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PDE 5 Inhibitors

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https://www.readbyqxmd.com/read/29916224/effect-of-phosphodiesterase-5-inhibition-on-joint-and-muscle-damage-in-rats-with-adjuvant-arthritis
#1
Faize Elif Bahadır, Mustafa Kutay Köroğlu, Meral Yüksel, Feriha Ercan, Y. İnci Alican
Background/aim: This study was designed to examine the effect of tadalafil, a phosphodiesterase (PDE)5 inhibitor, on the severity of joint and muscle damage in rats with adjuvant-induced arthritis (AA). Materials and methods: AA was induced by intradermal inoculation into right hind paw of male Sprague Dawley rats (300-450g) with complete Freund's adjuvant (CFA; 0.1 mL). AA rats were treated with either tadalafil (10 mg/kg; per oral) alone or along with the soluble guanylyl cyclase inhibitor 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ; 10 mg/kg; intraperitoneally)...
June 14, 2018: Turkish Journal of Medical Sciences
https://www.readbyqxmd.com/read/29909756/phosphodiesterase-5-inhibitors-in-chinese-tonic-liquors-by-liquid-chromatography-coupled-with-quadrupole-time-of-flight-mass-spectrometry
#2
Bo Ding, Zhiyuan Wang, Jianjun Xie, Guangfeng Zeng, Wenrui Chen
Chinese tonic liquor is an important dietary supplement in daily use, but it often happens that illicitly adulterated drugs in Chinese tonic liquor could lead to food safety issues. In this survey an analytical method consisting of a liquid chromatography quadrupole time of flight mass spectrometer (LC-Q-TOF-MS), coupled with QuEChERS pretreatment, was established for identification of phosphodiesterase type 5 enzyme (PDE-5) inhibitors in Chinese tonic liquors. 86 PDE-5 inhibitors were qualitatively analyzed by employing information dependent acquisition mass spectrometry (IDA-MS) in comparison with the accurate mass of the protonated molecular ion, isotopic pattern, library and chemical formula...
June 18, 2018: Food Additives & Contaminants. Part B, Surveillance
https://www.readbyqxmd.com/read/29901310/-current-role-of-sildenafil-in-the-management-of-erectile-dysfunction
#3
N D Akhvlediani, I P Matyukhov
Sildenafil is the first phosphodiesterase type 5 inhibitor (PDE-5), used in the management of erectile dysfunction (ED). The effectiveness and safety of the original drug have been studied most extensively among ED medications. Sildenafil has been successfully used for ED of different etiology and severity. To date, this PDE-5 remains the drug of choice for many patients with erectile dysfunction.
May 2018: Urologii︠a︡
https://www.readbyqxmd.com/read/29901304/-the-role-of-tadalafil-in-the-management-of-sexual-dysfunctions
#4
E A Efremov, E V Kasatonova, Ya I Mel'nik, A A Nikushina
Erectile dysfunction (ED) has a significant negative impact on the quality of life of the patients and their partners. The sequence and regimens of ED therapy have become quite evident since the advent of phosphodiesterase type 5 inhibitors (PDE-5). However, there have been continued basic research of the efficacy and safety of these agents and studies aimed at new therapeutic goals. In recent years, the attention of researchers has shifted into a wider range of issues related to the personalized PDE-5 therapy, including sexual satisfaction, psychosocial variables (e...
May 2018: Urologii︠a︡
https://www.readbyqxmd.com/read/29887595/utilization-and-prescription-patterns-of-phosphidiesterase-5-inhibitor-medications-in-the-united-states-military-health-system
#5
Jon Montgomery, Cathaleen Madsen, Todd Leroux, Tracey Pérez Koehlmoos
Phosphodiesterase-5 inhibitors (PDE-5Is) are the first-line medical treatments for erectile dysfunction (ED), but are often restricted in public formularies. This study assesses PDE-5I usage among active-duty service members before and after the addition of sildenafil to the formulary of the Military Health System (MHS) in 2012. To assess, a cross-sectional evaluation was conducted, utilizing encounter and pharmaceutical claims data from the Military Health System Data Repository between 2010 and 2014. Separate zero-inflated, negative binomial models were used to assess changes in usage rates by prescription and by number of pills issued, for 37 947 patients...
June 11, 2018: International Journal of Impotence Research
https://www.readbyqxmd.com/read/29886357/inhibition-of-pde3a-sustains-meiotic-arrest-and-gap-junction-of-bovine-growing-oocytes-in-in-vitro-growth-culture
#6
Md Hasanur Alam, Jibak Lee, Takashi Miyano
Bovine growing oocytes with a diameter of 105-115 μm from early antral follicles (1.2-1.8 mm) are able to resume meiosis, but lack the competence to mature to metaphase II. To confer full maturation competence onto the oocytes, culture systems which can support their growth and prevent their meiotic resumption during culture are needed. In this study, we cultured growing oocytes for 5 days to examine the effects of different phosphodiesterase (PDE) inhibitors on meiotic arrest and acquisition of full maturation competence of growing oocytes, and their gap junctional communication with cumulus cells...
May 25, 2018: Theriogenology
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
#7
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/29872554/phosphodiesterase-5-inhibition-reduces-postoperative-metastatic-disease-by-targeting-surgery-induced-myeloid-derived-suppressor-cell-dependent-inhibition-of-natural-killer-cell-cytotoxicity
#8
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/29867490/a-novel-catecholopyrimidine-based-small-molecule-pde4b-inhibitor-suppresses-inflammatory-cytokines-in-atopic-mice
#9
Baskaran Purushothaman, Parthasarathy Arumugam, Joon Myong Song
Degradation of cyclic adenosine mono phosphate (cAMP) by phosphodiesterase-4B (PDE-4B) in the inflammatory cells leads to elevated expression of inflammatory cytokines in inflammatory cells. Suppression of cytokines has proved to be beneficial in the treatment of atopic dermatitis (AD). Henceforth, application of PDE4B specific inhibitor to minimize the degradation of cAMP can yield better results in the treatment of AD. PDE4B specific inhibitor with a limited side effect is highly warranted. Herein, we synthesized a novel PDE4 inhibitor, compound 2 comprising catecholopyrimidine core functionalized with trifluoromethyl (-CF3 ) group...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29733479/levosimendan-differentially-modulates-electrophysiological-activities-of-sinoatrial-nodes-pulmonary-veins-and-the-left-and-right-atria
#10
Yung-Kuo Lin, Yao-Chang Chen, Yi-Ann Chen, Jen-Hung Huang, Shih-Ann Chen, Yi-Jen Chen
INTRODUCTION: Calcium overload increases the risk of atrial fibrillation (AF). Levosimendan, a calcium sensitizer, increases myofilament contractility. Clinical reports suggested that levosimendan might increase AF occurrence, but the electrophysiological effects of levosimendan on AF substrates and triggers (pulmonary veins, PVs) are not clear. METHODS AND RESULTS: Conventional microelectrodes were used to record action potentials (APs) in isolated rabbit PVs, sinoatrial nodes (SANs), the left atrium (LA), and right atrium (RA) before and after application of different concentrations of levosimendan with or without milrinone (a phosphodiesterase [PDE] III inhibitor), and glibenclamide (an ATP-sensitive potassium channel [KATP ] inhibitor)...
May 7, 2018: Journal of Cardiovascular Electrophysiology
https://www.readbyqxmd.com/read/29729992/proteomics-functional-characterization-and-antivenom-neutralization-of-the-venom-of-pakistani-russell-s-viper-daboia-russelii-from-the-wild
#11
Tasnim Faisal, Kae Yi Tan, Si Mui Sim, Naeem Quraishi, Nget Hong Tan, Choo Hock Tan
The venom proteome of wild Pakistani Russell's viper (Daboia russelii) was investigated through nano-ESI-LCMS/MS of the reverse-phase HPLC fractions. A total of 54 venom proteins were identified and clustered into 11 protein families. Phospholipase A2 (PLA2 , 63.8%) and Kunitz-type serine protease inhibitor (KSPI, 16.0%) were most abundant, followed by snake venom serine protease (SVSP, 5.5%, mainly Factor V activating enzyme), vascular endothelial growth factor (VEGF, 4.3%), snake venom metalloprotease (SVMP, 2...
May 3, 2018: Journal of Proteomics
https://www.readbyqxmd.com/read/29713919/phosphodiesterase-4-and-7-inhibitors-produce-protective-effects-against-high-glucose-induced-neurotoxicity-in-pc12-cells-via-modulation-of-the-oxidative-stress-apoptosis-and-inflammation-pathways
#12
Nazanin Namazi Sarvestani, Saeedeh Saberi Firouzi, Reza Falak, Mohammad Yahya Karimi, Mohammad Davoodzadeh Gholami, Akram Rangbar, Asieh Hosseini
Diabetic neuropathy (DN) is the most common diabetic complication. It is estimated diabetic population will increase to 592 million by the year 2035. This is while at least 50-60% of all diabetic patients will suffer from neuropathy in their lifetime. Oxidative stress, mitochondrial dysfunction, apoptosis, and inflammation are crucial pathways in development and progression of DN. Since there is also no selective and effective therapeutic agent to prevent or treat high glucose (HG)-induced neuronal cell injury, it is crucial to explore tools by which one can reduce factors related to these pathways...
April 30, 2018: Metabolic Brain Disease
https://www.readbyqxmd.com/read/29704309/the-neuroprotective-and-antidepressant-like-effects-of-hcyb1-a-novel-selective-pde2-inhibitor
#13
Li Liu, Jing Zheng, Xian-Feng Huang, Xia Zhu, Shu-Ming Ding, Heng-Ming Ke, James M O'Donnell, Han-Ting Zhang, Guo-Qiang Song, Ying Xu
AIMS: Depression is currently the most common mood disorder. Regulation of intracellular cyclic adenosine monophosphate (cAMP) and/or cyclic guanosine monophosphate (cGMP) signaling by phosphodiesterase (PDE) inhibition has been paid much attention for treatment of depression. This study aimed to investigate the neuroprotective effects of Hcyb1, a novel PDE2 inhibitor, in HT-22 cells and antidepressant-like effects in mouse models of depression. METHODS: Hcyb1 was synthesized and its selectivity upon PDE2 was tested...
July 2018: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/29672041/targeting-a-subpocket-in-trypanosoma-brucei-phosphodiesterase-b1-tbrpdeb1-enables-the-structure-based-discovery-of-selective-inhibitors-with-trypanocidal-activity
#14
Antoni R Blaazer, Abhimanyu K Singh, Erik de Heuvel, Ewald Edink, Kristina M Orrling, Johan J N Veerman, Toine van den Bergh, Chimed Jansen, Erin Balasubramaniam, Wouter J Mooij, Hans Custers, Maarten Sijm, Daniel N A Tagoe, Titilola D Kalejaiye, Jane C Munday, Hermann Tenor, An Matheeussen, Maikel Wijtmans, Marco Siderius, Chris de Graaf, Louis Maes, Harry P de Koning, David S Bailey, Geert Jan Sterk, Iwan J P de Esch, David G Brown, Rob Leurs
Several trypanosomatid cyclic nucleotide phosphodiesterases (PDEs) possess a unique, parasite-specific cavity near the ligand-binding region that is referred to as the P-pocket. One of these enzymes, Trypanosoma brucei PDE B1 (TbrPDEB1), is considered a drug target for the treatment of African sleeping sickness. Here, we elucidate the molecular determinants of inhibitor binding and reveal that the P-pocket is amenable to directed design. By iterative cycles of design, synthesis, and pharmacological evaluation and by elucidating the structures of inhibitor-bound TbrPDEB1, hPDE4B, and hPDE4D complexes, we have developed 4a,5,8,8a-tetrahydrophthalazinones as the first selective TbrPDEB1 inhibitor series...
May 10, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29568269/camp-catalyzing-phosphodiesterases-control-cholinergic-muscular-activity-but-their-inhibition-does-not-enhance-5-ht-4-receptor-mediated-facilitation-of-cholinergic-contractions-in-the-murine-gastrointestinal-tract
#15
Vicky Pauwelyn, Romain A Lefebvre
Background: As the signal transduction of 5-HT4 receptors on cholinergic neurons innervating smooth muscle is controlled by phosphodiesterase (PDE) 4 in porcine stomach and colon, and human large intestine, the in vivo gastroprokinetic effects of a 5-HT4 receptor agonist might be enhanced by combination with a selective PDE4 inhibitor. The presence of 5-HT4 receptors on cholinergic neurons towards murine gastrointestinal circular muscle was recently shown. If the control of this receptor pathway by PDE4 is also present in mice, this might be a good model for in vivo testing of the combination therapy...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29557941/effects-of-the-phosphodiesterase-5-pde-5-inhibitors-avanafil-and-zaprinast-on-bone-remodeling-and-oxidative-damage-in-a-rat-model-of-glucocorticoid-induced-osteoporosis
#16
Zübeyir Huyut, Nuri Bakan, Serkan Yıldırım, Hamit Hakan Alp
No abstract text is available yet for this article.
March 13, 2018: Medical Science Monitor Basic Research
https://www.readbyqxmd.com/read/29549244/effects-of-sildenafil-treatment-on-thermogenesis-and-glucose-homeostasis-in-diet-induced-obese-mice
#17
Kornelia Johann, Marlen Colleen Reis, Lisbeth Harder, Beate Herrmann, Sogol Gachkar, Jens Mittag, Rebecca Oelkrug
Stimulation of thermogenic pathways appears to be a promising approach to find new ways of tackling metabolic diseases like obesity and diabetes mellitus type 2. Thermogenic, weight reducing and insulin sensitizing effects of phosphodiesterase 5 (PDE 5) inhibitors have recently been postulated, suggesting that modulators of endogenous cGMP signaling have the therapeutic potential to treat metabolic disorders. However, most studies have been performed in vitro or in animals that were not glucose intolerant. We, thus, aimed to test the metabolic effects of the PDE 5 inhibitor sildenafil by treating diet-induced obese (DIO) mice orally for 8 days...
March 13, 2018: Nutrition & Diabetes
https://www.readbyqxmd.com/read/29501590/modeling-of-pharmacokinetics-efficacy-and-hemodynamic-effects-of-macitentan-in-patients-with-pulmonary-arterial-hypertension
#18
Andreas Krause, Jochen Zisowsky, Jasper Dingemanse
BACKGROUND: Macitentan is the first endothelin receptor antagonist with demonstrated efficacy on morbidity and mortality in pulmonary arterial hypertension (PAH) in the pivotal study SERAPHIN. METHODS: The pharmacokinetics (PK) of macitentan and its active metabolite, ACT-132577, were characterized in a population model. Efficacy and hemodynamics (pharmacodynamics, PD) were related to PK based on PK/PD modeling. RESULTS: Sex, age, and body weight influenced the PK to a statistically significant extent...
April 2018: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29484221/peyronie-s-disease-surgery-surgical-outcomes-of-268-cases
#19
Ateş Kadıoğlu, Emre Salabaş, Abdulkadir Özmez, Abdullah Feyyaz Ural, Ömer Barış Yücel, Mazhar Ortaç, Yaşar Pazır, Bahadır Ermeç
Objective: To assess the outcomes of the surgical techniques used in Peyronie's disease (PD) surgery. Material and methods: Two hundred and sixty-eight patients received surgical treatment for PD. Fifty four and 144 patients underwent simple corporoplasties (shortening procedure, SP, group 1) or plaque incision and grafting surgery (lengthening surgery, LP, group 2), respectively, whereas 70 patients with erectile dysfunction underwent penile prosthesis implantation...
January 2018: Turkish Journal of Urology
https://www.readbyqxmd.com/read/29477888/synthesis-and-molecular-docking-of-new-roflumilast-analogues-as-preferential-selective-potent-pde-4b-inhibitors-with-improved-pharmacokinetic-profile
#20
Bahia A Moussa, Asmaa A El-Zaher, Mohamed K El-Ashrey, Marwa A Fouad
In the present work, we designed and synthesized new roflumilast analogues with preferential-selective PDE-4B inhibition activity and improved pharmacokinetic properties. The unsubstituted benzo[d]thiazol-2-yl and -6-yl benzamide derivatives (4a and 6a) showed both good potency and preferential selectivity for PDE-4B. More remarkably, 6c revealed 6 times preferential PDE-4B/4D selectivity with a significant increase of in vitro cAMP and good % inhibition of TNF-α concentration. In addition, the in vitro pharmacokinetics of 6c showed good metabolic stability with in vitro CLint (5...
March 25, 2018: European Journal of Medicinal Chemistry
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