keyword
MENU ▼
Read by QxMD icon Read
search

Phosphodiesterase 5 inhibitors

keyword
https://www.readbyqxmd.com/read/28642047/erectile-dysfunction-in-young-men-a-review-of-the-prevalence-and-risk-factors
#1
REVIEW
Hoang Minh Tue Nguyen, Andrew T Gabrielson, Wayne J G Hellstrom
INTRODUCTION: Erectile dysfunction (ED) is an important health concern that can significantly affect a man's psychosocial well-being. ED has traditionally been considered a disease of old age; however, contemporary evidence suggests a growing incidence of ED in men younger than 40 years. The process of achieving an erection is multifaceted; there are many potential mechanisms that can be disrupted. It is critical to identify the specific causes of ED before proceeding with potentially costly and invasive therapeutic options...
June 19, 2017: Sexual Medicine Reviews
https://www.readbyqxmd.com/read/28640077/improvement-of-peripheral-artery-disease-with-sildenafil-and-bosentan-combined-therapy-in-a-patient-with-limited-cutaneous-systemic-sclerosis-a-case-report
#2
Loukman Omarjee, Cedric Fontaine, Guillaume Mahe, Vincent Jaquinandi
RATIONALE: Sildenafil, a phosphodiesterase-5-inhibitor and Bosentan, an endothelin-1-receptor antagonist combined therapy could have beneficial effect in systemic sclerosis (SSc) patients with peripheral artery disease. PATIENT CONCERNS: We report a case of a 48-year-old Black woman, who developed severe left limb claudication and walking limitation following a left femoropopliteal bypass occlusion in 2014. She was a heavy smoker and had a history of right middle cerebral artery ischemic stroke and bilateral Raynaud phenomenon...
June 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28628863/simultaneous-quantification-of-endothelin-receptor-antagonists-and-phosphodiesterase-5-inhibitors-currently-used-in-pulmonary-arterial-hypertension
#3
Yeliz Enderle, Lukas Witt, Heinrike Wilkens, Ekkehard Grünig, Walter E Haefeli, Jürgen Burhenne
Combination treatment with endothelin receptor antagonists (ERA) and phosphodiesterase 5 inhibitors (PDE5I) improved efficacy of pulmonary arterial hypertension (PAH) therapy. However, drug-drug interactions, variable exposure, non-adherence can influence plasma levels. For these reasons, drug quantification may be advantageous particularly in patients with poor treatment responses. We developed, validated, and applied an assay for the simultaneous quantification of ambrisentan, bosentan, macitentan, sildenafil, and tadalafil as well as their main (and partly active) metabolites in human plasma...
June 10, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28626017/amyloid-beta-peptide-is-needed-for-cgmp-induced-long-term-potentiation-and-memory
#4
Agostino Palmeri, Roberta Ricciarelli, Walter Gulisano, Daniela Rivera, Claudia Rebosio, Elisa Calcagno, Maria Rosaria Tropea, Silvia Conti, Utpal Das, Subhojit Roy, Maria A Pronzato, Ottavio Arancio, Ernesto Fedele, Daniela Puzzo
High levels of amyloid-beta peptide (Aβ) have been related to Alzheimer's disease pathogenesis. However, in the healthy brain, low physiologically relevant concentrations of Aβ are necessary for long-term potentiation (LTP) and memory. Because cGMP plays a key role in these processes, here we investigated whether the cyclic nucleotide cGMP influences Aβ levels and function during LTP and memory. We demonstrate that the increase of cGMP levels by the phosphodiesterase-5 inhibitors (PDE5-Is) sildenafil and vardenafil induces a parallel release of Aβ due to a change in the approximation of amyloid precursor protein (APP) and the β-site APP cleaving enzyme 1 (BACE1)...
June 16, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28620954/propentofylline-phosphodiesterase-and-adenosine-reuptake-inhibitor-modulates-lymphocyte-subsets-and-lymphocyte-activity-after-in-vivo-administration-in-non-immunized-and-srbc-immunized-mice
#5
Marianna Szczypka, Magdalena Lis, Agnieszka Suszko-Pawłowska, Aleksandra Pawlak, Angelika Sysak, Bożena Obmińska-Mrukowicz
OBJECTIVES: The aim of the study was to investigate immunomodulatory effect of in-vivo administered propentofylline on the subsets and activity of murine lymphocytes. METHODS: Propentofylline (3 mg/kg) was administered orally to 8-week-old Balb/c mice, once or six times at 12-h intervals. The lymphocyte subsets, regulatory T cells, IL-5 and TNF levels were determined 12 h and 24 h after a single dose or after the sixth dose of the drug in non-immunized mice. Humoral immune response in sheep red blood cells (SRBC)-immunized mice was determined 4, 7 and 14 days after immunization...
June 16, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28618988/synthesis-docking-and-anti-inflammatory-activity-of-triazole-amine-derivatives-as-potential-phosphodiesterase-4-inhibitors
#6
Ajmer Singh Grewal, Viney Lather, Deepti Pandita, Ruchi Dalal
BACKGROUND: Phosphodiesterase 4 (PDE4), one of the member of PDE superfamily catalyzes, the hydrolysis of cyclic adenosine monophosphate to adenosine monophosphate in pro-inflammatory and immunomodulatory cells leading to increased inflammatory processes. PDE4 has been reported as an attractive therapeutic target involved in various inflammatory disorders. OBJECTIVE: The present work was designed to synthesize and evaluate the anti-inflammatory activity of some new triazole amine derivatives as potential PDE4 inhibitors...
June 16, 2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28613871/discovery-of-n-4-5-4-fluoro-phenyl-3-methyl-2-methylsulfanyl-3h-imidazol-4-yl-pyridin-2-yl-acetamide-cbs-3595-a-dual-p38%C3%AE-mapk-pde-4-inhibitor-with-activity-against-tnf%C3%AE-related-diseases
#7
Wolfgang Albrecht, Anke Unger, Silke M Bauer, Stefan A Laufer
The anti-inflammatory potential of p38 mitogen-activated protein kinase (MAPK) inhibitors was coincidentally expanded to a dual inhibition of p38α MAPK and phosphodiesterase 4 (PDE4) and the potential benefits arising from the blockage of both inflammation-related enzymes were thoroughly investigated. The most promising compound, CBS-3595 (1), was successively evaluated in in vitro experiments as well as in ex vivo and in vivo preclinical studies after administration of 1 to rodents, dogs and monkeys. The resulting data clearly indicated a potent suppression of tumor necrosis factor alpha (TNFα) release...
June 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28607126/mechanisms-and-treatment-of-halogen-inhalation-induced-pulmonary-and-systemic-injuries-in-pregnant-mice
#8
James A Lambert, Matthew A Carlisle, Adam Lam, Saurabh Aggarwal, Stephen Doran, Changchun Ren, Wayne E Bradley, Louis Dell'Italia, Namasivayam Ambalavanan, David A Ford, Rakesh P Patel, Tamas Jilling, Sadis Matalon
Inhalation of oxidant gases has been implicated in adverse outcomes in pregnancy, but animal models to address mechanisms and studies to identify potential pregnancy-specific therapies are lacking. Herein, we show that inhalation of bromine at 600 parts per million for 30 minutes by pregnant mice on the 15th day of embryonic development results in significantly lower survival after 96 hours than an identical level of exposure in nonpregnant mice. On the 19th embryonic day, bromine-exposed pregnant mice have increased systemic blood pressure, abnormal placental development, severe fetal growth restriction, systemic inflammation, increased levels of circulating antiangiogenic short fms-like tyrosine kinase-1, and evidence of pulmonary and cardiac injury...
June 12, 2017: Hypertension
https://www.readbyqxmd.com/read/28606099/pulmonary-hemodynamics-and-effects-of-phosphodiesterase-type-5-inhibition-in-heart-failure-a-meta-analysis-of-randomized-trials
#9
In-Chang Hwang, Yong-Jin Kim, Jun-Bean Park, Yeonyee E Yoon, Seung-Pyo Lee, Hyung-Kwan Kim, Goo-Yeong Cho, Dae-Won Sohn
BACKGROUND: Previous studies suggested that phosphodiesterase 5 inhibitors (PDE5i) have a beneficial effect in patients with heart failure (HF), although the results were inconsistent. We performed a meta-analysis to evaluate the effect of PDE5i in HF patients, and investigated the relationship between PDE5i effects and pulmonary hemodynamics. METHOD: We searched PubMed, EMBASE and the Cochrane Library for randomized controlled trials (RCTs) that compared PDE5i with placebo in HF with reduced ejection fraction (HFrEF) or HF with preserved EF (HFpEF)...
June 12, 2017: BMC Cardiovascular Disorders
https://www.readbyqxmd.com/read/28605937/are-phosphodiesterase-5-inhibitors-a-sort-of-panacea-for-several-urological-diseases
#10
Guido Giusti, Silvia Proietti
no abstract.
June 12, 2017: Journal of Endourology
https://www.readbyqxmd.com/read/28603047/tadalafil-induces-antiproliferation-apoptosis-and-phosphodiesterase-type-5-downregulation-in-idiopathic-pulmonary-arterial-hypertension-in-vitro
#11
Aya Yamamura, Eri Fujitomi, Naoki Ohara, Kikuo Tsukamoto, Motohiko Sato, Hisao Yamamura
Idiopathic pulmonary arterial hypertension (IPAH) is a fatal disease of the pulmonary artery resulting from a currently unidentified etiology. IPAH is pathologically characterized as sustained vasoconstriction and vascular remodeling of the pulmonary artery. Vascular remodeling is mediated by enhanced proliferation and reduced apoptosis in pulmonary arterial smooth muscle cells (PASMCs). Based on its pathological mechanism, specific phosphodiesterase type 5 (PDE5) inhibitors have been used in the treatment of IPAH...
June 8, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28601316/oral-administration-of-cilostazol-improves-survival-rate-after-rat-liver-ischemia-reperfusion-injury
#12
Taku Fujii, Hideaki Obara, Kentaro Matsubara, Naoki Fujimura, Hiroshi Yagi, Taizo Hibi, Yuta Abe, Minoru Kitago, Masahiro Shinoda, Osamu Itano, Minoru Tanabe, Yohei Masugi, Michiie Sakamoto, Yuko Kitagawa
BACKGROUND: Cilostazol is a type III phosphodiesterase inhibitor used to treat the symptoms of intermittent claudication. Recent studies have shown that cilostazol decreases ischemia/reperfusion (I/R) injury in several organs. MATERIALS AND METHODS: We evaluated the effects of cilostazol in a rat model of liver I/R injury. Thirty male Wistar rats with liver I/R injury were divided into a cilostazol or saline (control) group (n = 15 each). Each rat was orally administered cilostazol or saline for 3 d before I/R injury...
June 1, 2017: Journal of Surgical Research
https://www.readbyqxmd.com/read/28597779/phosphodiesterase-type-5-inhibitor-to-riociguat-transition-is-associated-with-hemodynamic-and-symptomatic-improvement-in-pulmonary-hypertension
#13
Ryan Davey, Raymond L Benza, Srinivas Murali, Amresh Raina
Riociguat is a soluble guanylate cyclase stimulator approved for the treatment of pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension. We studied the clinical and hemodynamics effects of transitioning 12 pulmonary hypertension patients from Phosphodiesterase type 5 inhibitor (PDE5i) to riociguat, and demonstrated a significant increase in cardiac index, fall in pulmonary vascular resistance, and improvement in functional class with this switch. Switch from PDE5i to riociguat appeared to be safe and fairly well tolerated in most patients...
April 2017: Pulmonary Circulation
https://www.readbyqxmd.com/read/28597774/combination-therapy-in-pulmonary-arterial-hypertension-recent-accomplishments-and-future-challenges
#14
Annie-Christine Lajoie, Sebastien Bonnet, Steeve Provencher
Pulmonary arterial hypertension (PAH) is a life-threatening disease characterized by a progressive increase in pulmonary vascular resistance, ultimately leading to right heart failure and death. Throughout the past 20 years, numerous specific pharmacologic agents, including phosphodiesterase-5 inhibitors, endothelin receptor antagonists, prostaglandins, and more recently, soluble guanylate cyclase stimulators and selective IP prostacyclin receptor agonist, have emerged for the treatment of PAH. Early clinical trials were typically of short-term duration, comparing the effects of PAH-targeted therapies versus placebo and using exercise tolerance as the primary endpoint in most trials...
April 2017: Pulmonary Circulation
https://www.readbyqxmd.com/read/28597771/first-in-child-use-of-the-oral-selective-prostacyclin-ip-receptor-agonist-selexipag-in-pulmonary-arterial-hypertension
#15
Lianne M Geerdink, Harald Bertram, Georg Hansmann
Pulmonary arterial hypertension (PAH) is a complex disease with a poor prognosis. Selexipag is a selective prostacyclin receptor agonist with vasodilatory, anti-proliferative, anti-inflammatory, and pro-angiogenic properties. However, no clinical data on its therapeutic use in children with PAH are currently available. Here, we report the case of a 12-year-old girl who presented in World Health Organization (WHO) functional class III and right ventricular (RV) failure with recurrent syncope, dizziness, and progressive fatigue for two years...
April 2017: Pulmonary Circulation
https://www.readbyqxmd.com/read/28597753/circulatory-power-and-ventilatory-power-over-time-under-goal-oriented-sequential-combination-therapy-for-pulmonary-arterial-hypertension
#16
Akihiro Hirashiki, Shiro Adachi, Yoshihisa Nakano, Yoshihiro Kamimura, Shigetake Shimokata, Kyosuke Takeshita, Atsuya Shimizu, Kenji Toba, Toyoaki Murohara, Takahisa Kondo
Many therapeutic options are available for patients with pulmonary arterial hypertension (PAH). However, little is known about the effects of sequential combination therapy on exercise capacity. Here we monitored exercise capacity by cardiopulmonary exercise testing (CPX) and observed the benefit of using a peak VO2 cutoff of 15 mL/kg/min to guide combination therapy. Thirty patients newly diagnosed with PAH were treated with goal-oriented sequential combination therapy. Endothelin receptor antagonists (ERA) were the first-line treatment, with phosphodiesterase type 5 inhibitors (PDE-5i) as the preferred combination partner...
April 2017: Pulmonary Circulation
https://www.readbyqxmd.com/read/28594906/the-anti-inflammatory-and-immunomodulatory-potential-of-braylin-pharmacological-properties-and-mechanisms-by-in-silico-in-vitro-and-in-vivo-approaches
#17
Renan Fernandes Espírito-Santo, Cassio Santana Meira, Rafael Dos Santos Costa, Otávio Passos Souza Filho, Afranio Ferreira Evangelista, Gustavo Henrique Goulart Trossini, Glaucio Monteiro Ferreira, Eudes da Silva Velozo, Cristiane Flora Villarreal, Milena Botelho Pereira Soares
Braylin belongs to the group of natural coumarins, a group of compounds with a wide range of pharmacological properties. Here we characterized the pharmacological properties of braylin in vitro, in silico and in vivo in models of inflammatory/immune responses. In in vitro assays, braylin exhibited concentration-dependent suppressive activity on activated macrophages. Braylin (10-40 μM) reduced the production of nitrite, IL-1β, TNF-α and IL-6 by J774 cells or peritoneal exudate macrophages stimulated with LPS and IFN-γ...
2017: PloS One
https://www.readbyqxmd.com/read/28590829/aging-and-sexual-health-getting-to-the-problem
#18
Ecem Kaya, Suresh C Sikka, Philip J Kadowitz, Serap Gur
Erectile dysfunction (ED) is one of the most common disorders in male and is often associated with other age-related comorbidities. The aging process affects the structural organization and function of penile erectile components such as smooth muscle cell and vascular architecture. These modifications affect penile hemodynamics by impairing cavernosal smooth muscle cell relaxation, reducing penile elasticity, compliance and promoting fibrosis. This review aims to identify the mechanisms of ED in the penile aging process in experimental and clinical data...
June 2017: Aging Male: the Official Journal of the International Society for the Study of the Aging Male
https://www.readbyqxmd.com/read/28588484/akrinor-tm-a-cafedrine-theodrenaline-mixture-20-1-increases-force-of-contraction-of-human-atrial-myocardium-but-does-not-constrict-internal-mammary-artery-in-vitro
#19
Benjamin Kloth, Simon Pecha, Eileen Moritz, Yvonne Schneeberger, Klaus-Dieter Söhren, Edzard Schwedhelm, Hermann Reichenspurner, Thomas Eschenhagen, Rainer H Böger, Torsten Christ, Sebastian N Stehr
Background: Intraoperative hypotension is a common problem and direct or indirect sympathomimetic drugs are frequently needed to stabilize blood pressure. Akrinor(TM) consists of the direct and the indirect sympathomimetic noradrenaline and norephedrine. Both substances are covalently bound to the phosphodiesterase (PDE) inhibitor theophylline, yielding theodrenaline and cafedrine, respectively. We investigated pharmacodynamic effects of Akrinor(TM) and its constituents on contractile force and tension in human atrial trabeculae and internal A...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28587776/pharmacological-characterization-of-a-novel-potent-selective-and-orally-active-phosphodiesterase-2a-inhibitor-pdm-631
#20
Shunsuke Maehara, Keita Arakawa, Kotaro Hoshida, Hiroshi Nagasue, Noboru Chida, Kazunari Nakao, Shoji Furusako
Recently, we identified a novel phosphodiesterase 2A (PDE2A) inhibitor, PDM-631 ((S)-3-cyclopropyl-6-methyl-1-(1-(4-(trifluoromethoxy)phenyl)propan-2-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one). PDM-631 showed potent inhibitory activities for human and rat PDE2A with IC50 values of 1.5 and 4.2nM, respectively and more than 2000-fold selectivity against other phosphodiesterases. In rat studies, PDM-631 showed oral bioavailability and good brain penetration, and increased the cGMP levels in the cortex...
June 3, 2017: European Journal of Pharmacology
keyword
keyword
52726
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"