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PDE5 Inhibitors

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https://www.readbyqxmd.com/read/28986358/pulmonary-vasodilation-by-phosphodiesterase-5-inhibition-is-enhanced-and-nitric-oxide-independent-in-early-pulmonary-hypertension-after-myocardial-infarction
#1
Richard W B van Duin, Birgit Houweling, Andre Uitterdijk, Dirk J Duncker, Daphne Merkus
Myocardial infarction (MI) may result in pulmonary hypertension (PH). Inhibition of phosphodiesterase 5 (PDE5), the enzyme responsible for the breakdown of cGMP in vascular smooth muscle, has become part of the contemporary therapeutic armamentarium for pulmonary arterial hypertension and may also be of benefit in PH secondary to MI. Nitric oxide (NO) is an important source of cGMP and can be enhanced in early PH and decreased in severe PH. In the present study we investigated if PDE5-inhibition ameliorates pulmonary hemodynamics in swine with PH secondary to MI and whether NO is essential...
October 6, 2017: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/28985058/identification-of-a-novel-1-2-3-4-tetrahydrobenzo-b-1-6-naphthyridine-analog-as-a-potent-phosphodiesterase-5-inhibitor-with-improved-aqueous-solubility-for-the-treatment-of-alzheimer-s-disease
#2
Jole Fiorito, Jeremie Vendome, Faisal Saeed, Agnieszka Staniszewski, Hong Zhang, Shijun Yan, Shi-Xian Deng, Ottavio Arancio, Donald W Landry
Phosphodiesterase 5 (PDE5) hydrolyzes cyclic guanosine monophosphate (cGMP) leading to increased levels of cAMP response element binding protein (CREB), a transcriptional factor involved with learning and memory processes. We previously reported potent quinoline-based PDE5 inhibitors (PDE5Is) for the treatment of Alzheimer's disease (AD). However, the low aqueous solubility rendered them undesirable drug candidates. Here we report a series of novel PDE5Is with two new scaffolds, 1,2,3,4-tetrahydrobenzo[b][1,6]naphthyridine and 2,3-dihydro-1H-pyrrolo[3,4-b]quinolin-1-one...
October 6, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28977106/daily-use-of-phosphodiesterase-type-5-inhibitors-as-prevention-for-recurrent-priapism
#3
Archimedes Nardozza, Marcelo Rodrigues Cabrini
OBJECTIVE: The pathogenesis of recurrent priapism is currently being investigated based on the regulation of the phosphodiesterase 5 (PDE5) enzyme. We explored the daily use of PDE5 inhibitors to treat and prevent priapism recurrences. METHOD: We administered PDE5 inhibitors using a long-term therapeutic regimen in seven men with recurrent priapism, with a mean age of 29.2 years (range 21 to 35 years). Six men (85.7%) had idiopathic priapism recurrences and one man (24...
August 2017: Revista da Associação Médica Brasileira
https://www.readbyqxmd.com/read/28964803/cyclic-guanosine-monophosphate-modulates-accumulation-of-phosphodiesterase-5-inhibitors-in-human-platelets
#4
Gzona Bajraktari, Jürgen Burhenne, Peter Bugert, Walter Emil Haefeli, Johanna Weiss
Sildenafil and tadalafil are widely-used phosphodiesterase 5 (PDE5) inhibitors for which no clear dose-response relationship could be established. Using isolated and/or recombinant PDE5, it has been demonstrated that cGMP can increase the affinity of this enzyme for sildenafil and tadalafil. We thus hypothesized that in cells expressing the nitric oxide - soluble guanylyl cyclase - cyclic guanosine monophosphate - PDE5 (NO-sGC-cGMP-PDE5) pathway such as platelets, the presence of NO increases the intracellular cGMP content and thus promotes the intracellular accumulation of sildenafil or tadalafil...
September 27, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28956417/potential-risk-of-developing-herpes-simplex-encephalitis-in-patients-treated-with-sildenafil-following-primary-exposure-to-genital-herpes
#5
A Goren, J Mccoy, M Kovacevic, M Situm, N Lonky
Herpes simplex encephalitis (HSE) is associated with significant mortality and morbidity. As a consequence of HSE, up to 75% of infected individuals die or experience irreversible neurological damage. While the pathogenesis of the disease is unknown, it is traditionally hypothesized that the viral infection occurs by neuronal transmission directly from peripheral sites. Non-neuronal modes of infection have generally been overlooked as the brain is protected by the blood-brain-barrier (BBB). The BBB poses an effective barrier to pathogens as well as to drugs such as chemotherapies...
July 2017: Journal of Biological Regulators and Homeostatic Agents
https://www.readbyqxmd.com/read/28956342/genetic-understanding-of-stroke-treatment-potential-role-for-phosphodiesterase-inhibitors
#6
Anjana Munshi, Satrupa Das
Phosphodiesterase (PDE) gene family is a large family having at least 21 genes and multiple versions (isoforms) of the phosphodiesterase enzymes. These enzymes catalyze the inactivation of intracellular mediators of signal transduction such as cAMP and cGMP and therefore, play a pivotal role in various cellular functions. PDE inhibitors (PDEI) are drugs that block one or more of the five subtypes of the PDE family and thereby prevent inactivation of the intracellular cAMP and cGMP by the respective PDE-subtypes...
2017: Advances in Neurobiology
https://www.readbyqxmd.com/read/28956332/from-age-related-cognitive-decline-to-alzheimer-s-disease-a-translational-overview-of-the-potential-role-for-phosphodiesterases
#7
Pim R A Heckman, Arjan Blokland, Jos Prickaerts
Phosphodiesterase inhibitors (PDE-Is) are pharmacological compounds enhancing cAMP and/or cGMP signaling. Both these substrates affect neural communication by influencing presynaptic neurotransmitter release and postsynaptic intracellular pathways after neurotransmitter binding to its receptor. Both cAMP and cGMP play an important role in a variety of cellular functions including neuroplasticity and neuroprotection. This chapter provides a translational overview of the effects of different classes of PDE-Is on cognition enhancement in age-related cognitive decline and Alzheimer's disease (AD)...
2017: Advances in Neurobiology
https://www.readbyqxmd.com/read/28955799/liposomal-delivery-of-phosphodiesterase-5-inhibitors-augments-ut-15c-stimulated-atp-release-from-human-erythrocytes
#8
Elizabeth A Bowles, Dimitri Feys, Nuran Ercal, Randy S Sprague
The use of liposomes to affect targeted delivery of pharmaceutical agents to specific sites may result in the reduction of side effects and an increase in drug efficacy. Since liposomes are delivered intravascularly, erythrocytes, which constitute almost half of the volume of blood, are ideal targets for liposomal drug delivery. In vivo, erythrocytes serve not only in the role of oxygen transport but also as participants in the regulation of vascular diameter through the regulated release of the potent vasodilator, adenosine triphosphate (ATP)...
December 2017: Biochemistry and Biophysics Reports
https://www.readbyqxmd.com/read/28952072/role-of-the-unfolded-protein-response-in-determining-the-fate-of-tumor-cells-and-the-promise-of-multi-targeted-therapies
#9
REVIEW
Kunyu Shen, David W Johnson, David A Vesey, Michael A McGuckin, Glenda C Gobe
Although there have been advances in our understanding of carcinogenesis and development of new treatments, cancer remains a common cause of death. Many regulatory pathways are incompletely understood in cancer development and progression, with a prime example being those related to the endoplasmic reticulum (ER). The pathological sequelae that arise from disruption of ER homeostasis are not well defined. The ER is an organelle that is responsible for secretory protein biosynthesis and the quality control of protein folding...
September 27, 2017: Cell Stress & Chaperones
https://www.readbyqxmd.com/read/28938916/use-of-the-kladh3-promoter-for-the-quantitative-production-of-the-murine-pde5a-isoforms-in-the-yeast-kluyveromyces-lactis
#10
Silvia Cardarelli, Mauro Giorgi, Fabio Naro, Francesco Malatesta, Stefano Biagioni, Michele Saliola
BACKGROUND: Phosphodiesterases (PDE) are a superfamily of enzymes that hydrolyse cyclic nucleotides (cAMP/cGMP), signal molecules in transduction pathways regulating crucial aspects of cell life. PDEs regulate the intensity and duration of the cyclic nucleotides signal modulating the downstream biological effect. Due to this critical role associated with the extensive distribution and multiplicity of isozymes, the 11 mammalian families (PDE1 to PDE11) constitute key therapeutic targets...
September 22, 2017: Microbial Cell Factories
https://www.readbyqxmd.com/read/28922964/oral-treprostinil-in-the-treatment-of-pulmonary-arterial-hypertension
#11
Jeremy Feldman, Naomi Habib, John Radosevich, Mohan Dutt
Pulmonary arterial hypertension (PAH) is a rare disease resulting in progressive remodeling of the pulmonary vasculature and eventual right ventricular failure. Despite the development of 13 therapies for PAH since 2000, the use of continuously infused prostanoids retains a special role. Infused medications present unique challenges, and the search for an efficacious oral prostanoid culminated in the FDA approval of oral treprostinil - a first in class oral prostanoid medication approved to treat pulmonary arterial hypertension (PAH)...
October 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28888986/pde-5-inhibitor-improves-insulin-sensitivity-by-enhancing-mitochondrial-function-in-adipocytes
#12
Hea Min Yu, Hyo Kyun Chung, Koon Soon Kim, Jae Min Lee, Jun Hwa Hong, Kang Seo Park
Adipocytes are involved in many metabolic disorders. It was recently reported that phosphodiesterase type 5 (PDE5) is expressed in human adipose tissue. In addition, PDE5 inhibitors have been shown to improve insulin sensitivity in humans. However, the mechanism underlying the role of PDE5 inhibitors as an insulin sensitizer remains largely unknown. The present study was undertaken to investigate the role of the PDE5 inhibitor udenafil in insulin signaling in adipocytes and whether this is mediated through the regulation of mitochondrial function...
November 4, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28860509/age-related-differences-in-responsiveness-to-sildenafil-and-tamsulosin-are-due-to-myogenic-smooth-muscle-tone-in-the-human-prostate
#13
Sophie N Lee, Basu Chakrabarty, Brad Wittmer, Melissa Papargiris, Andrew Ryan, Mark Frydenberg, Nathan Lawrentschuk, Ralf Middendorff, Gail P Risbridger, Stuart J Ellem, Betty Exintaris
Lower urinary tract symptoms (LUTS) due to Benign Prostatic Hyperplasia (BPH) are highly prevalent in older men, having a profound impact on patient quality of life. Current therapeutics for BPH/LUTS target neurogenic smooth muscle tone, but response is unpredictable and many patients fail to respond. Spontaneous myogenic tone is another component of smooth muscle contractility that is uncharacterized in human prostate. To better understand and improve the predictability of patient response, we defined myogenic contractility using human prostate specimens and examined the effect of existing therapeutics...
August 31, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28830281/administration-of-daily-5%C3%A2-mg-tadalafil-improves-endothelial-function-in-patients-with-benign-prostatic-hyperplasia
#14
Toshiyasu Amano, Carolyn Earle, Tetsuya Imao, Yuki Matsumoto, Takahiro Kishikage
INTRODUCTION: Tadalafil is a promising phosphodiesterase (PDE) 5 inhibitor prescribed for erectile dysfunction (ED). Daily low dose (5 mg) of tadalafil has also been used for the treatment of male lower urinary tract symptoms (LUTS) associated with benign prostate hyperplasia (BPH). PDE5 inhibitors induce relaxation of smooth muscle cells in the urethra, prostate, bladder neck, and blood vessels. The aim of this study was to investigate the efficacy of tadalafil on vessels endothelial function, in patients with male LUTS symptoms associated with BPH...
August 22, 2017: Aging Male: the Official Journal of the International Society for the Study of the Aging Male
https://www.readbyqxmd.com/read/28798396/flavonoid-glycosides-isolated-from-epimedium-brevicornum-and-their-estrogen-biosynthesis-promoting-effects
#15
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
#16
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/28776160/-acute-monocular-loss-of-vision-differential-diagnostic-considerations-apart-from-the-internistic-etiological-clarification
#17
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
#18
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/28729555/inhibition-of-phosphodiesterase-5-suppresses-calcineurin-nfat-mediated-trpc6-expression-in-pulmonary-artery-smooth-muscle-cells
#19
Shaojun Li, Yilin Pan, Rui Ke, Xinming Xie, Cui Zhai, Wenhua Shi, Jian Wang, Xin Yan, Limin Chai, Qingting Wang, Qianqian Zhang, Xiaofan Su, Lan Yang, Li Gao, Manxiang Li
The up-regulation of transient receptor potential channel 6 (TRPC6) has been found to contribute to the proliferation of pulmonary artery smooth muscle cells (PASMCs), and inhibition of phosphodiesterase-5 (PDE5) has been shown to suppress TRPC6 expression in PASMCs. However, the molecular mechanisms underlying the up-regulation of TRPC6 expression and PDE5 modulation of TRPC6 expression in PASMCs remain largely unclear. The aim of this study is to address these issues. Endothelin-1 (ET-1) dose and time-dependently up-regulated TRPC6 expression in primary cultured rat PASMCs, and this was accompanied with the activation of calcineurin and subsequent translocation of NFATc4 to the nucleus...
July 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28728871/phosphodiesterase-type-5-inhibitors-and-risk-of-melanoma-a-meta-analysis
#20
Huilin Tang, Wenting Wu, Shuangshuang Fu, Suodi Zhai, Yiqing Song, Jiali Han
BACKGROUND: The association between phosphodiesterase type 5 (PDE5) inhibitors and melanoma risk is controversial. OBJECTIVE: We quantify the association between use of PDE5 inhibitors and melanoma. METHODS: We systematically searched PubMed, Embase, the Cochrane Central Register of Controlled Trials, Web of Science, and ClinicalTrials.gov for studies that were conducted up to July 13, 2016, and evaluated the association between PDE5 inhibitors and skin cancer...
September 2017: Journal of the American Academy of Dermatology
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