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Imidazoquinazolinone based inhibitors of Phosphodiesterase 3

2012
Phosphodiesterases (PDE) catalyze the deactivation of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). Inhibiting a cell’s PDE increases the level of cAMP or cGMP in the cytosol, enhancing the cells response to stimuli. Selectively inhibiting a PDE subtype can cause a specific cell or tissue type to elicit a therapeutic ...
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The Activity of 2′,3′‐Cyclic Nucleotide 3′‐Phosphodiesterase in Rat Tissues

Journal of Neurochemistry, 1982
Abstract: The activity of the myelin‐associated enzyme 2′,3′‐cyclic nucleotide 3′‐phosphodiesterase (CNP) was measured in 14 rat tissues and in subcellular fractions of rat liver by a sensitive fluorometric method, using cyclic NADP as substrate. CNP activity in brain (339 μmol/h/mg protein) was fourfold that of the sciatic nerve.
Ingrid Raes   +7 more
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Holothurin: an activator of bovine brain 3′-5′ phosphodiesterase

European Journal of Pharmacology, 1990
The effect of marine toxin, holothurin A, on calmodulin(CaM)-dependent bovine brain 3'-5' phosphodiesterase (PDE) was studied. Holothurin stimulated CaM-depleted PDE in a concentration dependent manner and this interaction was independent of Ca2+ concentrations. Activation of PDE by holothurin was pH and incubation temperature dependent. Heat treatment
D. Desaiah, B.D. Mehrotra, J.S. Vig
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Quinazolines: Combined type 3 and 4 phosphodiesterase inhibitors

Bioorganic & Medicinal Chemistry Letters, 1998
AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Irene Donze   +5 more
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Dual expression and differential regulation of phosphodiesterase 3A and phosphodiesterase 3B in human vascular smooth muscle: implications for phosphodiesterase 3 inhibition in human cardiovascular tissues.

Molecular Pharmacology, 2000
Cyclic nucleotide phosphodiesterases (PDEs) are a superfamily of enzymes whose physiological role is the attenuation of the signaling mediated by the ubiquitous second messengers cAMP and cGMP.
D. Palmer, D. Maurice
semanticscholar   +1 more source

3′:5′-cyclic-nucleotide phosphodiesterases of mammalian sera

Biochimica et Biophysica Acta (BBA) - Enzymology, 1975
Cyclic AMP and cyclic GMP phosphodiesterases (3':5'-cyclic-nucleotide 5'-nucleotidohydrolase EC 3.1.4.17) were found in the sera of human, dog, rabbit and rat. The formed elements of blood were not present in sera and thus not the source of the phosphodiesterase.
Tomiko Asano, Hiroyoshi Hidaka
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Peripheral participation of the phosphodiesterase 3 on formalin-evoked nociception

European Journal of Pharmacology, 2005
The local peripheral (subcutaneous) injection of phosphodiesterase 3 inhibitor trequinsin dose-dependently enhanced formalin-evoked flinching during late second phase of this test. Treatment with the nitric oxide synthase inhibitor N-L-nitro-arginine methyl ester or guanylyl cyclase inhibitor 1-H-[1,2,4,]oxadiazolo[4,3-a]quinoxalin-1-one significantly ...
Vinicio Granados-Soto   +1 more
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A microassay for guanosine 3′,5′-monophosphate phosphodiesterase activity

Analytical Biochemistry, 1974
Abstract The activity of cyclic GMP phosphodiesterase was determined using a three step procedure. In the first step, cyclic GMP phosphodiesterase catalyzes the conversion of cyclic GMP to 5′-GMP. In the second step, a known amount of ATP and guanylate kinase are incubated with the 5′-GMP formed in the first step.
Benjamin Weiss, Richard Fertel
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Cyclic 3′,5′-nucleotide phosphodiesterase of Serratia marcescens

Biochimica et Biophysica Acta (BBA) - Enzymology, 1970
Abstract 1. 1. A cyclic 3′,5′-nucleotide phosphodiesterase from the cells of Serratia marcescens was purified over 1000-fold. The purified preparation showed a pH maximum in the region of 7.5–8.5 in Tris-HCl buffer, with a K m of 0.52 mM for adenosine cyclic 3′,5′-phosphate.
Misao Ide, Tadashi Okabayashi
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Effect of some phosphodiesterase inhibitors on two different preparations of adenosine 3′,5′-monophosphate phosphodiesterase

Experientia, 1975
Neun Substanzen wurden an zwei verschiedenen PDE Praparationen auf ihre PDE hemmenden Eigenschaften untersucht. Dabei zeigte sich, dass die I50-Werte von der Art der Praparation und von der Substratkonzentration abhangen.
Joachim E. Schultz, A. du Moulin
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