phosphodiesterase i β

Siguazodan (SKF 94836) is an effective, selective, orally active phosphodiesterase III ((PDE-III)) inhibitor with an IC50 of 117 nM. Siguazodan inhibited phenylephrine induced 5-HT release with an IC50 value of 4.2 μM. Siguazodan can increase cAMP accumulation in intact platelets, with EC50 of 18.88 μM.

WAY127093B racemate is the racemic mixture of WAY127093B, a phosphodiesterase IV inhibitor with demonstrated oral activity in rats and guinea pigs.

Saterinone hydrochloride is an inhibitor of phosphodiesterase III (PDE III).

Phosphodiesterase-IN-3 (Example 20) is an inhibitor of phosphodiesterase 4B, with IC50 values for PDE4B1 and PDE4D3 of less than 10 nM and between 10-100 nM, respectively. Phosphodiesterase-IN-3 shows potential for research in idiopathic pulmonary fibrosis.

Phosphodiesterase-IN-4 (compound 18) is a potent inhibitor of Tyrosyl-DNA phosphodiesterase 1 (TDP1) and exhibits inhibitory effects on colorectal cancer cells, with an IC50 of 6.9 μM.

Phosphodiesterase-IN-2 (Compound C7) is an orally active and selective inhibitor of phosphodiesterase 10A (PDE10A), with an IC50 of 11.9 nM. It enhances hepatic microsomal stability and reduces blood-brain barrier permeability. Phosphodiesterase-IN-2 exhibits favorable pharmacokinetic properties in mouse models and can alleviate isoprenaline-induced cardiac hypertrophy.

Enprofylline (Enprofilina), a bronchodilator, acts primarily as a competitive nonselective phosphodiesterase inhibitor. Enprofylline is used in asthma, chronic obstructive pulmonary disease, and in the management of sickle cell disease, diabetic neuropathy, and cerebrovascular insufficiency.

Phosphodiesterase 2 (II), a key enzyme prominently involved in the hydrolysis of vital second messengers, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), is frequently utilized in biochemical research. This enzyme is expressed across various tissues including the adrenal medulla, brain, heart, platelets, macrophages, and endothelial cells, playing a significant role in the regulation of diverse intracellular processes [1].

Phosphodiesterase-IN-1 (Compound 7), a phosphodiesterase (PDE) inhibitor, exhibits anti-Plasmodium and antiproliferative activities. It effectively inhibits P. falciparum (strain 3D7) with an IC 50 value of 0.64 μM [1].