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Phosphodiesterase 5 inhibitors

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https://www.readbyqxmd.com/read/27914563/differential-effects-of-testosterone-and-estradiol-on-clitoral-function-an-experimental-study-in-rats
#1
Paolo Comeglio, Ilaria Cellai, Sandra Filippi, Chiara Corno, Francesca Corcetto, Annamaria Morelli, Elena Maneschi, Elisa Maseroli, Edoardo Mannucci, Massimiliano Fambrini, Mario Maggi, Linda Vignozzi
INTRODUCTION: Female sexual response is a complex phenomenon in which psychological, neurologic, and vascular mechanisms and hormonal factors interact. During the arousal phase, they cooperate to increase genital blood flow, thus inducing engorgement of the clitoris and lubrication of the vagina. Regulation of vascular and non-vascular smooth muscle tone is the crucial event in the erectile process. Preclinical studies have suggested that nitric oxide (NO) is the main vasodilator neurotransmitter modulating, through the second messenger cyclic guanosine monophosphate (cGMP), clitoral flow vessels...
December 2016: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/27910296/the-year-since-the-guidelines-a-concise-update-on-recent-advances-in-pulmonary-hypertension
#2
Abhishek Mishra, Maninder Singh, Edo Kaluski
Since the updated pulmonary hypertension (PH) guidelines published in 2015, two major landmark trials have provided additional insight regarding therapeutic algorithms of PH. In this review, we concisely summarized the key findings of peer‑reviewed studies published in the last one year in the field of PH. These studies have enhanced our therapeutic abilities by introducing a new potent agent, selexipag, and by demonstrating the advantage of upfront combination therapy (endothelin receptor antagonist and phosphodiesterase‑5 inhibitor) versus single agent therapy in group 1 PH...
February 2017: Minerva Cardioangiologica
https://www.readbyqxmd.com/read/27909693/unfractionated-and-low-molecular-weight-heparin-and-the-phosphodiesterase-inhibitors-ibmx-and-cilostazol-block-ex-vivo-equid-herpesvirus-type-1-induced-platelet-activation
#3
Tracy Stokol, Priscila B D Serpa, Muhammad N Zahid, Marjory B Brooks
Equid herpes virus type-1 (EHV-1) is a major pathogen of horses, causing abortion storms and outbreaks of herpes virus myeloencephalopathy. These clinical syndromes are partly attributed to ischemic injury from thrombosis in placental and spinal vessels. The mechanism of thrombosis in affected horses is unknown. We have previously shown that EHV-1 activates platelets through virus-associated tissue factor-initiated thrombin generation. Activated platelets participate in thrombus formation by providing a surface to localize coagulation factor complexes that amplify and propagate thrombin generation...
2016: Frontiers in Veterinary Science
https://www.readbyqxmd.com/read/27908707/the-role-of-nmda-receptor-and-nitric-oxide-cyclic-guanosine-monophosphate-pathway-in-the-antidepressant-like-effect-of-dextromethorphan-in-mice-forced-swimming-test-and-tail-suspension-test
#4
Ehsan Sakhaee, Sattar Ostadhadi, Muhammad Imran Khan, Farbod Yousefi, Abbas Norouzi-Javidan, Reyhaneh Akbarian, Mohsen Chamanara, Samira Zolfaghari, Ahmad-Reza Dehpour
Depression is a devastating disorder which has a high impact on the wellbeing of overall society. As such, need for innovative therapeutic agents are always there. Most of the researchers focused on N-methyl-d-aspartate receptor to explore the antidepressant like activity of new therapeutic agents. Dextromethorphan is a cough suppressant agent with potential antidepressant activity reported in mouse force swimming test. Considering N-methyl-d-aspartate as a forefront in exploring antidepressant agents, here we focused to unpin the antidepressant mechanism of dextromethorphan targeting N-methyl-d-aspartate receptor induced nitric oxide-cyclic guanosine monophosphate signaling...
November 28, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27903966/pde5-inhibitors-enhance-the-lethality-of-pemetrexed-through-inhibition-of-multiple-chaperone-proteins-and-via-the-actions-of-cyclic-gmp-and-nitric-oxide
#5
Laurence Booth, Jane L Roberts, Andrew Poklepovic, Sarah Gordon, Paul Dent
Phosphodiesterase 5 (PDE5) inhibitors prevent the breakdown of cGMP that results in prolonged protein kinase G activation and the generation of nitric oxide. PDE5 inhibitors enhanced the anti-NSCLC cell effects of the NSCLC therapeutic pemetrexed. [Pemetrexed + sildenafil] activated an eIF2α - ATF4 - CHOP - Beclin1 pathway causing formation of toxic autophagosomes; activated a protective IRE1 - XBP-1 - chaperone induction pathway; and activated a toxic eIF2α - CHOP - DR4 / DR5 / CD95 induction pathway. [Pemetrexed + sildenafil] reduced the expression of c-FLIP-s, MCL-1 and BCL-XL that was blocked in a cell-type -dependent fashion by either over-expression of HSP90 / GRP78 / HSP70 / HSP27 or by blockade of eIF2α-CHOP signaling...
November 26, 2016: Oncotarget
https://www.readbyqxmd.com/read/27903663/beyond-a-single-pathway-combination-therapy-in-pulmonary-arterial-hypertension
#6
REVIEW
Olivier Sitbon, Sean Gaine
There is a strong rationale for combining therapies to simultaneously target three of the key pathways implicated in the pathogenesis of pulmonary arterial hypertension (PAH). Evidence to support this strategy is growing, and a number of studies have demonstrated that combination therapy, administered as either a sequential or an initial regimen, can improve long-term outcomes in PAH. Dual combination therapy with a phosphodiesterase-5 inhibitor and an endothelin receptor antagonist is the most widely utilised combination regimen...
December 2016: European Respiratory Review: An Official Journal of the European Respiratory Society
https://www.readbyqxmd.com/read/27895461/sildenafil-potentiates-the-antitumor-activity-of-cisplatin-by-induction-of-apoptosis-and-inhibition-of-proliferation-and-angiogenesis
#7
Mona Mohamed El-Naa, Mohamed Othman, Sheren Younes
Sildenafil is the first phosphodiesterase-5 inhibitor used for the treatment of erectile dysfunction. However, recent studies have been suggesting an antitumor effect of sildenafil. The current study assessed the aforementioned activity of sildenafil in vivo and in vitro in solid-tumor-bearing mice and in a human cell line MCF-7, respectively. Moreover, we investigated the impact of sildenafil on cisplatin antitumor activity. The solid tumor was induced by inoculation of Ehrlich ascites carcinoma cells in female mice...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27890378/design-and-synthesis-of-4-5-6-7-tetrahydro-1h-1-2-diazepin-7-one-derivatives-as-a-new-series-of-phosphodiesterase-4-pde4-inhibitors
#8
Sara Guariento, Anna Karawajczyk, James A Bull, Gessica Marchini, Martyna Bielska, Xenia Iwanowa, Olga Bruno, Paola Fossa, Fabrizio Giordanetto
Phosphodiesterase 4 (PDE4) inhibitors have attractive therapeutic potential in respiratory, inflammatory, metabolic and CNS disorders. The present work details the design, chemical exploration and biological profile of a novel PDE4 inhibitor chemotype. A diazepinone ring was identified as an under-represented heterocyclic system fulfilling a set of PDE4 structure-based design hypotheses. Rapid exploration of the structure activity relationships for the series was enabled by robust and scalable two/three-steps parallel chemistry protocols...
November 16, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27888146/a-rhodium-iii-based-inhibitor-of-autotaxin-with-antiproliferative-activity
#9
Tian-Shu Kang, Wanhe Wang, Hai-Jing Zhong, Jia-Xin Liang, Chung-Nga Ko, Jin-Jian Lu, Xiu-Ping Chen, Dik-Lung Ma, Chung-Hang Leung
BACKGROUND: Cancer of the skin is by far the most common of all cancers. Melanoma accounts for only about 1% of skin cancers but causes a large majority of skin cancer deaths. Autotaxin (ATX), also known as ectonucleotide pyrophosphatase/phosphodiesterase 2 (ENPP2), regulates physiological and pathological functions of lysophosphatidic acid (LPA), and is thus an important therapeutic target. METHODS: We synthesized ten metal-based complexes and a novel cyclometalated rhodium(III) complex 1 was identified as an ATX enzymatic inhibitor using multiple methods, including ATX enzymatic assay, thermal shift assay, western immunoblotting and so on...
November 23, 2016: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/27887774/rationale-and-study-design-of-respite-an-open-label-phase-3b-study-of-riociguat-in-patients-with-pulmonary-arterial-hypertension-who-demonstrate-an-insufficient-response-to-treatment-with-phosphodiesterase-5-inhibitors
#10
Marius M Hoeper, James R Klinger, Raymond L Benza, Gerald Simonneau, David Langleben, Robert Naeije, Paul A Corris
Patients with pulmonary arterial hypertension (PAH) who do not have an adequate response to therapy with phosphodiesterase-5 inhibitors (PDE-5i) may have insufficient synthesis of cyclic guanosine monophosphate (cGMP). These patients may respond to a direct soluble guanylate cyclase (sGC) stimulator such as riociguat. RESPITE (NCT02007629) was an open-label, multicenter, uncontrolled, single-arm phase 3b study of riociguat in patients with PAH who demonstrated an insufficient response to treatment with PDE-5i...
November 5, 2016: Respiratory Medicine
https://www.readbyqxmd.com/read/27886893/erectile-dysfunction-agents-and-nonarteritic-anterior-ischemic-optic-neuropathy
#11
REVIEW
Howard D Pomeranz
Phosphodiesterase-5 inhibitors (PDE5I) are used for treatment of erectile dysfunction and pulmonary arterial hypertension and have been implicated as a causative factor for development of nonarteritic anterior ischemic optic neuropathy (NAION). Controversy remains regarding a cause and effect between PDE5I use and NAION because the mechanism by which NAION occurs is still not well understood. Because neuro-ophthalmologists have accepted that there is a potential relationship between ingestion of the PDE5I class of medications and NAION, the neuro-ophthalmologist should inquire about PDE5I use when evaluating a patient with a new diagnosis of NAION, and counsel patients regarding the implication of continued use of PDE5I...
February 2017: Neurologic Clinics
https://www.readbyqxmd.com/read/27883117/combination-therapies-for-improved-management-of-lower-urinary-tract-symptoms-benign-prostatic-hyperplasia
#12
C De Nunzio, F Presicce, A Tubaro
Several urological and non-urological conditions can contribute to the onset of lower urinary tract symptoms (LUTS), including benign prostatic hyperplasia (BPH), which is one of the main underlying causes in male patients. Six pharmacological classes (alpha-adrenoceptor blockers [ABs], 5alpha-reductase inhibitors [5ARIs], phytotherapeutics, antimuscarinics [AMs], beta3-adrenoceptor agonists and phosphodiesterase type 5 inhibitors [PDE5Is]) are available, alone or in combination, for the treatment of male LUTS...
September 2016: Drugs of Today
https://www.readbyqxmd.com/read/27879305/partial-segmental-thrombosis-of-the-corpus-cavernosum-presenting-with-perineal-pain
#13
Michelle Christodoulidou, Arie Parnham, Navin Ramachandran, Asif Muneer
We describe the case of a man aged 43 years who presented with a 2-week history of a palpable lump in the right proximal penile shaft. This was preceded by a 6-month history of perineal pain, accompanied by erectile dysfunction. An urgent MRI scan of his penis identified a thrombus within the right crus and corpus of the penis. His thrombophilia screen was normal. The patient was started on oral anticoagulation and a phosphodiesterase inhibitor (PDE-5i) to prevent thrombus progression and maintain erectile function...
November 22, 2016: BMJ Case Reports
https://www.readbyqxmd.com/read/27872007/the-role-of-pde5-inhibitors-and-the-no-cgmp-pathway-in-cancer
#14
REVIEW
Taylor C Peak, Ashley Richman, Serap Gur, Faysal A Yafi, Wayne J G Hellstrom
INTRODUCTION: Phosphodiesterase 5 (PDE5) inhibitors (PDE5i) have been used clinically for the treatment of erectile dysfunction, acting on the nitric oxide/cyclic guanosine monophosphate (NO/cGMP) signaling pathway. Simultaneously, researchers have elucidated the roles that this pathway plays in the regulation of cell proliferation, tumor development, and progression. As a result, our knowledge of PDE5i and cancer biology has expanded and provides an integration that holds great promise for some, but concern for others...
January 2016: Sexual Medicine Reviews
https://www.readbyqxmd.com/read/27871960/useful-implications-of-low-dose-long-term-use-of-pde-5-inhibitors
#15
REVIEW
Taymour Mostafa
INTRODUCTION: Phosphodiesterase type 5 (PDE-5) hydrolyzes cyclic guanylate monophosphate (cGMP) specifically to 5' GMP, promoting successful corporeal vascular relaxation and penile erection during sexual stimulation. Oral PDE-5 inhibitors such as sildenafil, vardenafil, tadalafil, and avanafil have provided noninvasive, effective, well-tolerated treatment for erectile dysfunction (ED) patients and, at the same time, stimulated both academic and clinical interests. Lately, some oral PDE-5 inhibitors were released as low-dose preparations with the concept of potential daily administration and long-term use...
July 2016: Sexual Medicine Reviews
https://www.readbyqxmd.com/read/27871958/current-perspectives-on-stem-cell-therapy-for-erectile-dysfunction
#16
REVIEW
Taylor C Peak, James Anaissie, Wayne J G Hellstrom
INTRODUCTION: Erectile dysfunction (ED) is a common sexual disorder that affects the lives of millions of male patients and their partners. Various medical and surgical therapies exist, with the most common being oral intake of phosphodiesterase 5 inhibitors. One therapeutic strategy in preclinical development to treat ED is stem cell transplantation. AIM: To examine the studies that have investigated stem cells for the treatment of ED. METHODS: A literature review was performed through PubMed focusing on stem cells and ED...
July 2016: Sexual Medicine Reviews
https://www.readbyqxmd.com/read/27869315/aminoalkyl-derivatives-of-8-alkoxypurine-2-6-diones-multifunctional-5-ht1a-5-ht7-receptor-ligands-and-pde-inhibitors-with-antidepressant-activity
#17
Grażyna Chłoń-Rzepa, Agnieszka Zagórska, Paweł Żmudzki, Adam Bucki, Marcin Kołaczkowski, Anna Partyka, Anna Wesołowska, Grzegorz Kazek, Monika Głuch-Lutwin, Agata Siwek, Gabriela Starowicz, Maciej Pawłowski
In the search for potential psychotropic agents, a new series of 3,7-dimethyl- and 1,3-dimethyl-8-alkoxypurine-2,6-dione derivatives of arylpiperazines, perhydroisoquinolines, or tetrahydroisoquinolines with flexible alkylene spacers (5-16 and 21-32) were synthesized and evaluated for 5-HT1A /5-HT7 receptor affinities as well as PDE4B1 and PDE10A inhibitory properties. The 1-(4-(4-(2-hydroxyphenyl)piperazin-1-yl)butyl)-3,7-dimethyl-8-propoxypurine-2,6-dione (16) and 7-(2-hydroxyphenyl)piperazinylalkyl-1,3-dimethyl-8-ethoxypurine-2,6-diones (31 and 32) as potent dual 5-HT1A /5-HT7 receptor ligands with antagonistic activity produced an antidepressant-like effect in the forced swim test in mice...
December 2016: Archiv der Pharmazie
https://www.readbyqxmd.com/read/27860455/papaverine-sensitive-phosphodiesterase-activity-is-measured-in-bovine-spermatozoa
#18
A Bergeron, A Hébert, C Guillemette, A Laroche, M-P Poulin, J P Aragon, P Leclerc, R Sullivan, P Blondin, C Vigneault, F J Richard
Cyclic adenosine monophosphate (cAMP) plays a crucial role as a signaling molecule for capacitation, motility, and acrosome reaction in mammalian spermatozoa. It is well-known that cAMP degradation by phosphodiesterase (PDE) enzyme has a major impact on sperm functions. This study was undertaken to characterize cAMP-PDE activity in bovine spermatozoa. Total cAMP-PDE activity in cauda epididymal and ejaculated spermatozoa was 543.2 ± 49.5 and 1252.6 ± 86.5 fmoles/min/10(6) spermatozoa, respectively. Using different family-specific PDE inhibitors, we showed that in cauda epididymal and ejaculated spermatozoa, the major cAMP-PDE activity was papaverine-sensitive (44...
November 16, 2016: Andrology
https://www.readbyqxmd.com/read/27859531/increase-of-intracellular-cyclic-amp-by-pde4-inhibitors-affects-hepg2-cell-cycle-progression-and-survival
#19
Mara Massimi, Silvia Cardarelli, Francesca Galli, Maria Federica Giardi, Federica Ragusa, Nadia Panera, Benedetta Cinque, Maria Grazia Cifone, Stefano Biagioni, Mauro Giorgi
Type 4 cyclic nucleotide phosphodiesterases (PDE4) are major members of a superfamily of enzymes (PDE) involved in modulation of intracellular signaling mediated by cAMP. Broadly expressed in most human tissues and present in large amounts in the liver, PDEs have in the last decade been key therapeutic targets for several inflammatory diseases. Recently, a significant body of work has underscored their involvement in different kinds of cancer, but with no attention paid to liver cancer. The present study investigated the effects of two PDE4 inhibitors, rolipram and DC-TA-46, on the growth of human hepatoma HepG2 cells...
November 16, 2016: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/27855624/the-women-s-heart-insights-into-new-potential-targeted-therapy
#20
Daniele Gianfrilli, Ricardo Pofi, Tiziana Feola, Andrea Lenzi, Elisa Giannetta
Cardiovascular disease represents an increasing cause of death in women. The analysis of cardiovascular risk factors in women has not reached a consensus with respect to a specific and personalized treatment designed in pre-menopausal and post-menopausal phases. Clinically significant cardioprotective and antiremodeling effects were detected in animal and human study exploring chronic inhibition of Phosphodiesterase type 5 (PDE5). The relationship between heart, estrogens and PDE5 inhibitors (PDE5i) remains unclear...
November 18, 2016: Current Medicinal Chemistry
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