Results 341 to 350 of about 2,888,163 (384)
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Journal of Medicinal Chemistry, 2014
We report the discovery of a series of imidazo[1,2-a]pyrazine derivatives as novel inhibitors of phosphodiesterase 10A (PDE10A). In a high-throughput screening campaign we identified the imidazopyrazine derivative 1, a PDE10A inhibitor with limited ...
J. Bartolomé-Nebreda +13 more
semanticscholar +1 more source
We report the discovery of a series of imidazo[1,2-a]pyrazine derivatives as novel inhibitors of phosphodiesterase 10A (PDE10A). In a high-throughput screening campaign we identified the imidazopyrazine derivative 1, a PDE10A inhibitor with limited ...
J. Bartolomé-Nebreda +13 more
semanticscholar +1 more source
Disaggregatory action of phosphodiesterase inhibitors
Pharmacological Research Communications, 1981Summary Papaverine and three hypotensive xanthines were shown to disaggregate platelet clumps in anaesthetized cats. The order of disaggregatory potency was: IMBX > papaverine > > aminophylline ≫ xantinol nicotinate. This effect was not associated with the release of prostacyclin. It is concluded that disaggregatory action of papaverine and xanthines
Ryszard J. Gryglewski +2 more
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The new inotropic phosphodiesterase inhibitors
Archives Internationales de Physiologie et de Biochimie, 1984Compounds with phosphodiesterase inhibitory activity stimulate myocardial contractility by increasing the intracellular cyclic AMP concentrations. They can also increase Ca2+ entry and inhibit Ca2+ sequestration by the sarcoplasmic reticulum. Xanthines produce bronchodilation with associated venous and arteriolar dilation. However, their use is limited
D El Allaf +2 more
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Phosphodiesterase-4 inhibitor therapy for lung diseases.
American Journal of Respiratory and Critical Care Medicine, 2013Phosphodiesterases (PDEs) are a superfamily of enzymes that catalyze the breakdown of cAMP and/or cyclic guanosine monophosphate (GMP) to their inactive form. PDE4 is the main selective cAMP-metabolizing enzyme in inflammatory and immune cells.
B. Beghé, K. Rabe, L. Fabbri
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Phosphodiesterase inhibitors in clinical urology
Expert Review of Clinical Pharmacology, 2013To date, benign diseases of the male and female lower urinary and genital tract, such as erectile dysfunction, bladder overactivity, lower urinary tract symptomatology secondary to benign prostatic hyperplasia and symptoms of female sexual dysfunction (including arousal and orgasmic disorders), can be therapeutically approached by influencing the ...
Markus A. Kuczyk +2 more
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Phosphodiesterase Inhibitors for Cognitive Enhancement
Current Pharmaceutical Design, 2005An effective treatment for age-related cognitive deficits remains an unmet medical need. Currently available drugs for the symptomatic treatment of Alzheimer's disease or other dementias have limited efficacy. This may be due to their action at only one of the many neurotransmitter systems involved in the complex mechanisms that underlie cognition.
Ashok Tehim +3 more
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Recent Advances in Cardiovascular Drug Discovery (Formerly Recent Patents on Cardiovascular Drug Discovery), 2009
Systemic vascular disease is the greatest cause of mortality in the western world. Treatment options have been preventative with medical therapy or curative with surgical bypass. Recently, there has been an increase in the use and popularity of minimally
S. Dindyal, C. Kyriakides
semanticscholar +1 more source
Systemic vascular disease is the greatest cause of mortality in the western world. Treatment options have been preventative with medical therapy or curative with surgical bypass. Recently, there has been an increase in the use and popularity of minimally
S. Dindyal, C. Kyriakides
semanticscholar +1 more source
The role of phosphodiesterase inhibitors in impotence
Expert Opinion on Investigational Drugs, 1997Penile erection is mediated by nitric oxide (NO) and its second messenger cyclic guanosine monophosphate (cGMP). The activity of cGMP is modulated by the enzyme phosphodiesterase (PDE). The most important physiological isoform of the enzyme in the penis is PDE5.
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Targeting cancer with phosphodiesterase inhibitors
Expert Opinion on Investigational Drugs, 2009For many cancers, there has been a shift from management with traditional, nonspecific cytotoxic chemotherapies to treatment with molecule-specific targeted therapies that are used either alone or in combination with traditional chemotherapy and radiation therapy.
Ralph T. Schermuly +6 more
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Phosphodiesterase Inhibitors: History of Pharmacology
2011The first pharmacological investigations of phosphodiesterase (PDE) inhibitors were developed with the clinical efficacies of drugs isolated from coffee, cacao and tea but only later their relevant ingredients were identified as xanthines that act as PDE.
Rolf Beume +3 more
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