introduction: it was shown in a previous study, that mcpip, a cilostamide derivative, increased atrial contraction force without changing contraction rate. to improve this property, two new derivatives of cilostamide were synthesized and their effects on pde3 activity and isolated rat atria contraction were investigated. methods: the inhibitory effect of each compound on pde3 enzyme was determi...

Abstract Background Coronavirus disease 2019 (Covid-19) is an infectious worldwide pandemic triggered by severe acute respiratory coronavirus 2 (SARS-CoV-2). This can lead to pro-inflammatory activation with associated lung injury and distress syndrome. Main body of the abstract SARS-CoV-2 infection linked inhibition adenosine phosphodiesterase. Dipyridamole (DIP) a nucleoside transport phospho...

Pentoxifylline a derivative of methylxanthine and nonspecific inhibitor the phosphodiesterase with vasodilatory properties rheological on blood that made it useful in treatment intermittent claudication.

The genome of Drosophila melanogaster has been surveyed for chromosomal regions which exert a dosage effect on the activities of cAMP phosphodiesterase or cGMP phosphodiesterase. Two regions increase cAMP phosphodiesterase activity when present as duplications. A region of the X chromosome increases cAMP phosphodiesterase activity when duplicated and decreases that activity when deficient. This...

       In this study, we investigated the interactive effects of intraperitoneal (i.p.) injections of three different phosphodiesterase inhibitors (PDEIs) on morphine-induced analgesia in mice using tail-flick method. Subcutaneous administration of morphine (1, 3 and 6 mg/kg) caused significant antinociceptive effects in a dose dependent manner. Administration of pentoxifylline (12.5, 25, 50 an...

Phosphodiesterase is an enzyme that degrades the phosphodiester bond in second messenger molecules cAMP and cGMP, regulates localization, duration, amplitude of cyclic nucleotide signaling within subcellular domains. Sildenafil a potent selective inhibitor type 5 cGMP-specific phosphodiesterase used clinically to treat erectile dysfunction pulmonary arterial hypertension. In this study, we exam...

Chemotactic stimulation of vegetative or aggregative Dictyostelium discoideum cells induced a transient elevation of cyclic GMP levels. The addition of chemoattractants to postvegetative cells by pulsing induced phosphodiesterase activity. The following lines of evidence suggest a messenger function for cyclic GMP in the induction of phosphodiesterase: (i) Folic acid and cyclic AMP increased cy...

Background: The clinical phenotyping of patients with achromatopsia harboring variants in phosphordiesterase 6C (PDE6C) has poorly been described in the literature. PDE6C encodes the catalytic subunit of the cone phosphodiesterase, which hydrolyzes the cyclic guanosine monophosphate that proceeds with the hyperpolarization of photoreceptor cell membranes, as the final step of the phototransduct...

Frog (Rana catesbiana) rod outer segment disc membranes contain a cyclic nucleotide phosphodiesterase (EC 3.1.4.17) which is activated by light in the presence of ATP. This enzyme is firmly bound to the disc membrane, but can be eluted from the membrane with 10 mM Tris-HCl buffer, pH 7.4 and 2 mM EDTA. The eluted phosphodiesterase has reduced activity, but can be activated approximately 10-fold...

Cyclic nucleotide phosphodiesterase activities in soluble Neurospora crassa mycelial extracts were resolved into two peaks, phosphodiesterase I and II, by chromatography on DEAE-cellulose columns. Phosphodiesterase I hydrolysed cyclic AMP and cyclic GMP equally well. Phosphodiesterase II was active on cyclic GMP but scarcely active on cyclic AMP. Phosphodiesterase I was resolved by gel filtrati...