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Phosphodiesterase 5 inhibitors

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https://www.readbyqxmd.com/read/28819824/-update-pulmonary-arterial-hypertension-definitions-diagnosis-therapy
#1
N Sommer, M J Richter, K Tello, F Grimminger, W Seeger, H A Ghofrani, H Gall
The term pulmonary arterial hypertension comprises a group of pulmonary vascular diseases of different etiologies that are characterized by similar precapillary vascular remodeling processes and result in exertional dyspnea and right heart insufficiency. The specific pharmacological treatment approach considers the risk of mortality and phenotypical properties and includes treatment with phosphodiesterase type 5 inhibitors, endothelin receptor antagonists and prostanoids, as well as with more novel substances, such as a soluble guanylyl cyclase stimulator and an oral prostacyclin receptor agonist...
August 17, 2017: Der Internist
https://www.readbyqxmd.com/read/28816715/testosterone-therapy-improves-erectile-function-and-libido-in-hypogonadal-men
#2
Paul J Rizk, Taylor P Kohn, Alexander W Pastuszak, Mohit Khera
PURPOSE OF REVIEW: Erectile dysfunction and decreased libido are common complaints in the older male population. Recent studies have elucidated the role testosterone therapy (TTh) can play in men with low testosterone levels. The aim of this review is to provide an overview of these findings and the utility of TTh. We specifically examine the role of TTh on erectile function, coadministration with phosphodiesterase type 5 inhibitors, and libido. RECENT FINDINGS: Recent publications suggest that TTh improves mild erectile dysfunction, though may be less useful in men with more severe erectile dysfunction...
August 14, 2017: Current Opinion in Urology
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
#3
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
#4
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
#5
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
#6
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/28793090/prevalence-of-erectile-dysfunction-oral-drugs-use-in-a-city-of-southern-brazil
#7
Daniel Vanti Duarte, María Clara Restrepo-Méndez, Mariângela Freitas da Silveira
The last decade has seen a breakthrough in the treatment of erectile dysfunction (ED) with the advent of phosphodiesterase-5 inhibitors. There are few population-based observational studies on the prevalence of use of these drugs. We conducted a cross-sectional population-based study in the city of Pelotas (Brazil). Our sample comprised 1,082 men aged 20 years or older who answered a confidential and self-administered questionnaire. Prevalence of EDD use was 5% (IC95% = 4%;7%). ED and advanced age were strongly associated with a higher prevalence of EDD use...
August 2017: Ciência & Saúde Coletiva
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
#8
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
#9
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/28777888/sildenafil-for-pulmonary-hypertension-in-neonates
#10
REVIEW
Lauren E Kelly, Arne Ohlsson, Prakeshkumar S Shah
BACKGROUND: Persistent pulmonary hypertension in the neonate (PPHN) is associated with high mortality. Currently, the therapeutic mainstay for PPHN consists of assisted ventilation and administration of inhaled nitric oxide (iNO). However, nitric oxide is costly, and its use may not be appropriate in resource-poor settings. Approximately 30% of patients fail to respond to iNO. High concentrations of phosphodiesterases in the pulmonary vasculature have led to the use of phosphodiesterase inhibitors such as sildenafil or milrinone...
August 4, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28776160/-acute-monocular-loss-of-vision-differential-diagnostic-considerations-apart-from-the-internistic-etiological-clarification
#11
A Rickmann, M A Macek, P Szurman, K Boden
We report the case of acute painless monocular loss of vision in a 53-year-old man. An interdisciplinary etiological evaluation remained without pathological findings with respect to arterial branch occlusion. A reevaluation of the patient history led to a possible association with the administration of phosphodiesterase type 5 inhibitor (PDE5 inhibitor). A critical review of the literature on PDE5 inhibitor administration with ocular participation was performed.
August 3, 2017: Der Ophthalmologe: Zeitschrift der Deutschen Ophthalmologischen Gesellschaft
https://www.readbyqxmd.com/read/28776122/mechanisms-involved-in-the-remyelinating-effect-of-sildenafil
#12
Daniela Díaz-Lucena, María Gutierrez-Mecinas, Beatriz Moreno, José Lupicinio Martínez-Sánchez, Paula Pifarré, Agustina García
Remyelination occurs in demyelinated lesions in multiple sclerosis (MS) and pharmacological treatments that enhance this process will critically impact the long term functional outcome in the disease. Sildenafil, a cyclic GMP (cGMP)-specific phosphodiesterase 5 inhibitor (PDE5-I), is an oral vasodilator drug extensively used in humans for treatment of erectile dysfunction and pulmonary arterial hypertension. PDE5 is expressed in central nervous system (CNS) neuronal and glial populations and in endothelial cells and numerous studies in rodent models of neurological disease have evidenced the neuroprotective potential of PDE5-Is...
August 3, 2017: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
https://www.readbyqxmd.com/read/28769012/in-vitro-p-glycoprotein-mediated-transport-of-tadalafil-a-comparison-with-sildenafil
#13
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/28760490/%C3%AE-3-adrenergic-receptor-activation-relaxes-human-corpus-cavernosum-and-penile-artery-through-a-hydrogen-sulfide-cgmp-dependent-mechanism
#14
Emma Mitidieri, Teresa Tramontano, Danila Gurgone, Ciro Imbimbo, Vincenzo Mirone, Ferdinando Fusco, Giuseppe Cirino, Roberta d'Emmanuele di Villa Bianca, Raffaella Sorrentino
Erectile function is a widely accepted indicator of systemic endothelial activity since from a clinical standpoint erectile dysfunction (ED) often precedes cardiovascular events. Recently it has been described a potential role for β3 adrenoceptor in cardiovascular diseases emphasizing a possible development of new drugs. β3 adrenoceptor stimulation relaxes human corpus cavernosum (HCC) strips in cyclic guanosine monophosphate (cGMP)-dependent and endothelium/nitric oxide (NO)-independent manner. Hydrogen sulfide (H2S), along with NO, is another gaseous molecule involved in cardiovascular system and as a consequence also in penile erection...
July 29, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
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
#15
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
#16
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/28756724/medical-expulsive-therapy-in-urolithiasis-a-mixed-treatment-comparison-network-meta-analysis-of-randomized-controlled-clinical-trials
#17
Kannan Sridharan, Gowri Sivaramakrishnan
BACKGROUND: Medical expulsive therapy (MET) using alpha blockers, calcium channel blockers (CCB), phosphodiesterase inhibitors (PDEI) and spasmolytics have been shown to be effective in clinical trials on urolithiasis. The present study is a network meta-analysis comparing the above mentioned drug classes. RESEARCH DESIGN AND METHODS: Electronic databases were searched for randomized controlled trials comparing the above mentioned drug classes in patients with urolithiasis using appropriate search strategy...
August 4, 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28756610/treatment-of-obesity-associated-overactive-bladder-by-the-phosphodiesterase-type-4-inhibitor-roflumilast
#18
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/28748375/attenuation-of-ethanol-abstinence-induced-anxiety-and-depressive-like-behavior-by-the-phosphodiesterase-4-inhibitor-rolipram-in-rodents
#19
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
#20
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
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