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PDE5 inhibitor

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https://www.readbyqxmd.com/read/29885420/sub-efficacious-doses-of-phosphodiesterase-4-and-5-inhibitors-improve-memory-in-a-mouse-model-of-alzheimer-s-disease
#1
Walter Gulisano, Maria Rosaria Tropea, Ottavio Arancio, Agostino Palmeri, Daniela Puzzo
Cyclic nucleotides cAMP and cGMP cooperate to ensure memory acquisition and consolidation. Increasing their levels by phosphodiesterase inhibitors (PDE-Is) enhanced cognitive functions and rescued memory loss in different models of aging and Alzheimer's disease (AD). However, side effects due to the high doses used limited their application in humans. Based on previous studies suggesting that combinations of sub-efficacious doses of cAMP- and cGMP-specific PDE-Is improved synaptic plasticity and memory in physiological conditions, here we aimed to study whether this treatment was effective to counteract the AD phenotype in APPswe mice...
June 6, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29884471/the-association-between-phosphodiesterase-type-5-inhibitor-use-and-risk-of-non-arteritic-anterior-ischemic-optic-neuropathy-a-systematic-review-and-meta-analysis
#2
REVIEW
Bing Liu, Linxin Zhu, Jingxiang Zhong, Guohua Zeng, Tuo Deng
INTRODUCTION: Phosphodiesterase type 5 inhibitors (PDE5-Is) are first-line drugs for erectile dysfunction. Non-arteritic anterior ischemic optic neuropathy (NAION) has been linked with PDE5-I use. However, no meta-analysis or conclusive review has explored the association between NAION and PDE5-I use. AIM: To investigate the association between PDE5-I use and risk of NAION. METHODS: A comprehensive literature search was conducted using online databases in October 2017 to obtain studies researching the association between PDE5-I application and occurrence of NAION...
June 5, 2018: Sexual Medicine
https://www.readbyqxmd.com/read/29872554/phosphodiesterase-5-inhibition-reduces-postoperative-metastatic-disease-by-targeting-surgery-induced-myeloid-derived-suppressor-cell-dependent-inhibition-of-natural-killer-cell-cytotoxicity
#3
Lee-Hwa Tai, Almohanad A Alkayyal, Amanda L Leslie, Shalini Sahi, Sean Bennett, Christiano Tanese de Souza, Katherine Baxter, Leonard Angka, Rebecca Xu, Michael A Kennedy, Rebecca C Auer
Cancer surgery while necessary for primary tumor removal, has been shown to induce immune suppression and promote metastases in preclinical models and human cancer surgery patients. Activating the immune system and reversing immunosuppression have emerged as promising ways to treat cancer and they can be safely employed in the perioperative period. In this study, we evaluated the immunotherapeutic potential of phosphodiesterase-5 (PDE-5) inhibitors to target surgery-induced myeloid-derived suppressor cells (MDSC) and restore natural killer (NK) cell function in the clinically relevant perioperative period...
2018: Oncoimmunology
https://www.readbyqxmd.com/read/29847860/a-novel-synthetic-phosphodiesterase-5-inhibitor-kjh-1002-ameliorates-scopolamine-induced-cognitive-impairments-in-mice-by-activating-the-cgmp-creb-signaling-pathway-and-attenuating-oxidative-damage
#4
Lijun Zhang, Jae Hong Seo, Huan Li, Ghilsoo Nam, Hyun Ok Yang
BACKGROUND AND PURPOSE: Inhibition of PDE5 has been demonstrated to improve synaptic plasticity and memory via enhancing of cGMP expression, thus activating the cGMP/CREB signaling pathway. This study aimed to investigate the ameliorating effect of PDE5 inhibitor on scopolamine-induced cognitive dysfunction using memory-related behavioral tests and biochemical assays. EXPERIMENTAL APPROACH: After the mice were pretreated with PDE5 inhibitor, amnesia was induced by scopolamine administration...
May 30, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29797572/chronic-phosphodiesterase-type-5-inhibition-has-beneficial-effects-on-subcutaneous-adipose-tissue-plasticity-in-type-2-diabetic-mice
#5
Daniela Fiore, Daniele Gianfrilli, Silvia Cardarelli, Fabio Naro, Andrea Lenzi, Andrea M Isidori, Mary A Venneri
Different adipose tissue (AT) depots are associated with multiple metabolic risks. Phosphodiesterase type 5 (PDE5) is involved in adipocyte physiology and PDE5 inhibition may affect adipogenesis and ameliorate white AT quality. The aim of this study is to investigate the distribution of AT and the composition of the stroma-vascular fraction (SVF) of subcutaneous AT (SAT) in type 2 diabetic mice after prolonged treatment with a PDE5 inhibitor, Sildenafil. 18 db/db mice were treated with Sildenafil or vehicle for 12 weeks...
May 24, 2018: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/29773995/hypoxia-reoxygenation-of-rat-renal-arteries-impairs-vasorelaxation-via-modulation-of-endothelium-independent-sgc-cgmp-pkg-signaling
#6
Diana Braun, Christa Zollbrecht, Stefanie Dietze, Rudolf Schubert, Stefan Golz, Holger Summer, Pontus B Persson, Mattias Carlström, Marion Ludwig, Andreas Patzak
Ischemia/reperfusion injury holds a key position in many pathological conditions such as acute kidney injury and in the transition to chronic stages of renal damage. We hypothesized that besides a reported disproportional activation of vasoconstrictor response, hypoxia/reoxygenation (H/R) adversely affects endothelial dilatory systems and impairs relaxation in renal arteries. Rat renal interlobar arteries were studied under isometric conditions. Hypoxia was induced by application of 95% N2 , 5% CO2 for 60 min to the bath solution, followed by a 10 min period of reoxygenation (95% O2 , 5% CO2 )...
2018: Frontiers in Physiology
https://www.readbyqxmd.com/read/29750687/evaluation-of-clinical-outcomes-with-phosphodiesterase-5-inhibitor-therapy-for-right-ventricular-dysfunction-after-left-ventricular-assist-device-implantation
#7
Katherine L Roberts, Jerrica E Shuster, Nicholas S Britt, Keki R Balsara, Thomas J Graetz, Mohammad Helwani, Akinobu Itoh, Bethany R Tellor
Few studies have evaluated the use of phosphodiesterase-5 inhibitors (PDE5-i) for right ventricular (RV) dysfunction after left ventricular assist device (LVAD) implantation. The study purpose was to examine the impact of postoperative inpatient PDE5-i therapy on clinical outcomes in patients with LVADs. This single-center, retrospective cohort study screened 428 LVAD recipients between January 2011 and May 2015 for eligibility. Subjects receiving post-LVAD PDE5-i were compared with those who did not. The primary outcome was the proportion of all-cause hospital readmission at 30 days...
May 7, 2018: ASAIO Journal: a Peer-reviewed Journal of the American Society for Artificial Internal Organs
https://www.readbyqxmd.com/read/29743944/repurposing-drugs-in-oncology-redo-selective-pde5-inhibitors-as-anti-cancer-agents
#8
Pan Pantziarka, Vidula Sukhatme, Sergio Crispino, Gauthier Bouche, Lydie Meheus, Vikas P Sukhatme
Selective phosphodiesterase 5 inhibitors, including sildenafil, tadalafil and vardenafil, are widely-used in the treatment of erectile dysfunction and pulmonary arterial hypertension. They are also well-known as examples of successful drug repurposing in that they were initially developed for angina and only later developed for erectile dysfunction. However, these drugs may also be effective cancer treatments. A range of evidentiary sources are assessed in this paper and the case made that there is pre-clinical and clinical evidence that these drugs may offer clinical benefit in a range of cancers...
2018: Ecancermedicalscience
https://www.readbyqxmd.com/read/29743519/transdermal-water-in-oil-nanocarriers-of-nitric-oxide-for-triggering-penile-erection
#9
Eunryel Nam, Saejong Yoo, Hwi-Yool Kim, Young-Rok Kim, Yun Jung Heo
Men's sexual health can have significant effects on a man's self-esteem, sexual relationship and male reproductive functions. Although commercially available drugs (e.g., VIAGRA and CIALIS) show effective treatment of erectile dysfunction (ED), patients with severe ED fail to respond to these medicines. Topical nitric-oxide (NO) delivery to penis can be a painless, alternative solution with severe ED because NO triggers erection and diffuses to the trabecular arteries and smooth muscles in the penis. We here develop water-in-oil (W/O) nanoemulsions (NEs) that contain NO and can directly spread on the penis...
May 9, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29738821/discovery-and-development-of-sgc-stimulators-for-the-treatment-of-pulmonary-hypertension-and-rare-diseases
#10
REVIEW
Peter Sandner, Eva-Maria Becker-Pelster, Johannes Peter Stasch
The NO/sGC/cGMP signaling cascade plays a pivotal role in regulation of cardiovascular, cardiopulmonary and cardiorenal diseases and impairment of this cascade results in severe pathologies. Therefore, pharmacological interventions, targeting this pathway are promising strategies for treating a variety of diseases. Nitrates, supplementing NO and, PDE5 inhibitors preventing cGMP degradation, are used for angina pectoris treatment and the treatment of pulmonary arterial hypertension (PAH), respectively. More recently, a new class of drugs which directly stimulate the sGC enzyme and trigger NO-independent cGMP production was introduced and termed sGC stimulators...
May 5, 2018: Nitric Oxide: Biology and Chemistry
https://www.readbyqxmd.com/read/29735634/evaluation-of-sildenafil-and-tadalafil-for-reversing-constriction-of-fetal-arteries-in-a-human-placenta-perfusion-model
#11
Robert B Walton, Luckey C Reed, Sarah M Estrada, Stacey S Schmiedecke, Diana L Villazana-Kretzer, Peter G Napolitano, Nicholas Ieronimakis
Fetal growth restriction resulting from reduced placental blood perfusion is a major cause of neonatal morbidity and mortality. Aside from intense surveillance and early delivery, there is no treatment for fetal growth restriction. A potential treatment associated with placental vasoconstriction is the class of PDE5 (phosphodiesterase type 5) inhibitors such as sildenafil, which is known to cross the placenta. In contrast, tadalafil, a more potent and selective PDE5 inhibitor has not been studied in pregnancy or experimental models of fetal growth restriction...
May 7, 2018: Hypertension
https://www.readbyqxmd.com/read/29724712/mutations-of-the-pde5a-gene-confer-a-survival-advantage-in-patients-with-colon-cancer
#12
Steven Lehrer, Peter H Rheinstein, Kenneth Rosenzweig
Sildenafil is a small molecule that inhibits PDE5. The study of Islam et al validates PDE5 as a colon cancer chemoprevention target in mice (2), as did a second mouse study (3). Our analysis of TCGA data corroborates this finding in humans. Further studies are needed to determine whether sildenafil or other PDE5 inhibitors might be colon cancer preventives or treatments.
May 3, 2018: Cancer Prevention Research
https://www.readbyqxmd.com/read/29724204/efficacy-and-safety-of-pde5-is-and-%C3%AE-1-blockers-for-treating-lower-ureteric-stones-or-luts-a-meta-analysis-of-rcts
#13
Xifeng Sun, Wei Guan, Haoran Liu, Kun Tang, Libin Yan, Yangjun Zhang, Jin Zeng, Zhiqiang Chen, Hua Xu, Zhangqun Ye
BACKGROUND: Lower ureteric stones and lower urinary tract symptoms are common in urology.Drug treatment is one of standard therapy,but the efficacy was controversial.Thus we aimed to investigate the efficacy and safety of monotherapy or combination therapy of adrenoceptor1 blockers and phosphodiesterase5 inhibitors for treatment. METHODS: Randomized controlled trials up to November 2016 were retrieved from PubMed, the Cochrane Library, Web of Science and Embase...
May 3, 2018: BMC Urology
https://www.readbyqxmd.com/read/29687019/phosphodiesterase-5-inhibition-potentiates-cerebrovascular-reactivity-in-chronic-traumatic-brain-injury
#14
Kimbra Kenney, Franck Amyot, Carol Moore, Margalit Haber, L Christine Turtzo, Christian Shenouda, Erika Silverman, Yunhua Gong, Bao-Xi Qu, Leah Harburg, Eric M Wassermann, Hanzhang Lu, Ramon Diaz-Arrastia
Background: Traumatic cerebrovascular injury (TCVI), a common consequence of traumatic brain injury (TBI), presents an attractive therapeutic target. Because phosphodiesterase-5 (PDE5) inhibitors potentiate the action of nitric oxide (NO) produced by endothelial cells, they are candidate therapies for TCVI. This study aims to: (1) measure cerebral blood flow (CBF), cerebrovascular reactivity (CVR), and change in CVR after a single dose of sildenafil (ΔCVR) in chronic TBI compared to uninjured controls; (2) examine the safety and tolerability of 8-week sildenafil administration in chronic symptomatic moderate/severe TBI patients; and as an exploratory aim, (3) assess the effect of an 8-week course of sildenafil on chronic TBI symptoms...
April 2018: Annals of Clinical and Translational Neurology
https://www.readbyqxmd.com/read/29686697/ppar-%C3%AE-antagonizes-hypoxia-induced-activation-of-hepatic-stellate-cell-through-cross-mediating-pi3k-akt-and-cgmp-pkg-signaling
#15
Qinghui Zhang, Shihao Xiang, Qingqian Liu, Tao Gu, Yongliang Yao, Xiaojie Lu
Background and Aims: Accumulating evidence reveals that PPAR γ plays a unique role in the regulation of hepatic fibrosis and hepatic stellate cells (HSCs) activation. This study was aimed at investigating the role of PPAR γ in hypoxia-induced hepatic fibrogenesis and its possible mechanism. Methods: Rats used for CCl4-induced hepatic fibrosis model were exposed to hypoxia for 8 hours each day. Rats exposed to hypoxia were treated with or without the PPAR γ agonist rosiglitazone...
2018: PPAR Research
https://www.readbyqxmd.com/read/29677206/synergistic-interaction-between-a-pde5-inhibitor-sildenafil-and-a-new-adenosine-a2a-receptor-agonist-lassbio-1359-improves-pulmonary-hypertension-in-rats
#16
Allan K Alencar, Fábio I Carvalho, Ananssa M Silva, Sabrina T Martinez, Jorge A Calasans-Maia, Carlos M Fraga, Eliezer J Barreiro, Gisele Zapata-Sudo, Roberto T Sudo
INTRODUCTION: Pulmonary hypertension (PH) is characterized by enhanced pulmonary vascular resistance, which causes right ventricle (RV) pressure overload and results in right sided heart failure and death. This work investigated the effectiveness of a combined therapy with PDE5 inhibitor (PDE5i) and a new adenosine A2A receptor (A2AR) agonist in mitigating monocrotaline (MCT) induced PH in rats. METHODS: An in vitro isobolographic analysis was performed to identify possible synergistic relaxation effect between sildenafil and LASSBio 1359 in rat pulmonary arteries (PAs)...
2018: PloS One
https://www.readbyqxmd.com/read/29667180/pde5-inhibitors-pharmacology-and-clinical-applications-20-years-after-sildenafil-discovery
#17
REVIEW
K-E Andersson
The discovery of the nitric oxide/cGMP pathway was the basis for our understanding of many normal physiological functions and the pathophysiology of several diseases. Since the discovery and introduction of sildenafil, inhibitors of PDE5 have been the first-line therapy for erectile dysfunction (ED). The success of sildenafil in the treatment of ED stimulated research in the field of PDE5 inhibition and led to many new applications, such as treatment of lower urinary symptoms, and pulmonary arterial hypertension, which are now approved indications...
April 17, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29665366/3-7-bis-2-hydroxyethyl-icaritin-a-potent-inhibitor-of-phosphodiesterase-5-prevents-monocrotaline-induced-pulmonary-arterial-hypertension-via-no-cgmp-activation-in-rats
#18
Tao-Hua Lan, Xiao-Ling Chen, Yun-Shan Wu, Hui-Liang Qiu, Jun-Zhe Li, Xin-Min Ruan, Dan-Ping Xu, Dong-Qun Lin
Pulmonary arterial hypertension (PAH) is a chronic progressive disease which leads to elevated pulmonary arterial pressure and right heart failure. 3,7-Bis(2-hydroxyethyl)icaritin (ICT), an icariin derivatives, was reported to have potent inhibitory activity on phosphodiesterase type 5 (PDE5) which plays a crucial role in the pathogenesis of PAH. The present study was designed to investigate the effects of ICT on monocrotaline (MCT)-induced PAH rat model and reveal the underlying mechanism. MCT-induced PAH rat models were established with intragastric administration of ICT (10, 20, 40 mg/kg/d), Icariin (ICA) (40 mg/kg/d) and Sildenafil (25 mg/kg/d)...
June 15, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29660387/long-term-inhibition-of-pde5-ameliorates-aging-induced-changes-in-rat-testis
#19
Srdjan J Sokanovic, Ivan Capo, Marija M Medar, Silvana A Andric, Tatjana S Kostic
NO-cGMP signaling pathway has been implicated in reduction of testicular steroidogenesis during aging. Here we analyzed the effect of PDE5 inhibition on old testicular phenotype formation. The old phenotype exhibited low testosterone and increased nitrite levels in circulation, increased cGMP accumulation in testicular interstitial fluid (TIF), progressive atrophy of testicular seminiferous tubules and enlargement of interstitial area followed by rise in blood vessel density and slight increase in the number of Leydig cells and macrophages...
July 15, 2018: Experimental Gerontology
https://www.readbyqxmd.com/read/29656464/design-and-synthesis-of-novel-annulated-thienopyrimidines-as-phosphodiesterase-5-pde5-inhibitors
#20
Lina Y El-Sharkawy, Rowaida A El-Sakhawy, Mohammad Abdel-Halim, Kevin Lee, Gary A Piazza, Christian Ducho, Rolf W Hartmann, Ashraf H Abadi
Novel cycloalkene-fused thienopyrimidine analogues with enhanced phosphodiesterase 5 (PDE5) inhibitory properties are presented. The structure of the reported scaffold was modulated through variation of the terminal cycloalkene ring size, as well as by varying the substituents at position 4 through the attachment of different groups including aniline, benzylamine, cyclohexylethylamine, methyl/acetyl/aryl piperazines, and aryl hydrazones. Compound 15Y with a benzylamine substituent and cycloheptene as terminal ring showed the highest PDE5 inhibitory activity with an IC50 value as low as 190 nM and with good selectivity versus PDE7 and PDE9...
May 2018: Archiv der Pharmazie
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