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Journal articles on the topic 'PDE-5 inhibitors'

Author: Grafiati

Published: 5 June 2025

Last updated: 2 August 2025

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1

Sarfati, Marika, Véronique Mateo, Sylvie Baudet, et al. "Sildenafil and vardenafil, types 5 and 6 phosphodiesterase inhibitors, induce caspase-dependent apoptosis of B-chronic lymphocytic leukemia cells." Blood 101, no. 1 (2003): 265–69. http://dx.doi.org/10.1182/blood-2002-01-0075.

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Abstract Type 4 phosphodiesterase (PDE4) inhibitors reportedly induce apoptosis in chronic lymphocytic leukemia (CLL) cells. Following clinical improvement of one previously untreated CLL patient with sildenafil therapy, we evaluated the in vitro induction of apoptosis in CLL cells by 4 PDE5/6 inhibitors, including sildenafil, vardenafil, zaprinast, and methoxyquinazoline (MQZ). After 24 hours of culture, the various PDE inhibitors differed in their ability to induce apoptosis, with zaprinast displaying no killing effect. Normal B cells isolated from control donors were totally resistant to PD

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2

Germain, Nöella, Elisabeth Boichot, Jean-Michel Planquois, and Vincent Lagente. "Reduced Airway Hyperresponsiveness by Phosphodiesterase 3 and 4 Inhibitors in Guinea-Pigs." Mediators of Inflammation 8, no. 3 (1999): 153–57. http://dx.doi.org/10.1080/09629359990487.

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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&l

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3

Ivey, F. Douglas, Lili Wang, Didem Demirbas, Christina Allain, and Charles S. Hoffman. "Development of a Fission Yeast-Based High-Throughput Screen to Identify Chemical Regulators of cAMP Phosphodiesterases." Journal of Biomolecular Screening 13, no. 1 (2007): 62–71. http://dx.doi.org/10.1177/1087057107312127.

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Cyclic nucleotide phosphodiesterases (PDEs) comprise a superfamily of enzymes that serve as drug targets in many human diseases. There is a continuing need to identify high-specificity inhibitors that affect individual PDE families or even subtypes within a single family. The authors describe a fission yeast-based high-throughput screen to detect inhibitors of heterologously expressed adenosine 3′,5′-cyclic monophosphate (cAMP) PDEs. The utility of this system is demonstrated by the construction and characterization of strains that express mammalian PDE2A, PDE4A, PDE4B, and PDE8A and respond a

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4

Favot, Laure, Thérèse Keravis, Vincent Holl, Alain Bec, and Claire Lugnier. "VEGF-induced HUVEC migration and proliferation are decreased by PDE2 and PDE4 inhibitors." Thrombosis and Haemostasis 90, no. 08 (2003): 334–43. http://dx.doi.org/10.1160/th03-02-0084.

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SummaryMigration and proliferation of endothelial cells in response to VEGF play an important role in angiogenesis associated to pathologies such as atherosclerosis, diabetes and tumor development. Elevation of cAMP in endothelial cells has been shown to inhibit growth factor-induced proliferation. Our hypothesis was that inactivation of cAMP-specific phosphodiesterases (PDEs) would inhibit angiogenesis. The purpose of this study was to evaluate the effect of PDE inhibitors on in vitro and in vivo angiogenesis, using human umbilical vein endothelial cell (HUVEC) and chick chorioallantoic membr

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Wójcik-Pszczoła, Katarzyna, Grażyna Chłoń-Rzepa, Agnieszka Jankowska та ін. "A Novel, Pan-PDE Inhibitor Exerts Anti-Fibrotic Effects in Human Lung Fibroblasts via Inhibition of TGF-β Signaling and Activation of cAMP/PKA Signaling". International Journal of Molecular Sciences 21, № 11 (2020): 4008. http://dx.doi.org/10.3390/ijms21114008.

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Phosphodiesterase (PDE) inhibitors are currently a widespread and extensively studied group of anti-inflammatory and anti-fibrotic compounds which may find use in the treatment of numerous lung diseases, including asthma and chronic obstructive pulmonary disease. Several PDE inhibitors are currently in clinical development, and some of them, e.g., roflumilast, are already recommended for clinical use. Due to numerous reports indicating that elevated intracellular cAMP levels may contribute to the alleviation of inflammation and airway fibrosis, new and effective PDE inhibitors are constantly b

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6

Blanco-Rivero, Javier, and Fabiano E. Xavier. "Therapeutic Potential of Phosphodiesterase Inhibitors for Endothelial Dysfunction- Related Diseases." Current Pharmaceutical Design 26, no. 30 (2020): 3633–51. http://dx.doi.org/10.2174/1381612826666200403172736.

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Cardiovascular diseases (CVD) are considered a major health problem worldwide, being the main cause of mortality in developing and developed countries. Endothelial dysfunction, characterized by a decline in nitric oxide production and/or bioavailability, increased oxidative stress, decreased prostacyclin levels, and a reduction of endothelium-derived hyperpolarizing factor is considered an important prognostic indicator of various CVD. Changes in cyclic nucleotides production and/ or signalling, such as guanosine 3&#039;, 5&#039;-monophosphate (cGMP) and adenosine 3&#039;, 5&#0

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7

Doumas, Michael, Antonios Lazaridis, Niki Katsiki, and Vasilios Athyros. "PDE-5 Inhibitors: Clinical Points." Current Drug Targets 16, no. 5 (2015): 420–26. http://dx.doi.org/10.2174/1389450115666141111111301.

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8

Efremov, E. A. Efremov, E. V. Kasatonova Kasatonova, Ya I. Mel’nik Mel’nik, and A. A. Nikushina Nikushina. "PDE-5 inhibitors: patients’ preferences." Urologiia 3_2017 (July 18, 2017): 120–26. http://dx.doi.org/10.18565/urol.2017.3.120-126.

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9

Kumar, Shivendra, Dr Mayank Kulshreshtha, and Sunam Saha. "Contribution of Phosphodiesterase-5 (PDE5) Inhibitors in the Various Diseases." International Journal of Science and Healthcare Research 7, no. 4 (2022): 164–72. http://dx.doi.org/10.52403/ijshr.20221023.

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The PDE-5 inhibitors, i.e., phosphodiesterase-5 inhibitors like sildenafil, vardenafil, and tadalafil, are the most used in premature erectile dysfunction. Many literature reviews suggest that these classes of drugs are commonly used in erectile dysfunction. Many of these reviews suggest that these inhibitors (PDE-5) are used in many other diseases apart from erectile dysfunction. So, in this review, we find the main mechanism of action of PDE-5 inhibitors in different disease conditions. These inhibitors have a major role in different diseases like erectile dysfunction, memory enhancement, ca

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10

McCullough, Andrew R. "An Update on the PDE-5 Inhibitors (PDE-5i)." Journal of Andrology 24, S6 (2003): S52—S58. http://dx.doi.org/10.1002/j.1939-4640.2003.tb02747.x.

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11

Manna, Sayan, Mingyang Liu Gray, Vivian F. Kaul, and George Wanna. "Phosphodiesterase-5 (PDE-5) Inhibitors and Ototoxicity." Otology & Neurotology 40, no. 3 (2019): 276–83. http://dx.doi.org/10.1097/mao.0000000000002148.

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12

Murthy, Karnam S., Huiping Zhou, and Gabriel M. Makhlouf. "PKA-dependent activation of PDE3A and PDE4 and inhibition of adenylyl cyclase V/VI in smooth muscle." American Journal of Physiology-Cell Physiology 282, no. 3 (2002): C508—C517. http://dx.doi.org/10.1152/ajpcell.00373.2001.

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Regulation of adenylyl cyclase type V/VI and cAMP-specific, cGMP-inhibited phosphodiesterase (PDE) 3 and cAMP-specific PDE4 by cAMP-dependent protein kinase (PKA) and cGMP-dependent protein kinase (PKG) was examined in gastric smooth muscle cells. Expression of PDE3A but not PDE3B was demonstrated by RT-PCR and Western blot. Basal PDE3 and PDE4 activities were present in a ratio of 2:1. Forskolin, isoproterenol, and the PKA activator 5,6-dichloro-1-β-d-ribofuranosyl benzimidazole 3′,5′-cyclic monophosphate, SP-isomer, stimulated PDE3A phosphorylation and both PDE3A and PDE4 activities. Phospho

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13

Teng, Bunyan, Daniel N. Darlington, and Andrew P. Cap. "Adenosine Regulation of cAMP through Phosphodiesterases." Blood 132, Supplement 1 (2018): 2424. http://dx.doi.org/10.1182/blood-2018-99-114929.

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Abstract Introduction: Adenosine, an autacoid and metabolite of ATP, has been known to have anti-platelet properties. Of the 4 adenosine receptors (ARs), only A2A AR have been implicated in adenosines anti-platelet properties in human. A2A AR is a G-Protein Coupled Receptors associated with a stimulatory G-Protein (Gs) that can activate adenylyl cyclase (AC) and increase intracellular cAMP. An elevation of cAMP has been shown to inhibit platelet aggregation to natural stimuli. Regulation of intracellular cAMP is balanced between synthesis by adenylate cyclase and degradation by phosphdiesteras

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14

Hood, Stuart, and Mike Kirby. "Review: PDE-5 inhibitors — a summary." British Journal of Diabetes & Vascular Disease 4, no. 6 (2004): 383–86. http://dx.doi.org/10.1177/14746514040040060401.

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15

Pomara, G., G. Morelli, F. Menchini-Fabris, et al. "Epistaxis after PDE-5 inhibitors misuse." International Journal of Impotence Research 18, no. 2 (2005): 213–14. http://dx.doi.org/10.1038/sj.ijir.3901383.

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16

LEVINE, STEPHEN B. "The PDE-5 Inhibitors and Psychiatry." Journal of Psychiatric Practice 12, no. 1 (2006): 46–49. http://dx.doi.org/10.1097/00131746-200601000-00007.

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17

Kirby, M. G. "PDE-5 inhibitors: spoilt for choice." International Journal of Clinical Practice 60, no. 8 (2006): 893–94. http://dx.doi.org/10.1111/j.1742-1241.2006.01050.x.

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18

Edwards, Angela F., and Raymond C. Roy. "Preoperative administration of PDE-5 Inhibitors." Journal of Clinical Anesthesia 21, no. 2 (2009): 149. http://dx.doi.org/10.1016/j.jclinane.2009.01.001.

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19

Malykhina, Anna I., Svetlana S. Efimova, and Olga S. Ostroumova. "Membrane-Mediated Action of Phosphodiesterase 5 Inhibitors." Pharmaceutics 17, no. 5 (2025): 563. https://doi.org/10.3390/pharmaceutics17050563.

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Background/Objectives: Phosphodiesterase 5 (PDE5) inhibitors, sildenafil, vardenafil, and tadalafil, activate the cyclic guanosine monophosphate pathway resulting in vascular smooth muscle relaxation. They have been tested for a broad variety of conditions from cancer to Alzheimer’s disease with a positive impact. The known mechanism of action of these drugs could not explain such a plethora of effects. We studied the influence of PDE5 inhibitors on lipid bilayers as a possible application point of their action. Methods: To monitor the membrane changes induced by PDE5 inhibitors, the different

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20

Stamatiou, Konstantinos, Gianpaolo Perletti, Vittorio Magri, and Alberto Trinchieri. "The Role of 5-Phosphodiesterase Inhibitors (PDE-5I) in Current Benign Prostatic Hyperplasia Treatment: A Narrative Review." Medicina 60, no. 11 (2024): 1736. http://dx.doi.org/10.3390/medicina60111736.

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Introduction: 5-phosphodiesterase inhibitors (PDE-5I) have been investigated as a treatment for urinary dysfunction for almost a decade. The general perception is that they play a significant role in managing lower urinary tract symptoms (LUTS), particularly those associated with benign prostatic hyperplasia (BPH). However, the specific biochemical processes by which PDE-5I repairs urinary function are still poorly understood and there is little instrumental evidence of significant improvement in urinary symptoms. Therefore, we explore the role of 5-phosphodiesterase inhibitors (PDE-5I) as com

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21

Li, Yuze, Zhe Wang, Shengyao Ma, Xiaowen Tang, and Hanting Zhang. "Chemical Space Exploration and Machine Learning-Based Screening of PDE7A Inhibitors." Pharmaceuticals 18, no. 4 (2025): 444. https://doi.org/10.3390/ph18040444.

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Background/Objectives: Phosphodiesterase 7 (PDE7), a member of the PDE superfamily, selectively catalyzes the hydrolysis of cyclic adenosine 3′,5′-monophosphate (cAMP), thereby regulating the intracellular levels of this second messenger and influencing various physiological functions and processes. There are two subtypes of PDE7, PDE7A and PDE7B, which are encoded by distinct genes. PDE7 inhibitors have been shown to exert therapeutic effects on neurological and respiratory diseases. However, FDA-approved drugs based on the PDE7A inhibitor are still absent, highlighting the need for novel com

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22

Kamaruzaman, Nur Azzalia, Mazlin Mohideen, Yin-Hui Leong, Azaharudin Awang Ahmad, and Norjuliana Mohd Noor. "Determination of Phosphodiesterase Type 5 Enzyme (PDE-5) Inhibitors and Analogues as Adulterants in Selected Herbal Products using Gas Chromatography–Electron Impact-Mass Spectrometer (GC-EI-MS)." Baghdad Science Journal 17, no. 4 (2020): 1190. http://dx.doi.org/10.21123/bsj.2020.17.4.1190.

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Sildenafil, tadalafil, and vardenafil are phosphodiesterase type 5 enzyme (PDE-5) inhibitors used for the treatment of male erectile dysfunction. This present study aims to investigate 55 herbal products indicated for men’s sexual health from the Malaysian market for adulteration of PDE-5 inhibitors and analogues. The screening and identification of 20 PDE-5 inhibitors and analogues in herbal products of various forms (powder, capsules, tablets, and pastels) were conducted using gas chromatography–electron impact-mass spectrometer (GC-EI-MS). The analysis has shown that 19 herbal products were

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23

Rickles, Richard J., Laura Pierce, Thomas Giordano, et al. "Adenosine A2A Receptor Agonism and PDE Inhibition: A Synergistic Multi-Target Mechanism Discovered through Systematic Combination Screening in Multiple Myeloma." Blood 112, no. 11 (2008): 847. http://dx.doi.org/10.1182/blood.v112.11.847.847.

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Abstract Using a combination high throughput screening technology, we have discovered an unexpected synergistic interaction between adenosine A2A receptor (A2A) agonism and phosphodiesterase (PDE) inhibition that displays substantial activity in preclinical Multiple Myeloma (MM) models. High throughput combination screening allows the systematic testing of combinations of approved drugs and other biologically active molecules in cell based assays of tumor cell proliferation and viability. In this approach we generate a dose matrix for each chemical combination, capturing the combined activity

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24

Idres, Sarah, Germain Perrin, Valérie Domergue, et al. "Contribution of BKCa channels to vascular tone regulation by PDE3 and PDE4 is lost in heart failure." Cardiovascular Research 115, no. 1 (2018): 130–44. http://dx.doi.org/10.1093/cvr/cvy161.

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Abstract Aims Regulation of vascular tone by 3′,5′-cyclic adenosine monophosphate (cAMP) involves many effectors including the large conductance, Ca2+-activated, K+ (BKCa) channels. In arteries, cAMP is mainly hydrolyzed by type 3 and 4 phosphodiesterases (PDE3, PDE4). Here, we examined the specific contribution of BKCa channels to tone regulation by these PDEs in rat coronary arteries, and how this is altered in heart failure (HF). Methods and results Concomitant application of PDE3 (cilostamide) and PDE4 (Ro-20-1724) inhibitors increased BKCa unitary channel activity in isolated myocytes fro

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25

Wang, Hua. "Development of a Robust Method for Screening PDE-5 Inhibitor Additives in Dietary Supplements Using UPLC-MS/MS." Asian Journal of Applied Chemistry Research 14, no. 4 (2023): 23–33. http://dx.doi.org/10.9734/ajacr/2023/v14i4274.

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A novel ultra-performance liquid chromatography coupled to tandem mass spectrometry (UPLC-MS/MS) method was developed to detect the illegal additive of phosphodiesterase type 5 (PDE-5) inhibitors in dietary supplements. With the optimized chromatographic program, vardenafil, sildenafil, and tadalafil were separated within 5 minutes. The MS1, MS2, and retention time of PDE-5 inhibitors were acquired simultaneously within the information dependent acquisition mass spectrometry mode. Quantification was achieved via the quantity ion current chromatogram that was extracted from the total ion curren

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Brousil, Philip, Majid Shabbir, E. Zacharakis, and Arun Sahai. "PDE-5 Inhibitors for BPH-Associated LUTS." Current Drug Targets 16, no. 11 (2015): 1180–86. http://dx.doi.org/10.2174/138945011611151013164756.

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MACNEIL, JANE SALODOF. "PDE-5 Inhibitors May Relieve Benign Prostatitis." Clinical Endocrinology News 1, no. 6 (2006): 28. http://dx.doi.org/10.1016/s1558-0164(06)70209-7.

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28

Luo, Weihao, Runduo Liu, Xinlin Cai, Qian Zhou, and Chen Zhang. "Molecular Dynamics-Assisted Discovery of Novel Phosphodiesterase-5 Inhibitors Targeting a Unique Allosteric Pocket." Molecules 30, no. 3 (2025): 588. https://doi.org/10.3390/molecules30030588.

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Phosphodiesterase-5 (PDE5) is a potent therapeutic target for the treatment of male erectile dysfunction and pulmonary arterial hypertension with several drugs available on the market. However, most of the reported PDE5 inhibitors lack specificity over PDE6, a holoenzyme in eleven PDE families, which may cause various adverse effects. Targeting a unique allosteric pocket has proved to be an effective approach to designing selective PDE5 inhibitors. In the present study, an integrated virtual screening procedure consisting of pharmacophore modeling screening, molecular docking, molecular dynami

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29

Pernkopf, D. G., G. Untergasser, P. Berger, and E. Plas. "Phosphodiesterase (PDE) inhibitors reduce in vitro proliferation of prostate primary cells but do not interfere with growth of prostate carcinoma cell lines." Journal of Clinical Oncology 24, no. 18_suppl (2006): 14604. http://dx.doi.org/10.1200/jco.2006.24.18_suppl.14604.

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14604 Background: PDE 5 is highly expressed in cavernosal and prostatic tissue. The mechanism of PDE-5 inhibitors on cavernosal tissue is well established but the effects of PDE-5 inhibitors on prostatic cells are unknown. The aim of this study was to analyze in vitro effects of PDE-5 inhibitors on prostate primary cells, fibroblasts (PrSC), basal epithelial cells (PrEC) and prostate cancer cell lines. Methods: Cultivated PrEC and PrSC, immortalized BPH cells (BPH 1), androgen dependent (LNCaP) and androgen independent (PC3) prostate carcinoma cell lines were exposed to increasing concentratio

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Rabe, K. F., H. Tenor, G. Dent, C. Schudt, S. Liebig, and H. Magnussen. "Phosphodiesterase isozymes modulating inherent tone in human airways: identification and characterization." American Journal of Physiology-Lung Cellular and Molecular Physiology 264, no. 5 (1993): L458—L464. http://dx.doi.org/10.1152/ajplung.1993.264.5.l458.

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The effects of the nonselective phosphodiesterase (PDE)-inhibitor 3-isobutyl-1-methylxanthine (IBMX) and the selective PDE inhibitors SKF 94120 (type III), rolipram (type IV), zardaverine (type III/IV), and zaprinast (type V) on inherent tone in human airways were investigated. Substantial relaxation was achieved by IBMX [concentration eliciting 50% of maximum response (EC50): 2.9 microM, n = 14] and SKF 94120 (EC50: 1.4 microM, n = 15); rolipram and zaprinast were almost ineffective. Zardaverine (EC50: 0.31 microM, n = 8), and the combination of SKF 94120 and rolipram (1 microM; EC50: 0.41 mi

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31

Lugnier, Claire. "The Complexity and Multiplicity of the Specific cAMP Phosphodiesterase Family: PDE4, Open New Adapted Therapeutic Approaches." International Journal of Molecular Sciences 23, no. 18 (2022): 10616. http://dx.doi.org/10.3390/ijms231810616.

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Cyclic nucleotides (cAMP, cGMP) play a major role in normal and pathologic signaling. Beyond receptors, cyclic nucleotide phosphodiesterases; (PDEs) rapidly convert the cyclic nucleotide in its respective 5′-nucleotide to control intracellular cAMP and/or cGMP levels to maintain a normal physiological state. However, in many pathologies, dysregulations of various PDEs (PDE1-PDE11) contribute mainly to organs and tissue failures related to uncontrolled phosphorylation cascade. Among these, PDE4 represents the greatest family, since it is constituted by 4 genes with multiple variants differently

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Leal, Gabriel Vieira, and André Tomaz Terra Júnior. "Inibidores da enzima Fosfodiesterase-5 (PDE-5)." Revista Científica FAEMA 8, no. 1 (2017): 124. http://dx.doi.org/10.31072/rcf.v8i1.435.

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O presente trabalho possui o objetivo de apresentar de forma clara, concisa e sistemática, uma revisão de literatura de natureza qualitativa sobre o uso recreativo de inibidores da enzima fosfodiesterase-5 (PDE-5). Metodologicamente, realizou-se uma pesquisa bibliográfica visando à obtenção de dados para a pesquisa, sendo utilizados materiais já publicados, como, livros, artigos científicos, teses e dissertações nas áreas de fisiopatologia da disfunção erétil e farmacologia, além do uso desses medicamentos pelos jovens. A princípio, compreendeu-se a fisiopatologia de quem realmente sofre com a

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Haynes, J., P. A. Kithas, A. E. Taylor, and S. J. Strada. "Selective inhibition of cGMP-inhibitable cAMP phosphodiesterase decreases pulmonary vasoreactivity." American Journal of Physiology-Heart and Circulatory Physiology 261, no. 2 (1991): H487—H492. http://dx.doi.org/10.1152/ajpheart.1991.261.2.h487.

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Guanosine 3',5'-cyclic monophosphate (cGMP) and adenosine 3',5'-cyclic monophosphate (cAMP) are mediators of smooth muscle relaxation. In this study, selective inhibitors of phosphodiesterase (PDE) isozymes were used to assess the role of cyclic nucleotide hydrolysis in angiotensin II (ANG II) and hypoxic pulmonary vasoconstriction. In isolated rat lungs, the hypoxic pressor response (HPR) was induced with a 95% N2-5% CO2 gas mixture. When administered during the plateau of the HPR, trequinsin (nonselective PDE inhibitor) and indolidan (cGMP-inhibitable cAMP PDE inhibitor) significantly (P = 0

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Rohan, Magdum* Pratik Magdum Babaso Udugade. "Repuroising Of Fda Approved Thiothixine a Typical Antipychotic Agent as A Pde-5 Inhbitor For Erectile Dysfunction." International Journal of Scientific Research and Technology 2, no. 4 (2025): 348–56. https://doi.org/10.5281/zenodo.15236366.

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Erectile dysfunction (ED) is a common disorder that affects men's physical and psychological health. The treatment of ED has evolved with the approval of new PDE-5 inhibitors such as sildenafil, which causes an erection through inhibition of the PDE-5 enzyme that regulates and maintains blood flow in the penis. Although PDE-5 inhibitors have shown efficacy in treating ED, approximately 30% of patients will not have a satisfactory response to these medications. In these patients, alternatives should be explored. Thiothixene is a first-generation antipsychotic primarily used to treat schizophren

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MacNEIL, JANE SALODOF. "Use PDE-5 Inhibitors for Antidepressant Side Effects." Clinical Psychiatry News 38, no. 3 (2010): 11. http://dx.doi.org/10.1016/s0270-6644(10)70126-0.

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Masson, Puneet, Sarah M. Lambert, Melissa Brown, and Ridwan Shabsigh. "PDE-5 Inhibitors: Current Status and Future Trends." Urologic Clinics of North America 32, no. 4 (2005): 511–25. http://dx.doi.org/10.1016/j.ucl.2005.08.012.

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MACNEIL, JANE SALODOF. "PDE-5 Inhibitors May Relieve Male Urinary Symptoms." Internal Medicine News 39, no. 9 (2006): 1–2. http://dx.doi.org/10.1016/s1097-8690(06)73403-5.

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Shtarkshall, R. "Beyond PDE-5 Inhibitors: Sexuality in Primary Healthcare." Sexologies 17 (April 2008): S49. http://dx.doi.org/10.1016/s1158-1360(08)72650-1.

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Shabsigh, Ridwan. "Therapy of ED: PDE-5 Inhibitors." Endocrine 23, no. 2-3 (2004): 135–42. http://dx.doi.org/10.1385/endo:23:2-3:135.

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Ниткин, Д. М. "Phosphodiesterase Type 5 Inhibitors in the Treatment of Lower Urinary Tract Symptoms in Men." Репродуктивное здоровье. Восточная Европа 13, no. 4 (2023): 387–91. http://dx.doi.org/10.34883/pi.2023.13.4.009.

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Ингибиторы фосфодиэстеразы 5-го типа (ФДЭ-5) значительно улучшают эректильную функцию у мужчин и являются перспективной группой лекарственных средств для лечения пациентов с симптомами нижних мочевых путей (СНМП). В статье представлен обзор применения данной группы лекарственных средств в лечении симптомов нижних мочевых путей у мужчин с позиции доказательной медицины. Тадалафил является ингибитором ФДЭ-5 с доказанной эффективностью применения у пациентов с СНМП с эректильной дисфункцией или без эректильной дисфункции. Тадалафил имеет высокую биодоступность, оптимальную продолжительность дейст

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Marais, André. "The pharmacological management of erectile dysfunction – Update 2016." South African Family Practice 58, no. 4 (2016): 10–14. http://dx.doi.org/10.4102/safp.v58i4.4521.

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Erectile dysfunction (ED) is a trivial condition with a prevailing incidence worldwide. Phosphodiesterase-5 inhibitors (PDE-5) have revolutionised the treatment of ED and are regarded as one of the most successful drug groups in modern medicine. Generally PDE-5 inhibitors are well tolerated and the incidence of side-effects is low, however a small percentage of individuals experience headache, flushing and abdominal discomfort, resulting in discontinuation of therapy. This has led to the development of second generation PDE-5 inhibitors, displaying more selectivity for the PDE-5 enzyme thereby

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Impens, Ann J., Kristine Phillips, and Elena Schiopu. "PDE-5 Inhibitors in Scleroderma Raynaud Phenomenon and Digital Ulcers: Current Status of Clinical Trials." International Journal of Rheumatology 2011 (2011): 1–5. http://dx.doi.org/10.1155/2011/392542.

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Systemic sclerosis- (SSc-) related vasculopathy, as manifested by Raynaud's Phenomenon (RP) and digital ulcers (DUs), is associated with significant impairment of the quality of life and morbidity. The current vasoactive approach for SSc-RP, although employing vasodilators, is entirely off-label. PDE-5 inhibitors improve peripheral circulation, are well tolerated, and are widely used for various forms of constrictive vasculopathies. This class of medications has become one of the first lines of treatment of SSc-RP and SSc-DUs among rheumatologists that routinely treat SSc patients. Due to the

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Kim, Doo Ho, and Adam Lerner. "Type 4 Cyclic Adenosine Monophosphate Phosphodiesterase as a Therapeutic Target in Chronic Lymphocytic Leukemia." Blood 92, no. 7 (1998): 2484–94. http://dx.doi.org/10.1182/blood.v92.7.2484.

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Abstract Theophylline, a drug known to inhibit several classes of adenosine 3′5′ cyclic monophosphate (cAMP) phosphodiesterases (PDEs), induces apoptosis in chronic lymphocytic leukemia (CLL) cells. Because the PDE target for theophylline in CLL remains unknown, we examined the ability of isoform-specific PDE inhibitors to increase cAMP levels and induce apoptosis in primary CLL cells. Reverse transcriptase-polymerase chain reaction of purified CLL cDNA amplified transcripts for PDE1B, 4A and 4B. The type 4 PDE inhibitor rolipram but not the type 1 inhibitor vinpocetine increased CLL cAMP leve

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Kim, Doo Ho, and Adam Lerner. "Type 4 Cyclic Adenosine Monophosphate Phosphodiesterase as a Therapeutic Target in Chronic Lymphocytic Leukemia." Blood 92, no. 7 (1998): 2484–94. http://dx.doi.org/10.1182/blood.v92.7.2484.2484_2484_2494.

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Theophylline, a drug known to inhibit several classes of adenosine 3′5′ cyclic monophosphate (cAMP) phosphodiesterases (PDEs), induces apoptosis in chronic lymphocytic leukemia (CLL) cells. Because the PDE target for theophylline in CLL remains unknown, we examined the ability of isoform-specific PDE inhibitors to increase cAMP levels and induce apoptosis in primary CLL cells. Reverse transcriptase-polymerase chain reaction of purified CLL cDNA amplified transcripts for PDE1B, 4A and 4B. The type 4 PDE inhibitor rolipram but not the type 1 inhibitor vinpocetine increased CLL cAMP levels. Rolip

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Gheorghiu, Oana Ramona Cătălina, Anne Marie Ciobanu, Claudia Maria Guțu, et al. "Determination of Phosphodiesterase Type-5 Inhibitors (PDE-5) in Dietary Supplements." Molecules 28, no. 10 (2023): 4116. http://dx.doi.org/10.3390/molecules28104116.

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This study proposed a high-performance thin-layer chromatography (HPTLC) screening method to detect phosphodiesterase 5 (PDE-5) inhibitors as possible adulterant agents in various dietary supplements. Chromatographic analysis was performed on silica gel 60F254 plates using a mixture of ethyl acetate:toluene:methanol:ammonia in a volume ratio of 50:30:20:0.5 as a mobile phase. The system provided compact spots and symmetrical peaks of sildenafil and tadalafil with retardation factor values of 0.55 and 0.90, respectively. The analysis of products purchased from the internet or specialized stores

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Hoang Thi, Lan Anh, Oanh Nguyen Thi, Diu Dinh Thi, et al. "Simultaneous determination of acetyl vardenafil, homosildenafil, hydroxy acetildenafil and mirodenafil by CE-C4D." Heavy metals and arsenic concentrations in water, agricultural soil, and rice in Ngan Son district, Bac Kan province, Vietnam 5, no. 3 (2022): 291–302. http://dx.doi.org/10.47866/2615-9252/vjfc.3942.

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Dietary supplements are currently popular because of their natural origin, especially male enhancement products. However, some of these products have been found to contain erectile dysfunction drugs that inhibit the enzyme phosphodiesterase-5 (PDE-5), leading to adverse effects on human health. In this study, capillary electrophoresis with capacitively coupled contactless conductivity detection (CE-C4D) was used to determine four PDE-5 inhibitors (including acetyl vardenafil, homosildenafil, hydroxy acetildenafil and mirodenafil) in dietary supplement samples. The optimum analytical conditions

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Firdosh, Nikhat, Bindu Singh Yadav, Shaaista Rahman, and Hansraj Kumar. "PDE-5 Restore Cognitive and Metabolic Function in Patients with Alzheimer’s Disease (AD)." International Journal of Pharmaceutical Sciences and Medicine 9, no. 7 (2024): 11–23. http://dx.doi.org/10.47760/ijpsm.2024.v09i07.002.

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Given that life expectancy is increasing and the human population is constantly aging, the quest for new, effective diagnostic methods and therapies in the context of cognitive decline is wide open. The present review was based on the pde-5 restore cognitive and metabolic function in patients with Alzheimer’s disease (AD). PDE5 inhibitors, often known as PDE5i, are frequently given medications for the treatment of pulmonary arterial hypertension (PAH) and erectile dysfunction (ED). Their known mechanism in these disorders is to increase vasodilation that is dependent on nitric oxide by obstruc

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Rabe, K. F., H. Tenor, G. Dent, C. Schudt, M. Nakashima, and H. Magnussen. "Identification of PDE isozymes in human pulmonary artery and effect of selective PDE inhibitors." American Journal of Physiology-Lung Cellular and Molecular Physiology 266, no. 5 (1994): L536—L543. http://dx.doi.org/10.1152/ajplung.1994.266.5.l536.

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The effects of the nonselective phosphodiesterase (PDE) inhibitor 3-isobutyl-1-methylxanthine (IBMX) and the selective PDE inhibitors motapizone (type III), rolipram (type IV), zardaverine (type III/IV), and zaprinast (type V and I) on prostaglandin F2 alpha (PFG2 alpha)-induced tone in human pulmonary arteries was investigated. Relaxation was achieved by IBMX [concentration eliciting 50% of maximum response (EC50): 11.3 microM, n = 10], motapizone (EC50:3.0 microM, n = 7), zardaverine (EC50: 3.2 microM, n = 9), and zaprinast (EC50: 31.8 microM, n = 6), whereas rolipram was almost ineffective.

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Argyrousi, Elentina K., Pim RA Heckman, Britt TJ van Hagen, Hannah Muysers, Nick P. van Goethem, and Jos Prickaerts. "Pro-cognitive effect of upregulating cyclic guanosine monophosphate signalling during memory acquisition or early consolidation is mediated by increased AMPA receptor trafficking." Journal of Psychopharmacology 34, no. 1 (2019): 103–14. http://dx.doi.org/10.1177/0269881119885262.

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Background: Episodic memory consists of different mnemonic phases, including acquisition and early and late consolidation. Each of these phases is characterised by distinct molecular processes. Although both cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) are implicated in the acquisition phase, early consolidation only depends on cGMP, whereas late consolidation is mediated by cAMP. Accordingly, the cGMP-selective phosphodiesterase 5 (PDE5) inhibitor vardenafil or the cAMP-selective PDE4 inhibitor rolipram can improve memory acquisition or consolidation when ap

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Fournier, Valérie, Pierre Leclerc, Nathaly Cormier, and Janice L. Bailey. "Implication of Calmodulin‐Dependent Phosphodiesterase Type 1 During Bovine Sperm Capacitation." Journal of Andrology 24, no. 1 (2003): 104–12. http://dx.doi.org/10.1002/j.1939-4640.2003.tb02648.x.

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ABSTRACT: Phosphodiesterases (PDEs) are enzymes that degrade cyclic nucleotides. The calcium‐calmodulin dependent PDE type 1 (PDE 1) and the cyclic adenosine monophosphate (cAMP)‐specific PDE type 4 (PDE 4) have been implicated in sperm function. We tested the hypothesis that specific PDEs regulate capacitation of bovine sperm in a manner independent of those that mediate motility. Our objectives were to determine the effects of inhibiting PDE 1 and PDE 4 on capacitation and motility, and to compare these effects to those of heparin, which is necessary for capacitation of bull sperm in vitro.

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