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https://www.readbyqxmd.com/read/28817686/use-of-phosphodiesterase-inhibitors-and-prevalence-of-self-reported-glaucoma-in-the-united-states
#1
Stephanie P Chen, Kuldev Singh, Shan C Lin
OBJECTIVE: While decreased ocular blood flow is thought to be a possible contributor to glaucoma pathogenesis, it is unclear what role systemic phosphodiesterase inhibitors (PDEi) play. We performed a cross-sectional study of a nationally representative sample of the U.S. population to investigate the relationship between the most commonly used PDEi, sildenafil and theophylline, and self-reported glaucoma. METHODS: We used the National Health and Nutrition Examination Survey 2005-2008 cycles for this observational study...
2017: PloS One
https://www.readbyqxmd.com/read/28817484/levosimendan-in-acute-and-advanced-heart-failure-an-appraisal-of-the-clinical-database-and-evaluation-of-its-therapeutic-applications
#2
J Altenberger, F Gustafsson, V-P Harjola, K Karason, D Kindgen-Milles, M Kivikko, G Malfatto, Z Papp, J Parissis, P Pollesello, G Pölzl, C Tschöpe
The use of inotropes for correcting haemodynamic dysfunction in patients with congestive heart failure has been described over many decades. However, negative or insufficient data have been collected regarding the effects of cardiac glycosides, catecholamines and phosphodiesterase inhibitors on quality of life and survival. More recently, the calcium sensitizer and potassium channel-opener levosimendan has been proposed as a safer inodilator than traditional agents in some heart failure settings, such as Advanced Heart Failure...
August 15, 2017: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/28811831/potent-phosphodiesterase-inhibition-and-nitric-oxide-release-stimulation-of-anti-impotence-thai-medicinal-plants-from-manosroi-iii-database
#3
Aranya Manosroi, Theeraphong Tangjai, Charinya Chankhampan, Worapaka Manosroi, Yaravee Najarut, Worapong Kitdamrongtham, Jiradej Manosroi
Seven plants in the top rank were selected from the "MANOSROI III" database using the two Thai keywords which meant impotence and sexual tonic. Boesenbergia rotunda (L.) Mansf. extract [EDP1-001(1)] gave the highest PDE inhibition activity of 4.36-fold sildenafil, a standard anti-impotence drug. Plumbago indica Linn. extract [EDP2-001(1)] exhibited the highest NO release stimulation activity of 666.85% which was 1.50-fold acetylcholine, a standard drug. Most selected plant extracts were nontoxic to EA.hy926 cells at 1...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/28799255/synergy-between-5-ht4-receptor-stimulation-and-phosphodiesterase-4-inhibition-in-facilitating-acetylcholine-release-in-human-large-intestinal-circular-muscle
#4
V Pauwelyn, W Ceelen, R A Lefebvre
BACKGROUND: Gastroprokinetic properties of 5-HT4 receptor agonists, such as prucalopride, are attributed to activation of 5-HT4 receptors on cholinergic nerves innervating smooth muscle in the gastrointestinal smooth muscle layer, increasing acetylcholine release and muscle contraction. In porcine stomach and colon, phosphodiesterase (PDE) 4 has been shown to control the signaling pathway of these 5-HT4 receptors. The aim of this study was to investigate the PDE-mediated control of these 5-HT4 receptors in human large intestine...
August 10, 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/28798396/flavonoid-glycosides-isolated-from-epimedium-brevicornum-and-their-estrogen-biosynthesis-promoting-effects
#5
Fu Li, Bao-Wen Du, Dan-Feng Lu, Wen-Xuan Wu, Kanjana Wongkrajang, Lun Wang, Wen-Chen Pu, Chang-Lu Liu, Han-Wei Liu, Ming-Kui Wang, Fei Wang
Epimedium brevicornum Maxim has a long history of use in the treatment of estrogen deficiency-related diseases. However, the chemical constituents and mechanism of action of this medicinal plant are not fully understood. In the present study, we isolated four new isoprenylated flavonoid glycosides, as well as 16 known flavonoids (13 isoprenylated flavonoids), from this plant. The chemical structures of the new flavonoid glycosides were elucidated by extensive spectroscopic analysis. The new compounds 1-4 were potent promoters of estrogen biosynthesis in human ovarian granulosa-like KGN cells...
August 10, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28798156/phosphodiesterase-4-inhibitor-and-phosphodiesterase-5-inhibitor-combination-therapy-has-antifibrotic-and-anti-inflammatory-effects-in-mdx-mice-with-duchenne-muscular-dystrophy
#6
Yasunori Nio, Masayuki Tanaka, Yoshihiko Hirozane, Yo Muraki, Mitsugi Okawara, Masatoshi Hazama, Takanori Matsuo
Duchenne muscular dystrophy (DMD) is the most common inherited muscular dystrophy. Patients experience DMD in their 20s from cardiac or respiratory failure related to progressive muscle wasting. Currently, the only treatments for the symptoms of DMD are available. Muscle fibrosis, a DMD feature, leads to reduced muscle function and muscle mass, and hampers pharmaceutical therapeutic efficacy. Although antifibrotic agents may be useful, none is currently approved. Phosphodiesterase (PDE)-4 inhibitors have exhibited antifibrotic effects in human and animal models...
August 10, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28796496/discovery-of-clinical-candidate-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-a-highly-potent-selective-and-brain-penetrating-phosphodiesterase-2a-inhibitor-for-the-treatment
#7
Satoshi Mikami, Shinji Nakamura, Tomoko Ashizawa, Izumi Nomura, Masanori Kawasaki, Shigekazu Sasaki, Hideyuki Oki, Hironori Kokubo, Isaac D Hoffman, Hua Zou, Noriko Uchiyama, Kosuke Nakashima, Naomi Kamiguchi, Haruka Imada, Noriko Suzuki, Hiroki Iwashita, Takahiko Taniguchi
Phosphodiesterase (PDE) 2A inhibitors have emerged as a novel mechanism with potential therapeutic option to ameliorate cognitive dysfunction in schizophrenia or Alzheimer's disease through upregulation of cyclic nucleotides in the brain, and thereby achieve potentiation of cyclic nucleotide signaling pathways. This article details the expedited optimization of our recently disclosed pyrazolo[1,5-a]pyrimidine lead compound 4b, leading to the discovery of clinical candidate 36 (TAK-915), which demonstrates an appropriate combination of potency, PDE selectivity, and favorable pharmacokinetic (PK) properties, including brain penetration...
August 10, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28794467/tdp2-suppresses-chromosomal-translocations-induced-by-dna-topoisomerase-ii-during-gene-transcription
#8
Fernando Gómez-Herreros, Guido Zagnoli-Vieira, Ioanna Ntai, María Isabel Martínez-Macías, Rhona M Anderson, Andrés Herrero-Ruíz, Keith W Caldecott
DNA double-strand breaks (DSBs) induced by abortive topoisomerase II (TOP2) activity are a potential source of genome instability and chromosome translocation. TOP2-induced DNA double-strand breaks are rejoined in part by tyrosyl-DNA phosphodiesterase 2 (TDP2)-dependent non-homologous end-joining (NHEJ), but whether this process suppresses or promotes TOP2-induced translocations is unclear. Here, we show that TDP2 rejoins DSBs induced during transcription-dependent TOP2 activity in breast cancer cells and at the translocation 'hotspot', MLL...
August 10, 2017: Nature Communications
https://www.readbyqxmd.com/read/28782191/tadalafil-a-phosphodiesterase-type-5-inhibitor-improves-bladder-blood-supply-and-restores-the-initial-phase-of-lower-urinary-tract-dysfunction-in-diabetic-rats
#9
Daisuke Gotoh, Kazumasa Torimoto, Yoshihiro Tatsumi, Shunta Hori, Atsushi Yamada, Makito Miyake, Yosuke Morizawa, Katsuya Aoki, Nobumichi Tanaka, Akihide Hirayama, Kiyohide Fujimoto
AIMS: To investigate the effect of tadalafil on bladder blood flow and lower urinary tract function in a rat model of diabetes. MATERIALS AND METHODS: We studied female Sprague-Dawley rats and induced diabetes in some using a single intraperitoneal injection of streptozotocin. We divided the rats into nondiabetes (ND), diabetes (D), and diabetes with tadalafil (DT) groups. The rats were raised for an additional 7 weeks after diabetes induction. The DT group received oral tadalafil (2 mg/kg/day) for 7 days before the experiments...
August 7, 2017: Neurourology and Urodynamics
https://www.readbyqxmd.com/read/28781213/quality-of-life-and-sexual-function-benefits-of-long-term-testosterone-treatment-longitudinal-results-from-the-registry-of-hypogonadism-in-men-rhyme
#10
Raymond C Rosen, Frederick Wu, Hermann M Behre, Hartmut Porst, Eric J H Meuleman, Mario Maggi, Javier Romero-Otero, Juan I Martinez-Salamanca, Thomas Hugh Jones, Frans M J Debruyne, Karl-Heinz Kurth, Geoff I Hackett, Richard Quinton, Peter Stroberg, Yacov Reisman, Edoardo S Pescatori, Antonio Morales, Lluis Bassas, Natalio Cruz, Glenn R Cunningham, Olivia A Wheaton
BACKGROUND: The benefits and risks of long-term testosterone administration have been a topic of much scientific and regulatory interest in recent years. AIM: To assess long-term quality of life (QOL) and sexual function benefits of testosterone replacement therapy (TRT) prospectively in a diverse, multinational cohort of men with hypogonadism. METHODS: A multinational patient registry was used to assess long-term changes associated with TRT in middle-age and older men with hypogonadism...
August 3, 2017: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/28769012/in-vitro-p-glycoprotein-mediated-transport-of-tadalafil-a-comparison-with-sildenafil
#11
Hiroki Higashi, Nao Watanabe, Rika Tamura, Masato Taguchi
Tadalafil and sildenafil are selective inhibitors of phosphodiesterase type 5, showing marked pharmacokinetic variability in patients with pulmonary arterial hypertension. It has been reported that sildenafil is a substrate for P-glycoprotein (P-gp), but whether tadalafil is a substrate for P-gp remains to be determined. The objective of the present study was to elucidate whether tadalafil is a substrate for P-gp. Transcellular transport of sildenafil and tadalafil (5 µM each) was examined using renal epithelial LLC-PK1 and P-gp-expressing LLC-GA5-COL150 cell monolayers...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28760246/efficacy-and-safety-of-a-fixed-dose-combination-therapy-of-tamsulosin-and-tadalafil-for-patients-with-lower-urinary-tract-symptoms-and-erectile-dysfunction-results-of-a-randomized-double-blinded-active-controlled-trial
#12
Sae Woong Kim, Nam Cheol Park, Seung Wook Lee, Dae Yul Yang, Jong Kwan Park, Du Geon Moon, Sang-Kuk Yang, Sung Won Lee, Ki Hak Moon, Tai Young Ahn, Soo Woong Kim, Kwangsung Park, Kweon Sik Min, Ji-Kan Ryu, Hankil Son, Jina Jung, Jae Seog Hyun
BACKGROUND: Phosphodiesterase type 5 inhibitors and α-adrenergic blocking agents (α-blockers) are widely used for the treatment of erectile dysfunction (ED) and lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH). AIMS: To assess the efficacy and safety of fixed-dose combinations (FDCs) of tamsulosin and tadalafil compared with tadalafil monotherapy in patients with comorbid BPH-associated LUTS and ED. METHODS: A randomized, double-blinded, active-controlled trial was conducted of 510 men with BPH-associated LUTS and ED...
August 2017: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/28759228/discovery-of-an-orally-bioavailable-brain-penetrating-in-vivo-active-phosphodiesterase-2a-inhibitor-lead-series-for-the-treatment-of-cognitive-disorders
#13
Satoshi Mikami, Shigekazu Sasaki, Yasutomi Asano, Osamu Ujikawa, Shoji Fukumoto, Kosuke Nakashima, Hideyuki Oki, Naomi Kamiguchi, Haruka Imada, Hiroki Iwashita, Takahiko Taniguchi
Herein, we describe the discovery of a potent, selective, brain-penetrating, in vivo active phosphodiesterase (PDE) 2A inhibitor lead series. To identify high-quality leads suitable for optimization and enable validation of the physiological function of PDE2A in vivo, structural modifications of the high-throughput screening hit 18 were performed. Our lead generation efforts revealed three key potency-enhancing functionalities with minimal increases in molecular weight (MW) and no change in topological polar surface area (TPSA)...
July 31, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28756610/treatment-of-obesity-associated-overactive-bladder-by-the-phosphodiesterase-type-4-inhibitor-roflumilast
#14
Honglin Ding, Ning Li, Xiaoning He, Bing Liu, Liming Dong, Yili Liu
PURPOSE: To prove that phosphodiesterase type-4 inhibitors could potentially treat obesity-associated overactive bladder through modulation of the systemic inflammatory response. METHODS: In this 12-week study, 90 female Sprague-Dawley rats were divided into three groups: (1) vehicle-treated normal diet (ND)-fed rats; (2) vehicle-treated high-fat diet (HFD)-fed rats; and (3) roflumilast-treated HFD-fed rats. Oral roflumilast (5 mg/kg/day) was administered during the last 4 weeks of HFD feeding in the test group...
July 29, 2017: International Urology and Nephrology
https://www.readbyqxmd.com/read/28753810/validation-of-cyclic-adenosine-monophosphate-phosphodiesterase-4d7-for-its-independent-contribution-to-risk-stratification-in-a-prostate-cancer-patient-cohort-with-longitudinal-biological-outcomes
#15
Marcia Alves de Inda, Dianne van Strijp, Eveline den Biezen-Timmermans, Anne van Brussel, Janneke Wrobel, Hans van Zon, Pieter Vos, George S Baillie, Pierre Tennstedt, Thorsten Schlomm, Miles D Houslay, Chris Bangma, Ralf Hoffmann
BACKGROUND: The clinical metrics used to date to assess the progression risk of newly diagnosed prostate cancer patients only partly represent the true biological aggressiveness of the underlying disease. OBJECTIVE: Validation of the prognostic biomarker phosphodiesterase-4D7 (PDE4D7) in predicting longitudinal biological outcomes in a historical surgery cohort to improve postsurgical risk stratification. DESIGN, PATIENTS, AND METHODS: RNA was extracted from biopsy punches of resected tumors from 550 patients...
June 13, 2017: European Urology Focus
https://www.readbyqxmd.com/read/28753652/the-phosphodiesterase-inhibitor-ibudilast-attenuates-neuroinflammation-in-the-mptp-model-of-parkinson-s-disease
#16
Joanna Schwenkgrub, Malgorzata Zaremba, Ilona Joniec-Maciejak, Agnieszka Cudna, Dagmara Mirowska-Guzel, Iwona Kurkowska-Jastrzębska
BACKGROUND/AIMS: Since the degeneration of the nigrostriatal dopaminergic pathway in Parkinson's disease (PD) is associated with the inflammation process and decreased levels of cyclic nucleotides, inhibition of up-regulated cyclic nucleotide phosphodiesterases (PDEs) appears to be a promising therapeutic strategy. We used ibudilast (IBD), a non-selective PDE3,4,10,11 inhibitor, due to the abundant PDE 4 and 10 expression in the striatum. The present study for the first time examined the efficacy of IBD in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mouse model of PD...
2017: PloS One
https://www.readbyqxmd.com/read/28748375/attenuation-of-ethanol-abstinence-induced-anxiety-and-depressive-like-behavior-by-the-phosphodiesterase-4-inhibitor-rolipram-in-rodents
#17
Mei-Fang Gong, Rui-Ting Wen, Ying Xu, Jian-Chun Pan, Ning Fei, Yan-Meng Zhou, Jiang-Ping Xu, Jian-Hui Liang, Han-Ting Zhang
RATIONALE: Withdrawal symptoms stand as a core feature of alcohol dependence. Our previous results have shown that inhibition of phosphodiesterase-4 (PDE4) decreased ethanol seeking and drinking in alcohol-preferring rodents. However, little is known about whether PDE4 is involved in ethanol abstinence-related behavior. OBJECTIVE: The objective of this study was to characterize the role of PDE4 in the development of anxiety- and depressive-like behavior induced by abstinence from ethanol exposure in different animal models...
July 27, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28744631/effects-of-fullerene-derivatives-on-activity-of-ca-2-atpase-of-the-sarcoplasmic-reticulum-and-cgmp-phosphodiesterase
#18
L V Tat'yanenko, E A Khakina, A V Zhilenkov, P A Troshin, O V Dobrokhotova, I Yu Pikhteleva, A I Kotel'nikov
We studied the effects of new water-soluble polysubstituted fullerene C60 (PFD) derivatives on activity of Ca(2+)-Mg(2+) ATPase of the sarcoplasmic reticulum and cGMP phosphodiesterase. All examined fullerene derivatives inhibited activity of both enzymes. For instance, PFD-I, PFD-II, PFD-III, PFD-V, PFD-IX, PFD-X, and PFD-XI in a concentration of 5×10(-5) M completely inhibited hydrolytic and transport functions of Ca(2+)-ATPase. These compounds in a concentration of 5×10(-6) suppressed active transport of calcium ions by 51±5, 77±8, 52±5, 52±5, 100±10, 80±8, and 100±10%, respectively, and inhibited ATP hydrolysis by 31±3, 78±8, 18±2, 29±3, 78±8, 63±7, and 73±9%, respectively, uncoupling the hydrolytic and transport functions of the enzyme...
July 25, 2017: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28743736/sfpq-a-multifunctional-nuclear-protein-regulates-the-transcription-of-pde3a
#19
Dong Keun Rhee, Steven C Hockman, Sun-Kyung Choi, Yong-Eun Kim, Chungoo Park, Vincent C Manganiello, Kee Kwang Kim
Phosphodiesterase 3A (PDE3A), a member of the cGMP-inhibited cyclic nucleotide phosphodiesterase (PDE) family, plays important roles in oocyte maturation and vascular smooth muscle cell proliferation. However, the molecular mechanisms that regulate PDE3A gene expression remain largely unknown. In this study, we investigated the transcriptional regulation of PDE3A , and found that the splicing factor proline and glutamine rich (SFPQ) protein modulated PDE3A mRNA levels. Multiple transcription start sites (TSS1, 2, and 3) were identified within the first exon of PDE3A using 5'-rapid amplification of cDNA ends (RACE)...
July 25, 2017: Bioscience Reports
https://www.readbyqxmd.com/read/28709568/current-and-emerging-topical-therapies-for-atopic-dermatitis
#20
Jeremy Udkoff, Andrea Waldman, Jusleen Ahluwalia, Jenna Borok, Lawrence F Eichenfield
The pathogenesis of atopic dermatitis (AD) involves epidermal barrier dysfunction and T helper cell type 2 (Th2) lymphocyte-driven inflammation. Cytokines, such as interleukin 4 (IL-4) and IL-13, are important in this reaction. They stimulate B cells to produce immunoglobulin E, causing atopic disease. This process has been well characterized, and new therapies for AD, such as phosphodiesterase 4 (PDE-4) inhibitors, Th2-expressed chemoattractant receptor-homologous molecule antagonists, and Janus kinase inhibitors, work by antagonizing this cellular pathway...
July 2017: Clinics in Dermatology
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