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PDE inhibitor.

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https://www.readbyqxmd.com/read/28338622/phosphodiesterase-inhibitors-as-a-therapeutic-approach-to-neuroprotection-and-repair
#1
REVIEW
Eric P Knott, Mazen Assi, Sudheendra N R Rao, Mousumi Ghosh, Damien D Pearse
A wide diversity of perturbations of the central nervous system (CNS) result in structural damage to the neuroarchitecture and cellular defects, which in turn are accompanied by neurological dysfunction and abortive endogenous neurorepair. Altering intracellular signaling pathways involved in inflammation and immune regulation, neural cell death, axon plasticity and remyelination has shown therapeutic benefit in experimental models of neurological disease and trauma. The second messengers, cyclic adenosine monophosphate (cyclic AMP) and cyclic guanosine monophosphate (cyclic GMP), are two such intracellular signaling targets, the elevation of which has produced beneficial cellular effects within a range of CNS pathologies...
March 24, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28337525/phosphodiesterase-1b-pde1b-knockout-mice-are-resistant-to-forced-swim-and-tail-suspension-induced-immobility-and-show-upregulation-of-pde10a
#2
Jillian R Hufgard, Michael T Williams, Matthew R Skelton, Olivera Grubisha, Filipa M Ferreira, Helen Sanger, Mary E Wright, Tracy M Reed-Kessler, Kurt Rasmussen, Ronald S Duman, Charles V Vorhees
RATIONALE: Major depressive disorder is a leading cause of suicide and disability. Despite this, current antidepressants provide insufficient efficacy in more than 60% of patients. Most current antidepressants are presynaptic reuptake inhibitors; postsynaptic signal regulation has not received as much attention as potential treatment targets. OBJECTIVES: We examined the effects of disruption of the postsynaptic cyclic nucleotide hydrolyzing enzyme, phosphodiesterase (PDE) 1b, on depressive-like behavior and the effects on PDE1B protein in wild-type (WT) mice following stress...
March 23, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28330503/caffeine-modulates-glucocorticoid-induced-expression-of-ctgf-in-lung-epithelial-cells-and-fibroblasts
#3
Markus Fehrholz, Kirsten Glaser, Christian P Speer, Silvia Seidenspinner, Barbara Ottensmeier, Steffen Kunzmann
BACKGROUND: Although caffeine and glucocorticoids are frequently used to treat chronic lung disease in preterm neonates, potential interactions are largely unknown. While anti-inflammatory effects of glucocorticoids are well defined, their impact on airway remodeling is less characterized. Caffeine has been ascribed to positive effects on airway inflammation as well as remodeling. Connective tissue growth factor (CTGF, CCN2) plays a key role in airway remodeling and has been implicated in the pathogenesis of chronic lung diseases such as bronchopulmonary dysplasia (BPD) in preterm infants...
March 23, 2017: Respiratory Research
https://www.readbyqxmd.com/read/28316997/sildenafil-can-affect-innate-and-adaptive-immune-system-in-both-experimental-animals-and-patients
#4
REVIEW
Monika Kniotek, Agnieszka Boguska
Sildenafil, a type 5 phosphodiesterase inhibitor (PDE5-I), is primarily used for treating erectile dysfunction. Sildenafil inhibits the degradation of cyclic guanosine monophosphate (cGMP) by competing with cGMP for binding site of PDE5. cGMP is a secondary messenger activating protein kinases and a common regulator of ion channel conductance, glycogenolysis, and cellular apoptosis. PDE5 inhibitors (PDE-Is) found application in cardiology, nephrology, urology, dermatology, oncology, and gynecology. Positive result of sildenafil treatment is closely connected with its immunomodulatory effects...
2017: Journal of Immunology Research
https://www.readbyqxmd.com/read/28306529/in-vitro-inhibition-of-phosphodiesterase-5-and-arginase-activities-from-rat-penile-tissue-by-two-nigerian-herbs-hunteria-umbellata-and-anogeissus-leiocarpus
#5
Ganiyu Oboh, Adeniyi Abiodun Adebayo, Ayokunle Olubode Ademosun, Aline August Boligon
BACKGROUND: Anogeissus leiocarpus and Hunteria umbellata have been reportedly used in traditional medicine for the management of erectile dysfunction (ED). However, the scientific basis for their use has not been well established. Therefore, this study was designed to investigate the inhibitory effects of water extractable phytochemicals of H. umbellata and A. leiocarpus on phosphodiesterase-5 (PDE-5) and arginase as well as pro-oxidants induced lipid peroxidation in rat penile tissue...
March 17, 2017: Journal of Basic and Clinical Physiology and Pharmacology
https://www.readbyqxmd.com/read/28302034/co-morbid-erectile-dysfunction-ed-and-antidepressant-treatment-in-a-patient-a-management-challenge
#6
Maszaidi Zainol, Hatta Sidi, Jaya Kumar, Srijit Das, Shaiful Ismail, Muhammad Hizri Hatta, Najwa Baharudin, Arun Ravindran
Across the globe, antidepressants (AD) and phosphodiesterase-5 inhibitors (PDE-5i) are commonly prescribed psychopharmacological agents for patients with co-morbid mental-health problem and sexual dysfunction (SD). The serotonergic and/or noradrenergic ADs, although is an effective agent are not without SD side-effects, especially erectile dysfunction (ED). ED is an inability to achieve, or maintain an erection for satisfactory sexual intercourse during the phases of male's sexual arousal. It is recognized as an important reason why non-adherence to treatment was observed in patients who are on AD...
March 15, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28267871/effect-of-bucladesine-pentoxifylline-and-h-89-as-cyclic-adenosine-monophosphate-analog-phosphodiesterase-and-protein-kinase-a-inhibitor-on-acute-pain
#7
Forouz Salehi, Mahshid Sadat Hosseini-Zare, Haleh Aghajani, Yalda Seyedi, Maryam Sadat Hosseini-Zare, Mohammad Sharifzadeh
The aim of the present study was to determine the effects of Cyclic adenosine monophosphate (cAMP) and its dependent pathway on thermal nociception in a mouse model of acute pain. Here we studied the effect of H-89 (protein kinase A inhibitor), Bucladesine (Db-cAMP) (membrane permeable analog of cAMP) and pentoxifylline (PTX) (non-specific phosphodiesterase (PDE) inhibitor) on pain sensation. Different doses of H-89 (0.05, 0.1 and 0.5 mg/100g), PTX (5, 10 and 20 mg/100g), and Db-cAMP (50, 100 and 300 nM/mouse) were administered intraperitoneally (I...
March 7, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28263828/6-hydroxy-5-7-dimethoxy-flavone-suppresses-the-neutrophil-respiratory-burst-via-selective-pde4-inhibition-to-ameliorate-acute-lung-injury
#8
Yung-Fong Tsai, Tzu-Chi Chu, Wen-Yi Chang, Yang-Chang Wu, Fang-Rong Chang, Shun-Chin Yang, Tung-Ying Wu, Yu-Ming Hsu, Chun-Yu Chen, Shih-Hsin Chang, Tsong-Long Hwang
Over-activated neutrophils produce enormous oxidative stress and play a key role in the development of acute and chronic inflammatory diseases. 6-Hydroxy-5,7-dimethoxy-flavone (UFM24), a flavone isolated from the Annonaceae Uvaria flexuosa, showed inhibitory effects on human neutrophil activation and salutary effects on lipopolysaccharide (LPS)-induced acute lung injury (ALI) in mice. UFM24 potently inhibited superoxide anion (O2(•-)) generation, reactive oxidants, and CD11b expression, but not elastase release, in N-formyl-l-methionyl-l-leucyl-l-phenylalanine (fMLF)-activated human neutrophils...
March 3, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28258674/ibudilast-a-non%C3%A2-selective-phosphodiesterase-inhibitor-in-brain-disorders
#9
Joanna Schwenkgrub, Małgorzata Zaremba, Dagmara Mirowska-Guzel, Iwona Kurkowska-Jastrzębska
Ibudilast (IBD) is a non‑selective (3, 4, 10, 11) phosphodiesterase (PDE) inhibitor, used mainly as a bronchodilator for the treatment of bronchial asthma. PDE play a central role in cellular function (e.g. differentiation, synaptic plasticity and inflammatory response) by metabolizing cyclic nucleotides. The results from preclinical and clinical studies indicate that IBD has a broader range of action through suppression of pro‑inflammatory cytokines (IL‑6, IL‑1β, TNF‑α), toll‑like receptor 4 blockade (TLR‑4), inhibition of a macrophage migration inhibitory factor (MIF), up‑regulation the anti‑inflammatory cytokine (IL‑10), and promotion of neurotrophic factors (GDNF, NGF, NT‑4)...
March 2, 2017: Postȩpy Higieny i Medycyny Doświadczalnej
https://www.readbyqxmd.com/read/28256546/promoting-in-vivo-remyelination-with-small-molecules-a-neuroreparative-pharmacological-treatment-for-multiple-sclerosis
#10
Eva María Medina-Rodríguez, Ana Bribián, Amanda Boyd, Valle Palomo, Jesús Pastor, Alfonso Lagares, Carmen Gil, Ana Martínez, Anna Williams, Fernando de Castro
Multiple Sclerosis (MS) is a neurodegenerative disease where immune-driven demyelination occurs with inefficient remyelination, but therapies are limited, especially those to enhance repair. Here, we show that the dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, VP3.15, a heterocyclic small molecule with good pharmacokinetic properties and safety profile, improves in vivo remyelination in mouse and increases both adult mouse and adult human oligodendrocyte progenitor cell (OPC) differentiation, in addition to its immune regulatory action...
March 3, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28248033/-contemporary-aspects-of-using-sildenafil
#11
E A Efremov, E V Kasatonova, Ya I Melnik, V V Simakov
Sildenafil has been thoroughly studied in 74 registered double-blind, placebo-controlled clinical trials assessing the efficacy and safety of the drug in a total of more than 16 000 men with erectile dysfunction (ED). However, practicing urologists have some questions regarding administering the drug in patients with multiple comorbidities. In this review, on a par with the now "classic" research, we outline the latest updates of meta-analyzes and comparative studies relating to the use of sildenafil in different groups of patients...
November 2016: Urologii︠a︡
https://www.readbyqxmd.com/read/28248021/-new-data-on-the-effectiveness-of-tadalafil-alone-and-in-combination-with-neyrodoz-in-treating-erectile-dysfunction-associated-with-secondary-premature-ejaculation
#12
N D Akhvlediani, I P Matyukhov
AIM: To compare the effectiveness of the phosphodiesterase type 5 inhibitor (PDE-5i) tadalafil alone and in combination with a biologically active dietary supplement (BADS) NeyroDoz, containing the precursors of serotonin in patients with erectile dysfunction (ED) associated with secondary premature ejaculation (SPE). MATERIAL AND METHODS: 105 patients (mean age 36.2+/-9.1 years) with concomitant ED and SPE were included in a prospective study and divided into 2 groups...
November 2016: Urologii︠a︡
https://www.readbyqxmd.com/read/28243607/treatment-with-sildenafil-and-donepezil-improves-angiogenesis-in-experimentally-induced-critical-limb-ischemia
#13
Ioana M Constantinescu, Pompei Bolfa, Dan Constantinescu, Aurel I Mironiuc, Claudia D Gherman
Objectives. In this study, we aimed to demonstrate the role of sildenafil (an antagonist of phosphodiesterase type 5 (PDE-5)) and donepezil (a specific and reversible inhibitor of acetylcholinesterase (Ach)) in increasing ischemia-induced angiogenesis. Method. Critical limb ischemia was induced by ligation of the common femoral artery followed by ligation of the common iliac artery. The operated animals were divided into 3 groups: receiving sildenafil, receiving donepezil, and surgery alone; the contralateral lower limb was used as a negative control...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28243299/assessment-of-the-role-of-no-cgmp-pathway-in-orthodontic-tooth-movement-using-pde5-inhibitors-an-animal-study
#14
Amir Hossein Mirhashemi, Mohammad Sadegh Ahmad Akhoundi, Rezvaneh Ghazanfari, Shahroo Etemad-Moghadam, Mojgan Alaeddini, Azam Khorshidian, Ahmad Reza Dehpour, Nafiseh Momeni
OBJECTIVES: Nitric oxide (NO) is a signaling molecule that mediates mechanical bone loading. Cyclic guanosine 3', 5' monophosphate (cGMP) is a NO-induced effector molecule. The aim of this study was to assess the effect of NO-cGMP pathway on orthodontic tooth movement (OTM) in rats by use of two phosphodiesterase 5 (PDE5) inhibitors namely sildenafil and tadalafil as chemical tools. MATERIALS AND METHODS: Forty-five male Wistar rats were divided into three equal groups (n=15) based on the substance they received...
November 2016: Journal of Dentistry of Tehran University of Medical Sciences
https://www.readbyqxmd.com/read/28235796/pulmonary-hypertension-therapy-and-a-systematic-review-of-efficacy-and-safety-of-pde-5-inhibitors
#15
REVIEW
Chinwe Unegbu, Corina Noje, John D Coulson, Jodi B Segal, Lewis Romer
Pulmonary hypertension (PH) is a syndrome that is of growing concern to pediatricians worldwide. Recent data led to concerns about the safety of phosphodiesterase type 5 (PDE5) inhibitors in children and a US Food and Drug Administration safety advisory. Our objective is to provide insight into therapies for PH in children and to systematically review the comparative effectiveness and safety of PDE5 inhibitors in the management of pediatric patients with PH. We searched the following databases through February 2015: Medline, Embase, SCOPUS, and the Cochrane Central Register of Controlled Trials...
March 2017: Pediatrics
https://www.readbyqxmd.com/read/28217446/the-dangers-of-sexual-enhancement-supplements-and-counterfeit-drugs-to-treat-erectile-dysfunction
#16
REVIEW
Jason Chiang, Faysal A Yafi, Philip J Dorsey, Wayne J G Hellstrom
Counterfeit phosphodiesterase-5 inhibitors (PDE-5i) are an increasing problem. Already in widespread use, the market for PDE-5i is steadily growing as the population ages. Counterfeiters are taking advantage of this growing market by developing illicit and counterfeit PDE-5i products. Many factors are contributing to the rapid growth of the illicit market, such as the low risk of prosecution, potentially high financial reward, and ease of distribution via Internet pharmacies. Consumers of illicit PDE-5i often do not realize they are using counterfeit products and placing themselves at an unnecessary health risk...
February 2017: Translational Andrology and Urology
https://www.readbyqxmd.com/read/28215172/the-phosphodiesterase-5-inhibitors-pde-5i-for-erectile-dysfunction-ed-a-therapeutic-challenge-for-psychiatrists
#17
Chong Siew Koon, Hatta Sidi, Jaya Kumar, Srijit Das, Ong Wan Xi, Muhammad Hizri Hatta, Cesar Alfonso
Erectile function (EF) is a prerequisite for satisfactory sexual intercourse (SI) and central to male sexual functioning. Satisfactory SI eventually leads to orgasm - a biopsychophysiological state of euphoria - leading to a sense of bliss, enjoyment and positive mental well being. For a psychiatrist, treating ED is self-propelled to harmonize these pleasurable experiences alongside with encouragement of physical wellness and sensuality. Hence, the role of PDE-5i is pivotal in the context of treating ED constitutes a therapeutic challenge...
February 15, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28204955/inactivation-of-non-canonical-cyclic-nucleotides-hydrolysis-and-transport
#18
Erich H Schneider, Roland Seifert
This chapter addresses cNMP hydrolysis by phosphodiesterases (PDEs) and export by multidrug resistance associated proteins (MRPs). Both mechanisms are well-established for the canonical cNMPs, cAMP, and cGMP. Increasing evidence shows that non-canonical cNMPs (specifically cCMP, cUMP) are also PDE and MRP substrates. Hydrolysis of cUMP is achieved by PDE 3A, 3B, and 9A, which possibly explains the cUMP-degrading activities previously reported for heart, adipose tissue, and brain. Regarding cCMP, the only known "conventional" (class I) PDE that hydrolyzes cCMP is PDE7A...
February 16, 2017: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28159622/the-discovery-complex-crystal-structure-and-recognition-mechanism-of-a-novel-natural-pde4-inhibitor-from-selaginella-pulvinata
#19
Yiyou Huang, Xin Liu, Deyan Wu, Guihua Tang, Zengwei Lai, Xuehua Zheng, Sheng Yin, Hai-Bin Luo
Phosphodiesterase-4 (PDE4) is an important drug target for treatment of inflammation-related diseases. Till now, natural PDE4 inhibitors are rare and their co-crystal structures with PDE4 are hardly available. In the present study, selaginpulvilins K and L (1 and 2), two novel fluorene derivatives, were isolated from a traditional Chinese medicine Selaginella pulvinata and exhibited remarkable inhibition against phosphodiesterase-4D (PDE4D) at IC50 11nM and 90nM, respectively. Compound 1 also showed a good selectivity across PDE families with the selective fold ranging from 30 to 909...
January 31, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28152479/inhibitor-of-phosphodiestearse-4-improves-memory-deficits-oxidative-stress-neuroinflammation-and-neuropathological-alterations-in-mouse-models-of-dementia-of-alzheimer-s-type
#20
Amit Kumar, Nirmal Singh
The study investigates the potential of Rolipram a phosphodiesterase-4 inhibitor in cognitive deficits induced by streptozotocin (STZ, 3mg/kg intracerebroventricularly) and natural ageing in mice. Morris water maze (MWM) test was employed to evaluate learning and memory of the animals. Extent of oxidative stress was measured by estimating the levels of brain glutathione (GSH) and thiobarbituric acid reactive species (TBARS). Brain acetylcholinestrase (AChE) activity was also estimated. The brain activity of myeloperoxidase (MPO) was measured as a marker of inflammation...
April 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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