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PDE 5 Inhibitors

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https://www.readbyqxmd.com/read/29220595/dose-dependent-effects-of-tadalafil-and-roflumilast-on-ovalbumin-induced-airway-hyperresponsiveness-in-guinea-pigs
#1
Anna Urbanova, Ivana Medvedova, Martin Kertys, Pavol Mikolka, Petra Kosutova, Daniela Mokra, Juraj Mokrý
INTRODUCTION: Chronic obstructive diseases of airways associated with cough and/or airway smooth muscle hyperresponsiveness are usually treated with bronchodilating and anti-inflammatory drugs. Recently, selective phosphodiesterase (PDE) 4 inhibitors have been introduced into the therapy of chronic obstructive pulmonary disease. Several studies have demonstrated their ability to influence the airway reactivity and eosinophilic inflammation by increasing the intracellular cAMP concentrations also in bronchial asthma...
December 8, 2017: Experimental Lung Research
https://www.readbyqxmd.com/read/29201504/effect-of-sildenafil-citrate-in-testosterone-induced-benign-prostate-hyperplasia-rat-model
#2
Selahattin Çalışkan, Muzaffer Oğuz Keleş, Metin İshak Öztürk, Musab Ali Kutluhan, Olgu Enis Tok, Feriha Ercan, Muhammet İhsan Karaman
Objective: Efficacy of treatments for benign prostate hyperplasia (BPH) is limited because the disease has complex etiopathogenesis. Recent studies have demonstrated the presence of phosphodiesterase-5 (PDE-5) receptors in prostate tissue. We investigated efficacy of sildenafil citrate in testosteron - induced BPH in rats. Material and methods: The rats were divided into three groups. Each groups had 7 rats. Group 1 was control group. Testosteron propionate 3 mg/kg/day was injected subcutaneously for two weeks in Group 2...
December 2017: Turkish Journal of Urology
https://www.readbyqxmd.com/read/29175000/cyclic-nucleotide-signaling-changes-associated-with-normal-aging-and-age-related-diseases-of-the-brain
#3
REVIEW
Michy P Kelly
Deficits in brain function that are associated with aging and age-related diseases benefit very little from currently available therapies, suggesting a better understanding of the underlying molecular mechanisms is needed to develop improved drugs. Here, we review the literature to test the hypothesis that a break down in cyclic nucleotide signaling at the level of synthesis, execution, and/or degradation may contribute to these deficits. A number of findings have been reported in both the human and animal model literature that point to brain region-specific changes in Galphas (a...
November 23, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/29159668/new-pulmonary-hypertension-model-in-conscious-dogs-to-investigate-pulmonary-selectivity-of-acute-pharmacological-interventions
#4
Thomas Mondritzki, Philip Boehme, Lena Schramm, Julia Vogel, Ilka Mathar, Peter Ellinghaus, Peter Kolkhof, Erwin Bischoff, Jörg Hüser, Wilfried Dinh, Peter Sandner, Hubert Truebel
PURPOSE: Testing of investigational drugs in animal models is a critical step in drug development. Current models of pulmonary hypertension (PH) have limitations. The most relevant outcome parameters such as pulmonary artery pressure (PAP) are measured invasively which requires anesthesia of the animal. We developed a new canine PH model in which pulmonary vasodilators can be characterized in conscious dogs and lung selectivity can be assessed non-invasively. METHODS: Telemetry devices were implanted to measure relevant hemodynamic parameters in conscious dogs...
November 20, 2017: European Journal of Applied Physiology
https://www.readbyqxmd.com/read/29151951/potential-synergistic-effect-of-phosphodiesterase-inhibitors-with-chemotherapy-in-lung-cancer
#5
Kalliopi Domvri, Konstantinos Zarogoulidis, Nikolaos Zogas, Paul Zarogoulidis, Savvas Petanidis, Konstantinos Porpodis, Efrosini Kioseoglou, Wolfgang Hohenforst-Schmidt
Purpose: Lung cancer remains the leading cause of cancer-related deaths worldwide and novel therapeutic approaches targeting crucial pathways are urgently needed to improve its treatment. Differentiation-based therapeutics (Methylxanthines) and phosphodiesterase inhibitors (type 4 and 5), have been implicated in cancer treatment. Our objectives were to capture any potential anti-tumor effect of these drug combinations with chemotherapeutic agents in vitro. Methods: Theophylline as Methylxanthines, Roflumilast as phosphodiesterase type 4 (PDE4) inhibitor and Sildenafil as phosphodiesterase type 5 (PDE5) inhibitor are the drugs that we combined with the chemotherapeutic agents (Docetaxel, Cisplatin and Carboplatin) in vitro...
2017: Journal of Cancer
https://www.readbyqxmd.com/read/29129027/factors-affecting-the-efficacy-and-safety-of-phosphodiesterase-5-inhibitor-and-placebo-in-treatment-for-lower-urinary-tract-symptoms-meta-analysis-and-meta-regression
#6
Hwa Yeon Sun, Bora Lee, Jae Heon Kim
PURPOSE: We aimed to investigate the real benefit and safety of phosphodiesterase 5 inhibitor (PDE 5I) for benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS) by determining the affecting factors and to overcome the previous meta-analysis studies. METHODS: We conducted a systematic review of improvements in LUTS using International Prostate Symptom Score (IPSS), voiding subscore of IPSS (voiding IPSS), storage subscore of IPSS (storage IPSS), quality of life (QoL), maximal urinary flow rate (Qmax), and post-voided residual volume (PVR), and also investigated adverse events and relevant withdrawal rate...
November 11, 2017: International Urology and Nephrology
https://www.readbyqxmd.com/read/29128622/efficacy-and-tolerability-of-pharmacological-interventions-for-pulmonary-arterial-hypertension-a-network-meta-analysis
#7
Hongjing Lin, Mupeng Wang, Ying Yu, Zeyu Qin, Xin Zhong, Jiahui Ma, Fangbo Zhao, Xueli Zhang
PURPOSE: This network meta-analysis (NMA) is designed to compare the efficacy and tolerability of various therapies and combinations for pulmonary arterial hypertension (PAH). METHOD: We conducted a systematic search in databases PubMed, Embase, and Cochrane Library. Treatment efficacy and tolerability were compared by synthesizing direct and indirect evidence. The surface under the curve ranking area was utilized to rank multiple interventions. RESULT: A total of 43 randomized clinical trials were included in our NMA...
November 8, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29101001/icariside-ii-a-pde5-inhibitor-from-epimedium-brevicornum-promotes-neuron-like-pheochromocytoma-pc12-cell-proliferation-via-activating-no-cgmp-pkg-pathway
#8
Jianmei Gao, Yingshu Xu, Ming Lei, Jingshan Shi, Qihai Gong
Icariside II (ICS II), a phosphodiesterase 5 inhibitor (PDE 5-I), is a major ingredient of Epimedium brevicornum, with wide spectrum of neuroprotective properties. However, little is known about the potential beneficial effect of ICS II on neuronal cell proliferation, and its possible underlying mechanism remains still unclear. We hypothesized that the beneficial effect of ICS II on neuron-like highly differentiated rat pheochromocytoma (PC12) cell proliferation is correlated with the nitric oxide (NO) signaling pathway and its upstream of PI3K/AKT pathway...
October 31, 2017: Neurochemistry International
https://www.readbyqxmd.com/read/29093293/discovery-of-a-novel-series-of-pyrazolo-1-5-a-pyrimidine-based-phosphodiesterase-2a-inhibitors-structurally-different-from-n-1s-1-3-fluoro-4-trifluoromethoxy-phenyl-2-methoxyethyl-7-methoxy-2-oxo-2-3-dihydropyrido-2-3-b-pyrazine-4-1h-carboxamide-tak-915-for
#9
Satoshi Mikami, Masanori Kawasaki, Shuhei Ikeda, Nobuyuki Negoro, Shinji Nakamura, Izumi Nomura, Tomoko Ashizawa, Hironori Kokubo, Isaac Dylan Hoffman, Hua Zou, Hideyuki Oki, Noriko Uchiyama, Yuuto Hiura, Maki Miyamoto, Yuuki Itou, Masato Nakashima, Hiroki Iwashita, Takahiko Taniguchi
It has been hypothesized that selective inhibition of phosphodiesterase (PDE) 2A could potentially be a novel approach to treat cognitive impairment in neuropsychiatric and neurodegenerative disorders through augmentation of cyclic nucleotide signaling pathways in brain regions associated with learning and memory. Following our earlier work, this article describes a drug design strategy for a new series of lead compounds structurally distinct from our clinical candidate 2 (TAK-915), and subsequent medicinal chemistry efforts to optimize potency, selectivity over other PDE families, and other preclinical properties including in vitro phototoxicity and in vivo rat plasma clearance...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29089445/novel-imaging-of-the-prostate-reveals-spontaneous-gland-contraction-and-excretory-duct-quiescence-together-with-different-drug-effects
#10
Robert Kügler, Andrea Mietens, Mathias Seidensticker, Sabine Tasch, Florian M Wagenlehner, Andre Kaschtanow, Yudy Tjahjono, Claudia U Tomczyk, Daniela Beyer, Gail P Risbridger, Betty Exintaris, Stuart J Ellem, Ralf Middendorff
Prostate carcinoma and benign prostate hyperplasia (BPH) with associated lower urinary tract symptoms (LUTS) are among the most prevalent and clinically relevant diseases in men. BPH is characterized by an enlargement of prostate tissue associated with increased tone of smooth muscle cells (SMCs) which surround the single glands composing the prostate. Secretions of the glands leave the prostate through local excretory ducts during the emission phase of ejaculation. Pharmacological treatment of BPH suggests different local drug targets based on reduction of prostate smooth muscle tone as the main effect and disturbed ejaculation as a common side effect...
October 31, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/29067241/effect-of-phosphodiesterase-5-inhibitors-on-glycemic-control-in-person-with-type-2-diabetes-mellitus-a-systematic-review-and-meta-analysis
#11
Nalinee Poolsup, Naeti Suksomboon, Nandar Aung
Chronic use of phosphodiesterase-5 inhibitors (PDE-5i) has been shown to improve insulin action on muscle glucose uptake by the prolongation of nitric oxide (NO)/cyclic guanosine monophosphate (cGMP)/protein kinase (PKG) signalling. AIMS: As the effects of PDE-5i on glycemic control in person with type 2 diabetes mellitus (T2DM) have not been systematically explored, we conducted a meta-analysis of available randomized controlled trials (RCTs). METHODS: A literature search was performed through electronic databases including MEDLINE (Pubmed), The Cochrane Library, SCOPUS, Web of Science, CINAHL, www...
December 2016: Journal of Clinical & Translational Endocrinology
https://www.readbyqxmd.com/read/29029361/the-mechanism-of-attenuation-of-epithelial-mesenchymal-transition-by-a-phosphodiesterase-5-inhibitor-via-renal-klotho-expression
#12
Seung Tae Han, Jae Seok Kim, Jun Young Lee, Min Keun Kim, Jin Sae Yoo, Byoung Geun Han, Seung Ok Choi, Jae Won Yang
OBJECTIVES: Phosphodiesterase-5 (PDE-5) inhibitors induces vasodilation in several organs by blocking cyclic GMP (guanosine monophosphate) degradation. However, the existence of alternative mechanism of action in case of an impaired nitric oxide (NO) system remains controversial. Previous studies suggested that decreased NO bioavailability may result in the down-regulation of klotho expression, but the relationship between klotho and NO remains obscure. Therefore, we investigated whether a PDE-5 inhibitor could preserve epithelial mesenchymal transition (EMT) and relationship exists between the NO and renal klotho expression...
October 13, 2017: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/28959341/expression-of-recombinant-phosphodiesterases-3a-and-3b-using-baculovirus-expression-system
#13
Yongmin Yan, Wenqian Jiang, Jingwen Liu, Wenrong Xu, Hui Qian
BACKGROUND: Phosphodiesterase 3A (PDE3A) and phosphodiesterase 3B (PDE3B) play a critical role in the regulation of intracellular level of adenosine 3´,5´-cyclic monophosphate (cyclic AMP, cAMP) and guanosine 3´,5´-cyclic monophosphate (cyclic GMP, cGMP). Subsequently PDE3 inhibitors have shown to relax vascular and inhibit platelet aggregation in cardiovascular disease. OBJECTIVES: In this study, our aim was to establish a method of expression for the recombinant human PDE3A and PDE3B proteins in insect cells using baculovirus expression system in order to investigate the activity of the expressed PDE3A and PDE3B proteins...
December 2016: Iranian Journal of Biotechnology
https://www.readbyqxmd.com/read/28956337/role-of-phosphodiesterases-in-huntington-s-disease
#14
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/28932631/tadalafil-has-biologic-activity-in-human-melanoma-results-of-a-pilot-trial-with-tadalafil-in-patients-with-metastatic-melanoma-tame
#15
Jessica C Hassel, Huanhuan Jiang, Carolin Bender, Julia Winkler, Alexandra Sevko, Ivan Shevchenko, Niels Halama, Antonia Dimitrakopoulou-Strauss, Walter E Haefeli, Dirk Jäger, Alexander Enk, Jochen Utikal, Viktor Umansky
Myeloid-derived suppressor cells (MDSCs) are known to play a critical role in the suppression of T cell antitumor responses. Our preclinical data showed that the phosphodiesterase (PDE)-5 inhibitor sildenafil impaired MDSC functions, enhanced intratumoral T cell activity and prolonged survival of melanoma-bearing mice. In this study, we evaluated biologic effects, safety and efficacy of palliative treatment with the PDE-5 inhibitor tadalafil in metastatic melanoma patients. We conducted an open-label, dose de-escalation trial with tadalafil in pretreated metastatic melanoma patients...
2017: Oncoimmunology
https://www.readbyqxmd.com/read/28903860/a-review-of-synthetic-phosphodiesterase-type-5-inhibitors-pde-5i-found-as-adulterants-in-dietary-supplements
#16
REVIEW
Chee-Leong Kee, Xiaowei Ge, Véronique Gilard, Myriam Malet-Martino, Min-Yong Low
To date, there are 80 synthetic PDE-5i found as adulterants in dietary supplements. Analogues of sildenafil remain as the top list with 50 (62%) and are followed by analogues of tadalafil, 21 (26%), analogues of vardenafil, 7 (9%) and others, 2 (3%). The sildenafil group can be sub-categorized into sulphonamide-bonded (24, 48%), acetyl-bonded (11, 22%), carbonyl or thiocarbonyl-bonded (8, 16%) and other types (7, 14%) based on the functional group linked to pyrazolopyrimidine-one moieties. Meanwhile, analogues of tadalafil have become popularly found as adulterants in dietary supplements like beverages and herbal extracts from 2015 to 2016...
August 9, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28891448/a-special-focus-on-selexipag-treatment-of-pulmonary-arterial-hypertension
#17
Louise Marqvard Sørensen, Markus Wehland, Marcus Krüger, Ulf Simonsen, Mohamed Zakaria Nassef, Manfred Infanger, Daniela Grimm
BACKGROUND: This review focuses on the treatment of pulmonary arterial hypertension (PAH) with selexipag and compares its drug-related therapeutic effects with those of prostacyclin analogues. METHODS: We searched the relevant literature and summarized the current clinical trials concerning selexipag and PAH. RESULTS: With only few cases per million, PAH is a rare disease, but when untreated it can be life threatening. PAH is linked to elevated levels of endothelin (ET-1) and decreased levels of nitric oxide (NO) and prostacyclin (PGI2)...
September 7, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28888986/pde-5-inhibitor-improves-insulin-sensitivity-by-enhancing-mitochondrial-function-in-adipocytes
#18
Hea Min Yu, Hyo Kyun Chung, Koon Soon Kim, Jae Min Lee, Jun Hwa Hong, Kang Seo Park
Adipocytes are involved in many metabolic disorders. It was recently reported that phosphodiesterase type 5 (PDE5) is expressed in human adipose tissue. In addition, PDE5 inhibitors have been shown to improve insulin sensitivity in humans. However, the mechanism underlying the role of PDE5 inhibitors as an insulin sensitizer remains largely unknown. The present study was undertaken to investigate the role of the PDE5 inhibitor udenafil in insulin signaling in adipocytes and whether this is mediated through the regulation of mitochondrial function...
November 4, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28870522/poly-i-c-impairs-no-donor-induced-relaxation-by-overexposure-to-no-via-the-nf-kappa-b-inos-pathway-in-rat-superior-mesenteric-arteries
#19
Makoto Ando, Takayuki Matsumoto, Kumiko Taguchi, Tsuneo Kobayashi
Recent studies have suggested a link between vascular dysfunction and innate immune activation including toll-like receptors (TLRs), but the detailed mechanism remains unclear. Here we investigated whether poly (I:C) [a synthetic double-strand RNA recognized by TLR3, melanoma differentiation-associated gene 5 (MDA5), and retinoic acid-inducible gene I (RIG-I)] affected nitric oxide (NO)/cGMP-related vascular relaxation, one of the major cascades of relaxation, in rat superior mesenteric arteries. Using organ-cultured arteries, we found that poly (I:C) (30μg/mL for approximately 1 day) markedly reduced sodium nitroprusside (SNP)-induced relaxation (vs...
September 1, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28845950/-pde-5-inhibitors-patients-preferences
#20
REVIEW
E A Efremov, E V Kasatonova, Ya I Melnik, A A Nikushina
To date, multidisciplinary approach is commonly used to treat erectile dysfunction (ED), and the first line of ED pharmacotherapy, despite its multiple causes, is phosphodiesterase inhibitors of type 5 (PDE-5). They are considered an effective and well tolerated treatment option [1-4]. Concurrently, sildenafil has the largest evidence base for efficacy and safety [5]. The satisfaction of patients with ED therapy is a complex and personal matter, and there are no clearly established and reliable criteria for showing preferences when choosing a PDE-5...
July 2017: Urologii︠a︡
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