keränen et al.
Cytokine, 94, 1-7 (2017-02-07)
Hee Jae Lee et al.
International journal of molecular sciences, 20(17) (2019-08-30)
The purpose of this study is to investigate whether nicotinamide riboside (NR) can improve inflammation and cognitive function in diabetic mice. ICR male mice were fed for 14 weeks with either high-fat chow diet (HF, 60% kcal fat) or standard...
Tae-Wook Kang et al.
Scientific reports, 4, 5546-5546 (2014-07-06)
Glioblastoma multiforme is the most common malignant brain tumor in adults, with an average survival of less than one year due to its resistance to therapy. Recent studies reported that GBM initiates from CD133-expressing cancer stem cells (CSC). However, the...
Belén Mollá et al.
Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics, 16(2), 432-449 (2019-02-15)
Friedreich's ataxia (FRDA) is a neurodegenerative disorder caused by an unstable GAA repeat expansion within intron 1 of the FXN gene and characterized by peripheral neuropathy. A major feature of FRDA is frataxin deficiency with the loss of large sensory...
Emmanuelle Motte et al.
Molecular and cellular endocrinology, 442, 1-11 (2016-12-03)
In acrodysostosis without hormone resistance, a disease caused by phosphodiesterase (PDE)-4D mutations, increased PDE activity leads to bone developmental defects but with normal renal responses to PTH. To identify potential mechanisms for these disparate responses, we compared the effect of...
B R Choi et al.
International journal of impotence research, 27(6), 225-232 (2015-10-09)
The objective was to investigate the cellular effect and action mechanism of Artemisia capillaris extract (ACE) and its component, scopoletin, on penile corpus cavernosum smooth muscle (PCCSM). In vitro study with PCCSM, the precontracted PCCSM with phenylephrine was treated with...
Xiaonan Liang et al.
Neuroscience letters, 677, 14-18 (2018-04-22)
Opioid-induced respiratory depression is a major obstacle to improving the clinical management of moderate to severe chronic pain. Opioids inhibit neuronal activity via various pathways, including calcium channels, adenylyl cyclase, and potassium channels. Currently, the underlying molecular pathway of opioid-induced...
Shailesh R Agarwal et al.
Frontiers in pharmacology, 9, 332-332 (2018-05-10)
Aim: Confining cAMP production to discrete subcellular locations makes it possible for this ubiquitous second messenger to elicit unique functional responses. Yet, factors that determine how and where the production of this diffusible signaling molecule occurs are incompletely understood. The...
Zhuoran Wang et al.
Aging, 10(9), 2394-2406 (2018-09-19)
Rolipram is a selective phosphodiesterase 4 (PDE4) inhibitor that exerts a variety of effects, including anti-inflammatory, immunosuppressive, and anti-tumor effects. The aim of this study was to investigate the effect of rolipram on metabolic disorder and its underlying mechanisms. Metabolic...
Miaojun Lai et al.
The international journal of neuropsychopharmacology, 17(9), 1397-1407 (2014-05-17)
Inhibition of phosphodiesterase-4 (PDE4), an enzyme that specifically hydrolyzes cyclic adenosine monophosphate (cAMP) increases intracellular cAMP/cAMP-response element binding protein (CREB) signaling. Activation of this signaling is considered as an important compensatory response that decreases motivational properties of drugs of abuse....
Yulu Wang et al.
Frontiers in cell and developmental biology, 8, 599389-599389 (2020-12-29)
A global, quantitative proteomics/systems-biology analysis of the selective pharmacological inhibition of phosphodiesterase-4D (PDE4D) revealed the differential regulation of pathways associated with neuroplasticity in memory-associated brain regions. Subtype selective inhibitors of PDE4D bind in an allosteric site that differs between mice...
Clementine J J van Zeijl et al.
American journal of physiology. Endocrinology and metabolism, 307(6), E527-E537 (2014-08-15)
Thyrostimulin, a putative glycoprotein hormone, comprises the subunits GPA2 and GPB5 and activates the TSH receptor (TSHR). The observation that proinflammatory cytokines stimulate GPB5 transcription suggested a role for thyrostimulin in the pathogenesis of nonthyroidal illness syndrome (NTIS). In the...
Laura Rinaldi et al.
Nature communications, 10(1), 2572-2572 (2019-06-14)
Activation of G-protein coupled receptors elevates cAMP levels promoting dissociation of protein kinase A (PKA) holoenzymes and release of catalytic subunits (PKAc). This results in PKAc-mediated phosphorylation of compartmentalized substrates that control central aspects of cell physiology. The mechanism of...
Lamei Yu et al.
European journal of pharmacology, 829, 54-62 (2018-04-14)
This study aimed to determine the effects of levosimendan, a calcium sensitizer, on atrial contractility and atrial natriuretic peptide (ANP) secretion and its modification in hypertrophied atria. Isolated perfused beating rat atria were used from control and isoproterenol-treated rats. Levosimendan...
Mohammad Abdur Rashid et al.
Neuropharmacology, 102, 174-185 (2015-11-21)
Previous studies demonstrated that prenatal exposure to ethanol interferes with embryonic and fetal development, and causes abnormal neurodevelopment. Docosahexaenoic acid (DHA), an omega-3 polyunsaturated fatty acid highly enriched in the brain, was shown to be essential for proper brain development...
Silja Meier et al.
European journal of pharmacology, 812, 174-183 (2017-07-13)
We have previously shown that the natriuretic peptide receptor B (NPR-B) agonist C-type natriuretic peptide (CNP) enhances cyclic adenosine 3´,5´-monophosphate (cAMP)-mediated signaling in failing hearts, through cyclic guanosine 3´,5´-monophosphate (cGMP)-mediated phosphodiesterase (PDE) 3 inhibition. As several signaling pathways are importantly...
Markus Fehrholz et al.
PloS one, 9(5), e97357-e97357 (2014-05-16)
Caffeine administration is an important part of the therapeutic treatment of bronchopulmonary dysplasia (BPD) in preterm infants. However, caffeine mediated effects on airway remodelling are still undefined. The TGF-β/Smad signalling pathway is one of the key pathways involved in airway...
Marcella Brescia et al.
International journal of molecular sciences, 21(19) (2020-10-01)
Duchenne muscular dystrophy (DMD) is the most frequent and severe form of muscular dystrophy. The disease presents with progressive body-wide muscle deterioration and, with recent advances in respiratory care, cardiac involvement is an important cause of morbidity and mortality. DMD...
Amy E Dunne et al.
American journal of respiratory cell and molecular biology, 60(4), 445-453 (2018-11-06)
Neutrophilic inflammation is characteristic of chronic obstructive pulmonary disease (COPD); yet, there are no effective antiinflammatory therapies. The PDE4 inhibitor roflumilast is approved for use in COPD and suppresses sputum neutrophilia. The mechanism underlying this observation is unclear; therefore, this...
Vanessa Vezzi et al.
Scientific reports, 10(1), 9111-9111 (2020-06-06)
Vasopressin receptor 2 (V2R) mutations causing the nephrogenic syndrome of inappropriate antidiuresis (NSIAD) can generate two constitutively active receptor phenotypes. One type results from residue substitutions in several V2R domains and is sensitive to vaptan inverse agonists. The other is...
Artur Świerczek et al.
Pharmaceutical research, 37(2), 19-19 (2020-01-04)
This study aimed to assess the activity of two phosphodiesterase (PDE) inhibitors, namely GRMS-55 and racemic lisofylline ((±)-LSF)) in vitro and in animal models of immune-mediated disorders. Inhibition of human recombinant (hr)PDEs and TNF-alpha release from LPS-stimulated whole rat blood...
Jolanta Wiejak et al.
Biochimica et biophysica acta. Molecular cell research, 1866(2), 264-276 (2018-11-12)
Exchange protein activated by cyclic AMP (EPAC1) suppresses multiple inflammatory actions in vascular endothelial cells (VECs), partly due to its ability to induce expression of the suppressor of cytokine signalling 3 (SOCS3) gene, the protein product of which inhibits interleukin...
Sandra Marie Schaal et al.
PloS one, 7(9), e43634-e43634 (2012-10-03)
The extent of damage following spinal cord injury (SCI) can be reduced by various neuroprotective regimens that include maintaining levels of cyclic adenosine monophosphate (cyclic AMP), via administration of the phosphodiesterase 4 (PDE4) inhibitor Rolipram. The current study sought to...
Mehmet Kürşat Derici et al.
European journal of pharmacology, 844, 118-129 (2018-12-12)
Phosphodiesterase enzymes (PDEs) are responsible for the adjustment of cyclic nucleotide levels. Alterations in PDE expressions in different tissues cause conflicts between functional and clinical effects of PDE inhibitors. Therefore, the aim of this study was to investigate the gene...
Sumita Chakrabarti et al.
Journal of neurochemistry, 152(4), 449-467 (2019-09-04)
We recently demonstrated in rat spinal cord that a regimen of escalating doses of systemic morphine, analogous to regimens used clinically for chronic pain management, selectively up-regulates the mu-opioid receptor (MOR) splice variants MOR-1B2 and MOR-1C1 mRNA and functional protein....
Pojeong Park et al.
Nature communications, 12(1), 413-413 (2021-01-20)
Long-term potentiation (LTP) at hippocampal CA1 synapses can be expressed by an increase either in the number (N) of AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid) receptors or in their single channel conductance (γ). Here, we have established how these distinct synaptic processes...
Loïze Maréchal et al.
Biochimica et biophysica acta, 1861(2), 147-156 (2016-11-12)
Cyclic adenosine monophosphate (cAMP) plays a crucial role as a signaling molecule for sperm functions such as capacitation, motility and acrosome reaction. It is well known that cAMP degradation by phosphodiesterase (PDE) enzyme has a major impact on sperm functions....
Amy Aldrich et al.
Annals of neurology, 80(6), 909-923 (2016-11-03)
Juvenile neuronal ceroid lipofuscinosis (JNCL), or juvenile Batten disease, is a pediatric lysosomal storage disease caused by autosomal recessive mutations in CLN3, typified by blindness, seizures, progressive cognitive and motor decline, and premature death. Currently, there is no treatment for...
Eva Degerman et al.
Acta oto-laryngologica, 137(1), 8-15 (2016-09-30)
The data indicate important roles for phosphodiesterase (PDE) 3, 4, 5, and related cAMP and cGMP pools in the regulation of inner ear fluid homeostasis. Thus, dysfunction of these enzymes might contribute to pathologies of the inner ear. The mechanisms...

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