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Showing 1-30 of 309 results for "R6520" within Papers
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.
Tao Zhu et al.
The journal of maternal-fetal & neonatal medicine : the official journal of the European Association of Perinatal Medicine, the Federation of Asia and Oceania Perinatal Societies, the International Society of Perinatal Obstetricians, 33(13), 2166-2175 (2018-10-31)
Objective: Preterm infants are especially vulnerable to intrauterine infection-induced brain injury, which is closely relevant with cognitive deficits and cerebral palsy. Rolipram, a phosphodiesterase-4 inhibitor, can improve cognition in rodents. However, the underlying roles and mechanisms are not well investigated.Methods:
Dan Li et al.
International immunopharmacology, 90, 107176-107176 (2020-11-28)
Roflupram (ROF) is a novel phosphodiesterase 4 inhibitor. We previously found that ROF suppressed the production of pro-inflammatory factors in microglial cells; however, the underlying mechanisms are largely unknown. The present study aimed to elucidate the underlying molecular mechanisms of
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.
Deniz Abat et al.
Journal of pediatric surgery, 53(11), 2261-2265 (2018-05-19)
The aim of the study is to investigate the effect of Rolipram, a selective phosphodiesterase 4 inhibitor, on testicular torsion - detorsion injury. Sixty young male rats were divided into five groups. In each group, the right testes of six
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
Joanna J Gell et al.
Stem cell reports, 14(3), 433-446 (2020-02-16)
The development of an in vitro system in which human primordial germ cell-like cells (hPGCLCs) are generated from human pluripotent stem cells (hPSCs) has been invaluable to further our understanding of human primordial germ cell (hPGC) specification. However, the means to
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
Ju-Ing Shao et al.
Journal of the Chinese Medical Association : JCMA, 82(7), 568-575 (2019-07-06)
Meconium aspiration syndrome (MAS) is a major cause of severe respiratory failure in near- and full-term neonates. Alleviating inflammation is key to successfully treating severe MAS. Phosphodiesterase (PDE) inhibitors are known to play a role in airway smooth muscle relaxation
J L Ortiz et al.
Allergy, 68(1), 64-73 (2012-11-06)
Several clinical studies have shown that smoking in asthmatics and chronic obstructive pulmonary disease patients is closely associated with corticosteroid refractoriness. In this work, we have analyzed glucocorticoid insensitivity in human pulmonary artery endothelial cells (HPAECs) under cigarette smoke extract
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
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
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
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
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
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
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
Joseph R Hedde et al.
Brain, behavior, and immunity, 64, 285-295 (2017-04-26)
Inhibitors of phosphodiesterase-4 (PDE4) have been approved for the treatment of inflammatory disorders, but are associated with dose-limiting nausea and vomiting. These side effects are hypothesized to be mediated by inhibition of the PDE4D isozyme. Here we demonstrate the anti-inflammatory
Min Zhong et al.
Acta pharmacologica Sinica, 36(3), 298-310 (2015-02-11)
Paeoniflorin from Chinese herb Paeoniae Radix has been shown to ameliorate middle cerebral artery occlusion-induced ischemia in rats. The aim of this study was to investigate the mechanisms underlying the neuroprotective action of PF in cultured rat cortical neurons. Primary
Emilie Degagné et al.
The Journal of clinical investigation, 124(12), 5368-5384 (2014-10-28)
Growing evidence supports a link between inflammation and cancer; however, mediators of the transition between inflammation and carcinogenesis remain incompletely understood. Sphingosine-1-phosphate (S1P) lyase (SPL) irreversibly degrades the bioactive sphingolipid S1P and is highly expressed in enterocytes but downregulated in
Shailesh R Agarwal et al.
British journal of pharmacology, 174(16), 2784-2796 (2017-06-13)
Previous studies indicate that prostaglandin EP FRET-based cAMP biosensors were targeted to different subcellular locations of primary human ASM cells. The Epac2-camps biosensor, which expresses throughout the cell, was used to measure bulk cytoplasmic responses. Epac2-MyrPalm and Epac2-CAAX were used
Xiaying Lu et al.
Scientific reports, 10(1), 175-175 (2020-01-15)
Sepsis is typically triggered by an overwhelming systemic inflammatory response to pathogens, and may lead to severe organ dysfunction and/or death. Sepsis consequently has a high mortality rate and a high rate of complications for survivors, despite modern medical advances.
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
Thomas Pham et al.
Cellular and molecular life sciences : CMLS, 80(12), 369-369 (2023-11-22)
Mutations of large conductance Ca2+- and voltage-activated K+ channels (BK) are associated with cognitive impairment. Here we report that CA1 pyramidal neuron-specific conditional BK knock-out (cKO) mice display normal locomotor and anxiety behavior. They do, however, exhibit impaired memory acquisition
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
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.
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
Tianfei Fan et al.
Communications biology, 5(1), 81-81 (2022-01-22)
Hypertension is a common chronic disease, which leads to cardio-cerebrovascular diseases, and its prevalence is increasing. The cyclic adenosine monophosphate (cAMP)-protein kinase A (PKA) pathway participates in multiple cardiovascular diseases. Phosphodiesterase (PDE) 4 has been shown to regulate PKA activity
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