phosphodiesterase 5

CM-675 is a dual inhibitor of phosphodiesterase 5 (PDE5) and class I histone deacetylases (IC50s: 114 nM and 673 nM for PDE5 and HDAC1) with the potential to treat Alzheimer's disease.

UK 227786 is an inhibitor of phosphodiesterase 5 (PDE5), used for treatment of prostatic diseases.

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.

Gisadenafil (UK-369003), a selective inhibitor of phosphodiesterase 5 (PDE5) with an IC50 of 3.6 nM, prevents the degradation of cGMP.

inhibitor of phosphodiesterase type 5 (PDE5).This compound is unstable in powder form and other related salt forms are recommended.

T-0156 is a novel, potent and selective phosphodiesterase type 5 inhibitor that inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) with low affinity for PDE6, PDE1, PDE2, PDE3 and PDE4.

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.

Tiflucarbine is a potential non-selective 5-HT agonist with antidepressant activity.Tiflucarbine dose-dependently increased the specific activity of soluble calmodulin (CaM)-dependent phosphodiesterase in rat brain.

Vardenafil (Vivanza) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.

Sildenafil citrate (UK-92480 citrate) , a cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5) Inhibitor, is used extensively for erectile dysfunction and less commonly for pulmonary hypertension.

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.

Tadalafil (IC-351) is a carboline-based compound with vasodilatory activity that selectively inhibits the cyclic guanosine monophosphate (cGMP)-specific type 5 phosphodiesterase (PDE-5), preventing cGMP degradation in the smooth muscle of the corpus cavernosa and corpus spongiosum of the penis, thereby causing prolonged muscle relaxation, vasodilation, and enhanced penile erection.

Avanafil (TA1790) is a selective inhibitor of phosphodiesterase type 5 (PDE5) and is used as therapy of erectile dysfunction.

N-Desmethyl Sildenafil is the major metabolite of Sildenafil, a potent phosphodiesterase type 5 (PDE5) inhibitor.

Vardenafil hydrochloride is a New Phosphodiesterase Type 5(PDE5) Inhibitor, in the Treatment of Erectile Dysfunction in Men With Diabetes

Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor,and is an antispasmodic drug, used to enhance cervical dilation during childbirth. Drotaverine hydrochloride is structurally related to papaverine

5-Bromoimidazo[1,2-a]pyrazine inhibits phosphodiesterase and beta-adrenergic receptors.5-Bromoimidazo[1,2-a]pyrazine shows antibronchospastic activity in vitro.

Thioquinapiperifil dihydrochloride is a phosphodiesterase (PDE-5) inhibitor (IC50: 0.074 nM) that is potent, selective and non-competitive for investigational maturation.

ER21355, utilized for the treatment of prostatic diseases, acts as a phosphodiesterase 5 (PDE5) inhibitor.

Gisadenafil besylate (UK 369003-26) is a potent and orally active PDE5 inhibitor (IC50=1.23 nM), 100 times more selective for PDE5 than PDE6, for the study of lower urinary tract symptoms associated with benign prostatic hyperplasia.

SIBA (5'-Deoxy-5'-isobutylthioadenosine) is a synthetic analogue of SAH, acts as an inhibitor of S-adenosylmethionine-mediated transmethylation. SIBA can interfere with a variety of enzymatic activities in vitro, such as SAH hydrolase, methylthioadenosine phosphorylase and cAMP phosphodiesterase. SIBA reversibly blocks the multiplication of herpes simplex type 1 virus (HSV)

Mirodenafil is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.

MY-5445 (N-(3-chlorophenyl)-4-phenylphthalazin-1-amine) is a specific inhibitor of phosphodiesterase type 5 (PDE5). MY-5445 selectively inhibits cGMP PDE (Ki:1.3 μM).

N-Ethyl tadalafil (NEthyl tadalafil) is a CGMP-specific 3',5'-cyclic phosphodiesterase (PDE) inhibitor used in the study of cardiovascular diseases such as angina pectoris, hypertension, and pulmonary hypertension.