scholarly journals Does levosimendan act as a Ca2+sensitizer or PDE3 inhibitor?: Commentary on Orstaviket al., Br J Pharmacol 171: 5169-5181

2015 ◽  
Vol 172 (18) ◽  
pp. 4594-4596 ◽  
Author(s):  
Masao Endoh
Keyword(s):  
Pde3 Inhibitor

Antiplatelet Therapy Using Cilostazol, a Specific PDE3 Inhibitor

1999 ◽  
Vol 82 (08) ◽  
pp. 435-438 ◽  
Author(s):  
Yasuo Ikeda
Keyword(s):  
Arterial Occlusion ◽  
Cyclic Adenosine Monophosphate ◽  
Adenosine Monophosphate ◽  
The United States ◽  
Peripheral Blood Flow ◽  
Antithrombotic Agent ◽  
United States Food ◽  
States Food ◽  
Peripheral Arterial ◽  
Pde3 Inhibitor

IntroductionCilostazol, 6-[ 4-( l-cyclohexy l-IH-tetrazol-5yl ) butoxy ]-3, 4-dihydro-2 (1H)-quinolinone, is an antiplatelet/ antithrombotic agent that has been used since 1988 in several countries, including Japan, for treatment of chronic peripheral arterial occlusion. Cilostazol was also approved by the United States Food and Drug Administration (FDA) in 1999 for the treatment of intermittent claudication. Cilostazol not only inhibits platelet activation but also increases vasodilation.1,2 In addition, it has been also shown to inhibit vascular smooth muscle cell proliferation.3 These properties of cilostazol may also improve peripheral blood flow. The mechanism of these effects is mediated through elevated cyclic adenosine monophosphate (AMP), brought about by inhibition of cyclic nucleotide phosphodiesterase (PDE3) activity.4 In this chapter, the pharmacological properties, as well as the clinical efficacy of cilostazol, are briefly discussed.

PDE3 Inhibition by Cilostazol Ameliorated Behavioral and Biochemical Deficits in Prenatal Alcohol Induced Experimental ADHD

2021 ◽  
Vol 17 ◽  
Author(s):  
Niti Sharma ◽  
Bhupesh Sharma ◽  
Neerupma Dhiman ◽  
Lalit K. Golani
Keyword(s):  
Oxidative Stress ◽  
Transcription Factor ◽  
Ethyl Alcohol ◽  
Neuronal Survival ◽  
Brain Inflammation ◽  
Protein Markers ◽  
Tnf Α ◽  
Brain Oxidative Stress ◽  
Prenatal Alcohol ◽  
Pde3 Inhibitor

Background: Attention deficit hyperactivity disorder (ADHD) is a neurodevelopmental disorder with complex aetiology and phenotypes. Maternal consumption of alcohol is known to produce deleterious effects in the progeny, generating ADHD related phenotypes. Phosphodiesterase-3 (PDE3) has been shown to provide benefits in various brain conditions. Objective: To investigate the role of a selective PDE3 inhibitor, effects of cilostazol administration on core phenotypes of prenatal alcohol exposure (PAE) model of ADHD were assessed. Methods: PAE was established by exposing animals to 6/4 g.kg-1 (weekdays/weekends) ethyl alcohol from gestational day 8-20 and cilostazol (30/60 mg.kg-1 p.o.) was administered to the offspring (PND21-48) of females exposed to ethyl alcohol. To identify probable mechanisms involved, the effects on protein markers of neuronal function such as, neuronal survival-BDNF, neuronal transcription factor-pCREB, brain inflammation (IL-6, IL-10 and TNF-α) and brain oxidative stress (TBARS and GSH) were studied in frontal cortex, cerebellum, and striatum. Also, effects on behaviour such as hyperactivity, inattention and anxiety were assessed. Result: PAE induced hyper-locomotion, inattention, and anxiety in tested animals. Administration of cilostazol to PAE group of animals resulted in amelioration of behavioural deficits. Also, cilostazol resulted in a significant increase in the levels of BDNF, pCREB, IL-10 and GSH along with significant decrease in TNF-α, IL-6 and TBARS in different brain areas of PAE group. Conclusion: Cilostazol, a selective PDE3 inhibitor rectified behavioural phenotypes associated with ADHD, possibly by altering protein markers associated with neuronal survival, neuronal transcription factor, brain inflammation, and brain oxidative stress.

scholarly journals Reduced Airway Hyperresponsiveness by Phosphodiesterase 3 and 4 Inhibitors in Guinea-Pigs

1999 ◽  
Vol 8 (3) ◽  
pp. 153-157 ◽  
Author(s):  
Nöella Germain ◽  
Elisabeth Boichot ◽  
Jean-Michel Planquois ◽  
Vincent Lagente
Keyword(s):  
Dose Response ◽  
Guinea Pigs ◽  
Airway Hyperresponsiveness ◽  
Response Curve ◽  
Pde5 Inhibitor ◽  
Pde4 Inhibitor ◽  
Potential Utility ◽  
Phosphodiesterase 3 ◽  
Pde Inhibitors ◽  
Pde3 Inhibitor

The aim of the present study was to compare the effects of selective phosphodiesterase (PDE) 3, 4 and 5 inhibitors on antigen-induced airway hyperresponsiveness in sensitized guinea-pigs. When the sensitized guinea-pigs were orally pre-treated with the selective PDE4 inhibitor, Ro 20-1724 (30 mg/kg), and studied 48 h after OA, a significant reduction (p<0.01) of the leftward shift of the dose-response curve to ACh was noted, whereas it was ineffective at the lower dose (10 mg/kg). Administration of the selective PDE3 inhibitor, milrinone (30 mg/kg) also elicited a significant reduction (p<0.01) of the airway hyperresponsiveness, whereas the PDE5 inhibitor zaprinast (30 mg/kg) was ineffective. These results show that both PDE3 and PDE4 inhibitors are able to inhibit the antigen-induced airway hyperresponsiveness in sensitized guinea-pigs and support the potential utility of selective PDE inhibitors in the treatment of asthma.

The effect of cilostazol, a phosphodiesterase 3 (PDE3) inhibitor, on human hair growth with the dual promoting mechanisms

2018 ◽  
Vol 91 (1) ◽  
pp. 60-68 ◽  
Author(s):  
Hye-In Choi ◽  
Dong Young Kim ◽  
Soon-Jin Choi ◽  
Chang-Yup Shin ◽  
Sungjoo Tommy Hwang ◽  
...  
Keyword(s):  
Human Hair ◽  
Hair Growth ◽  
Phosphodiesterase 3 ◽  
Pde3 Inhibitor

scholarly journals Effects of PDE3 Inhibitor Olprinone on the Respiratory Parameters, Inflammation, and Apoptosis in an Experimental Model of Acute Respiratory Distress Syndrome

2020 ◽  
Vol 21 (9) ◽  
pp. 3382
Author(s):  
Petra Kosutova ◽  
Pavol Mikolka ◽  
Sona Balentova ◽  
Marian Adamkov ◽  
Andrea Calkovska ◽  
...  
Keyword(s):  
Acute Respiratory Distress Syndrome ◽  
Respiratory Distress Syndrome ◽  
Respiratory Distress ◽  
Distress Syndrome ◽  
Arterial Oxygen Saturation ◽  
Oxygenation Index ◽  
Arterial Oxygen ◽  
Arterial Blood ◽  
Respiratory Parameters ◽  
Pde3 Inhibitor

This study aimed to investigate whether a selective phosphodiesterase-3 (PDE3) inhibitor olprinone can positively influence the inflammation, apoptosis, and respiratory parameters in animals with acute respiratory distress syndrome (ARDS) model induced by repetitive saline lung lavage. Adult rabbits were divided into 3 groups: ARDS without therapy (ARDS), ARDS treated with olprinone i.v. (1 mg/kg; ARDS/PDE3), and healthy ventilated controls (Control), and were oxygen-ventilated for the following 4 h. Dynamic lung–thorax compliance (Cdyn), mean airway pressure (MAP), arterial oxygen saturation (SaO2), alveolar-arterial gradient (AAG), ratio between partial pressure of oxygen in arterial blood to a fraction of inspired oxygen (PaO2/FiO2), oxygenation index (OI), and ventilation efficiency index (VEI) were evaluated every hour. Post mortem, inflammatory and oxidative markers (interleukin (IL)-6, IL-1β, a receptor for advanced glycation end products (RAGE), IL-10, total antioxidant capacity (TAC), 3-nitrotyrosine (3NT), and malondialdehyde (MDA) and apoptosis (apoptotic index and caspase-3) were assessed in the lung tissue. Treatment with olprinone reduced the release of inflammatory mediators and markers of oxidative damage decreased apoptosis of epithelial cells and improved respiratory parameters. The results indicate a future potential of PDE3 inhibitors also in the therapy of ARDS.

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