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https://www.readbyqxmd.com/read/29123207/atropine-augments-cardiac-contractility-by-inhibiting-camp-specific-phosphodiesterase-type-4
#1
Ruwan K Perera, Thomas H Fischer, Michael Wagner, Matthias Dewenter, Christiane Vettel, Nadja I Bork, Lars S Maier, Marco Conti, Juergen Wess, Ali El-Armouche, Gerd Hasenfuß, Viacheslav O Nikolaev
Atropine is a clinically relevant anticholinergic drug, which blocks inhibitory effects of the parasympathetic neurotransmitter acetylcholine on heart rate leading to tachycardia. However, many cardiac effects of atropine cannot be adequately explained solely by its antagonism at muscarinic receptors. In isolated mouse ventricular cardiomyocytes expressing a Förster resonance energy transfer (FRET)-based cAMP biosensor, we confirmed that atropine inhibited acetylcholine-induced decreases in cAMP. Unexpectedly, even in the absence of acetylcholine, after G-protein inactivation with pertussis toxin or in myocytes from M2- or M1/3-muscarinic receptor knockout mice, atropine increased cAMP levels that were pre-elevated with the β-adrenergic agonist isoproterenol...
November 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29098911/targeted-treatments-for-hidradenitis-suppurativa-a-review-of-the-current-literature-and-ongoing-clinical-trials
#2
Melody Maarouf, Ashley K Clark, Dylan E Lee, Vivian Y Shi
PURPOSE: Targeted, immune-modulating drugs are at the forefront of therapy for HS, and a comprehensive clinical trial registry is needed to facilitate data pooling and clinical efficacy comparison. MATERIALS AND METHODS: A systematic review of the ClinicalTrials.gov database was searched for planned, in-progress, completed, or terminated trials investigating the effect of targeted biologic therapies for hidradenitis suppurativa (HS). When results of RCTs were not available, case reports or series were included...
November 10, 2017: Journal of Dermatological Treatment
https://www.readbyqxmd.com/read/29098341/acute-administration-of-roflumilast-enhances-sensory-gating-in-healthy-young-humans-in-a-randomized-trial
#3
Pim R A Heckman, Marlies A Van Duinen, Arjan Blokland, Tolga Uz, Jos Prickaerts, Anke Sambeth
INTRODUCTION: Sensory gating is a process involved in early information processing which prevents overstimulation of higher cortical areas by filtering sensory information. Research has shown that the process of sensory gating is disrupted in patients suffering from clinical disorders including attention deficit hyper activity disorder, schizophrenia, and Alzheimer's disease. Phosphodiesterase (PDE) inhibitors have received an increased interest as a tool to improve cognitive performance in both animals and man, including sensory gating...
November 3, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/29076116/crisaborole-ointment-2-a-review-in-mild-to-moderate-atopic-dermatitis
#4
Sheridan M Hoy
Crisaborole ointment 2% (Eucrisa™) is a novel, anti-inflammatory inhibitor of phosphodiesterase 4 (PDE4) that is available in the USA for the topical treatment of mild to moderate atopic dermatitis in patients aged ≥ 2 years. In two short-term (28 days), identically designed, multicentre, phase III studies in this patient population, topical therapy with crisaborole ointment 2% reduced disease severity and pruritus severity compared with vehicle, with the effect established early and sustained over the course of treatment...
October 26, 2017: American Journal of Clinical Dermatology
https://www.readbyqxmd.com/read/29068290/otezla-warts-and-all-racks-up-sales-and-eyes-blockbuster-status
#5
Thomas Reinke
Otezla-the generic name is apremilast-also exploited a new mechanism of action as the first inhibitor of phosphodiesterase 4 (PDE4) that results in increased expression of both anti-inflammatory proteins and reduced expression of their pro-inflammatory counterparts.
October 2017: Managed Care
https://www.readbyqxmd.com/read/29065765/rolipram-loaded-polymeric-micelle-nanoparticle-reduces-secondary-injury-after-rat-compression-spinal-cord-injury
#6
Christian Macks, So-Jung Gwak, Michael Lynn, Jeoung Soo Lee
Among the complex pathophysiological events following spinal cord injury, one of the most important molecular level consequences is a dramatic reduction in neuronal cyclic adenosine monophosphate (cAMP) levels. Many studies shown that rolipram (Rm), a phosphodiesterase IV (PDE4) inhibitor, can protect against secondary cell death, reduce inflammatory cytokine levels and immune cell infiltration, and increase white matter sparing and functional improvement. Previously, we developed a polymeric micelle nanoparticle, (poly (lactide-co-glycolide)-g-polyethylenimine, PgP) for combinatorial delivery of therapeutic nucleic acids (TNAs) and drugs for SCI repair...
October 25, 2017: Journal of Neurotrauma
https://www.readbyqxmd.com/read/29063440/the-future-of-atopic-dermatitis-treatment
#7
Nupur Patel, Lindsay C Strowd
In recent years, there has been a growing movement towards the use of targeted therapies in treating of atopic dermatitis (AD), parallel to that which has occurred in psoriasis. Among the systemic medications being studied are subcutaneous or intravenously administered biologic drugs targeting specific molecules such as IL4, IL13, IL17, and IgE. Non-biologic oral therapies are also being developed for AD and include small molecule drugs targeting phosphodiesterase type IV (PDE4) inhibition or Janus Kinase (JAK) inhibition...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/28994166/newer-treatments-of-psoriasis-regarding-il-23-inhibitors-phosphodiesterase-4-inhibitors-and-janus-kinase-inhibitors
#8
REVIEW
Dominika Wcisło-Dziadecka, Martyna Zbiciak-Nylec, Ligia Brzezińska-Wcisło, Katarzyna Bebenek, Agata Kaźmierczak
The rapid progress of genetic engineering furthermore opens up new prospects in the therapy of this difficult-to-treat disease. IL-23 inhibitors, phosphodiesterase 4 (PDE4) inhibitors, and Janus kinase (JAK) inhibitors are currently encouraging further research. Two drugs which are IL-23 inhibitors are now in phase III of clinical trials. The aim of the action of both drugs is selective IL-23 inhibition by targeting the p19 subunit. Guselkumab is a fully human monoclonal antibody. Tildrakizumab is a humanized monoclonal antibody, which also belongs to IgG class and is targeted to subunit p19 of interleukin 23 (IL-23)...
October 10, 2017: Dermatologic Therapy
https://www.readbyqxmd.com/read/28956342/genetic-understanding-of-stroke-treatment-potential-role-for-phosphodiesterase-inhibitors
#9
Anjana Munshi, Satrupa Das
Phosphodiesterase (PDE) gene family is a large family having at least 21 genes and multiple versions (isoforms) of the phosphodiesterase enzymes. These enzymes catalyze the inactivation of intracellular mediators of signal transduction such as cAMP and cGMP and therefore, play a pivotal role in various cellular functions. PDE inhibitors (PDEI) are drugs that block one or more of the five subtypes of the PDE family and thereby prevent inactivation of the intracellular cAMP and cGMP by the respective PDE-subtypes...
2017: Advances in Neurobiology
https://www.readbyqxmd.com/read/28956337/role-of-phosphodiesterases-in-huntington-s-disease
#10
Francesca R Fusco, Emanuela Paldino
Huntington's disease (HD) is an autosomal-dominant rare inherited neurodegenerative disease characterized by a wide variety of symptoms encompassing movement, cognition and behaviour. The cause of the disease is a genetic mutation in the huntingtin protein. The mutation leads to an unstable CAG expansion, translated into a polyglutamine domain within the disease protein. Indeed, huntingtin has a CAG/polyglutamine expansion in the range of 6-39 units in normal individuals, whereas it reaches 39-180 units in HD patients...
2017: Advances in Neurobiology
https://www.readbyqxmd.com/read/28956333/the-past-present-and-future-of-phosphodiesterase-4-modulation-for-age-induced-memory-loss
#11
Rolf T Hansen, Han-Ting Zhang
The purpose of this chapter is to highlight the state of progress for phosphodiesterase-4 (PDE4) modulation as a potential therapeutic for psychiatric illness, and to draw attention to particular hurdles and obstacles that must be overcome in future studies to develop PDE4-mediated therapeutics. Pathological and non-pathological related memory loss will be the focus of the chapter; however, we will at times also touch upon other psychiatric illnesses like anxiety and depression. First, we will provide a brief background of PDE4, and the rationale for its extensive study in cognition...
2017: Advances in Neurobiology
https://www.readbyqxmd.com/read/28956332/from-age-related-cognitive-decline-to-alzheimer-s-disease-a-translational-overview-of-the-potential-role-for-phosphodiesterases
#12
Pim R A Heckman, Arjan Blokland, Jos Prickaerts
Phosphodiesterase inhibitors (PDE-Is) are pharmacological compounds enhancing cAMP and/or cGMP signaling. Both these substrates affect neural communication by influencing presynaptic neurotransmitter release and postsynaptic intracellular pathways after neurotransmitter binding to its receptor. Both cAMP and cGMP play an important role in a variety of cellular functions including neuroplasticity and neuroprotection. This chapter provides a translational overview of the effects of different classes of PDE-Is on cognition enhancement in age-related cognitive decline and Alzheimer's disease (AD)...
2017: Advances in Neurobiology
https://www.readbyqxmd.com/read/28956331/phosphodiesterase-4b-as-a-therapeutic-target-for-cognitive-impairment-and-obesity-related-metabolic-diseases
#13
Steven J Clapcote
People in modern, affluent societies are living longer but also becoming increasingly overweight. With increased life expectancy comes increased risk of developing age-related cognitive decline and neurodegenerative diseases, such that an increasing proportion of life may be lived with cognitive impairment as age increases. Obesity is associated with poorer cognitive function in elderly subjects, and often leads to ill-health arising from various complications such as metabolic syndrome and type-2 diabetes mellitus...
2017: Advances in Neurobiology
https://www.readbyqxmd.com/read/28956330/the-pde4-camp-specific-phosphodiesterases-targets-for-drugs-with-antidepressant-and-memory-enhancing-action
#14
Graeme B Bolger
The PDE4 cyclic nucleotide phosphodiesterases are essential regulators of cAMP abundance in the CNS through their ability to regulate PKA activity, the phosphorylation of CREB, and other important elements of signal transduction. In pre-clinical models and in early-stage clinical trials, PDE4 inhibitors have been shown to have antidepressant and memory-enhancing activity. However, the development of clinically-useful PDE4 inhibitors for CNS disorders has been limited by variable efficacy and significant side effects...
2017: Advances in Neurobiology
https://www.readbyqxmd.com/read/28952358/a-new-selaginellin-derivative-and-a-new-triarylbenzophenone-analog-from-the-whole-plant-of-selaginella-pulvinata
#15
Xin Liu, Gui-Hua Tang, Han-Zhuang Weng, Jun-Sheng Zhang, You-Kai Xu, Sheng Yin
Five selaginellin derivatives (1 and 3-6) including a new one, selaginellin T (1), and a new triarylbenzophenone analog, selagibenzophenone A (2), were isolated from the whole plants of Selaginella pulvinata. Their structures were determined by 1D- and 2D-NMR and HR-ESI-MS data. Selagibenzophenone A (2) is the first example of naturally occurring triarylbenzophenone. The results of the phosphodiesterase-4 (PDE4) inhibitory screening assays showed that compounds 1-6 exhibited potent activities with the IC50 values in the range of 1...
September 27, 2017: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/28937238/effects-of-roflumilast-a-phosphodiesterase-4-inhibitor-on-the-lung-functions-in-a-saline-lavage-induced-model-of-acute-lung-injury
#16
P Kosutova, P Mikolka, M Kolomaznik, S Rezakova, A Calkovska, D Mokra
Acute lung injury (ALI) is associated with deterioration of alveolar-capillary lining and transmigration and activation of inflammatory cells. Whereas a selective phosphodiesterase-4 (PDE4) inhibitor roflumilast has exerted potent anti-inflammatory properties, this study evaluated if its intravenous delivery can influence inflammation, edema formation, and respiratory parameters in rabbits with a lavage-induced model of ALI. ALI was induced by repetitive saline lung lavage (30 ml/kg). Animals were divided into 3 groups: ALI without therapy (ALI), ALI treated with roflumilast i...
September 22, 2017: Physiological Research
https://www.readbyqxmd.com/read/28924693/phosphodiesterase-4-inhibition-affects-both-the-direct-and-indirect-pathway-an-electrophysiological-study-examining-the-tri-phasic-response-in-the-substantia-nigra-pars-reticulata
#17
P R A Heckman, J V Schweimer, T Sharp, J Prickaerts, A Blokland
Fronto-striatal circuits constitute the neurobiological basis of many neuropsychiatric disorders. Part of the intracellular signaling within these circuits, including its dopaminergic modulation, is regulated by the cyclic adenosine monophosphate (cAMP)/protein kinase A (PKA) signaling cascade. Based on the overall expression in human fronto-striatal circuitry, we tested the effects of a cAMP selective phosphodiesterase 4 (PDE4) inhibitor on the tri-phasic response in the dorsomedial substantia nigra pars reticulata (SNr) upon stimulation of the infralimbic cortex in rats...
September 18, 2017: Brain Structure & Function
https://www.readbyqxmd.com/read/28922692/phosphodiesterase-4-inhibitors-for-chronic-obstructive-pulmonary-disease
#18
REVIEW
Jimmy Chong, Bonnie Leung, Phillippa Poole
BACKGROUND: Chronic obstructive pulmonary disease (COPD) is associated with cough, sputum production or dyspnoea and a reduction in lung function, quality of life and life expectancy. Apart from smoking cessation, there are no other treatments that slow lung function decline. Roflumilast and cilomilast are oral phosphodiesterase 4 (PDE4) inhibitors proposed to reduce the airway inflammation and bronchoconstriction seen in COPD. This is an update of a Cochrane review first published in 2011 and updated in 2013...
September 19, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28903491/use-of-rat-primary-mesenteric-cells-for-the-prediction-of-pde4-inhibitor-drug-induced-vascular-injury
#19
Mark M Gosink, Robert E Chapin, Dean Wilkie, Scott Davenport, Steven W Kumpf, Bradley E Enerson, Christopher Houle, Petra Koza-Taylor, Todd A Wisialowski, Michael P Lawton
Drug-induced vascular injury (DIVI) in preclinical studies can delay, if not terminate, a drug development program. Clinical detection of DIVI can be very difficult as there are no definitive biomarkers known to reliably detect this disorder in all instances. The preclinical identification of DIVI requires detailed microscopic examination of a wide range of tissues although one of the most commonly affected areas in rats is the mesenteric vasculature. The reason for this predisposition of mesenteric arteries in rats as well as the exact mechanism and cell types involved in the initial development of these lesions have not been fully elucidated...
September 1, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28888661/rational-design-of-conformationally-constrained-oxazolidinone-fused-1-2-3-4-tetrahydroisoquinoline-derivatives-as-potential-pde4-inhibitors
#20
Gaopeng Song, Xiang Zhu, Junhua Li, Dekun Hu, Dongsheng Zhao, Yixian Liao, Juntong Lin, Lian-Hui Zhang, Zi-Ning Cui
Improvement of subtype selectivity of an inhibitor's binding activity using the conformational restriction approach has become an effective strategy in drug discovery. In this study, we applied this approach to PDE4 inhibitors and designed a series of novel oxazolidinone-fused 1,2,3,4-tetrahydroisoquinoline derivatives as conformationally restricted analogues of rolipram. The bioassay results demonstrated the oxazolidinone-fused tetrahydroisoquinoline derivatives exhibited moderate to good inhibitory activity against PDE4B and high selectivity for PDE4B/PDE4D...
September 1, 2017: Bioorganic & Medicinal Chemistry
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