camp pde

Isoprenaline hydrochloride (NCI-c55630) is a potent beta-adrenergic agonist with the peripheral vasodilator, bronchodilator, and cardiac stimulating properties.

Torbafylline, a xanthine derivative, is a phosphodiesterase (PDE) inhibitor that attenuates burn-induced protein hydrolysis in rat skeletal muscle through activation of the PDE4 cAMP EPAC PI3K Akt pathway, and inhibits the enhanced ubiquitin-proteasome-dependent protein hydrolysis in skeletal muscle of cancer- and sepsis-prone rats.

IBMX (Methylisobutylxanthine) is a broad-spectrum phosphodiesterase (PDE) inhibitor with inhibitory activity against PDE3, PDE4, and PDE5 (IC50=6.5 26.3 31.7 μM). IBMX enhances the intracellular cAMP level.

Bucladesine sodium (DC2797) is a cAMP analog with cell-permeable properties. Bucladesine sodium is also a cAMP-dependent protein kinase (PKA) activator and a phosphodiester (PDE) inhibitor. Bucladesine sodium has anti-inflammatory activity.

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.

BC 11-38 is a potent, selective PDE biodepressant which is mainly effective against PDE11 (IC50 : 0.28 μM).

Saterinone is a potent and selective phosphodiesterase III inhibitor and a potent antagonist of the vascular α-1-adrenoceptor. Saterinone has vasodilatory properties and can be used in the acute treatment of chronic heart failure. Saterinone inhibited crude cAMP phosphodiesterase (PDE) activity in guinea pig right ventricular homogenates The ic50 value is 2.3 × 10(-5) mol l.

Roflumilast (APTA 2217) is an orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3', 5'-adenosine monophosphate (cAMP) and cAMP-mediated signaling.

MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4).

Butein is a cAMP-specific PDE inhibitor, protein tyrosine kinase inhibitor, and SIRT1 activator. It sensitizes HeLa cells to Cisplatin by targeting FoxO3a via the AKT and ERK p38 MAPK pathways.

RS 25344 hydrochloride is a phosphodiesterase (PDE) 4 inhibitor

(S)-(+)-Rolipram ((+)-Rolipram) inhibits human monocyte cyclic AMP-specific PDE4 with an IC50 of 0.75 μM and exhibits anti-inflammatory and anti-depressant activity in the central nervous system, though it is less potent than its R enantiomer.

TP-10 is a selective inhibitor of PDE10A against other PDEs with IC50 of 0.8 nM.

Ro 20-1724 (4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone) is a widely used inhibitor of cyclic nucleotide phosphodiesterase with IC50 of 2.0 μM and Ki of 3.1 μM.

Compound 4p (PDE4B D-IN-4) is an effective inhibitor of PDE-4B and PDE-4D, with IC50 values of 5.50 nM and 6.81 nM respectively. Following the administration of PDE4B D-IN-4, intracellular cAMP levels are elevated.

D-159404, as an allosteric inhibitor, demonstrates superior inhibitory effects on the full-length PDE 4D3 compared to its truncated form and exhibits higher cellular activity. This sets it apart from competitive inhibitors like roflumilast and cilomilast. These findings indicate that D-159404 and related compounds may offer valuable insights into PDE 4 pharmacology and serve as strong candidates for further study on cAMP signaling's impact on disease treatment.

CI-930 is a PDE-III inhibitor with broad-spectrum activity. It exerts its anti-aggregation effects through a dual mechanism: enhancing cAMP levels and selectively inhibiting the synthesis of TXA2 in platelets. CI-930 effectively inhibits platelet aggregation induced by AA, U-46619, ADP, collagen, and PAF, with IC50 values of 0.91, 0.73, 2.12, 2.35, and 7.15 mumols L, respectively.

Lixazinone is a cyclic adenosine monophosphate phosphodiesterase (cAMP PDE) inhibitor and a cardiac enhancer.

8-CPT-cAMP is a PDE Va inhibitor.

Lixazinone sulfate anhydrous is an inhibitor of cyclic adenosine monophosphate phosphodiesterase (cAMP PDE) and acts as a cardiac enhancer.

Lixazinone sulfate is a cyclic adenosine monophosphate phosphodiesterase (cAMP PDE) inhibitor with cardiotonic properties.

Trequinsin HCl is a phosphodiesterase (PDE) 3 inhibitor dependent on cyclic adenosine monophosphate (cAMP). It facilitates the accumulation of cAMP and enhances cell membrane capacitance.

MP 518 is a PDE inhibitor with antihypertensive properties. It prevents the degradation of cAMP, leading to increased ICa levels, and counteracts the effects of β-adrenergic stimulation, resulting in vasodilation.

8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA) and a potent inhibitor of cyclic GMP-specific phosphodiesterase (PDE VA) with an inhibitory concentration (IC50) of 0.9 μM. It also inhibits PDE III and PDE IV while significantly activating Epac, demonstrating diverse pharmacological activities [1] [2].