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The occurrence of side effects, or adverse drug reactions (ADRs), with PDE5 inhibitors depends on the dose and type of agent. [1] Headache is a very common ADR, occurring in >10% of patients. Other common ADRs include: dizziness, flushing, dyspepsia, nasal congestion or rhinitis. [6]
Phosphodiesterase-5. A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE), thereby preventing the inactivation of the intracellular second messengers, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) by the respective PDE subtype(s).
Cyclic guanosine monophosphate-specific phosphodiesterase type 5 is an enzyme (EC 3.1.4.17) from the phosphodiesterase class. It is found in various tissues, most prominently the corpus cavernosum of the clitoris and of the penis as well as the retina. [5] It has also been recently discovered to play a vital role in the cardiovascular system.
Phosphodiesterase 5 is widely expressed in several tissues in the body for example brain, lung, kidney, urinary bladder, smooth muscle and platelets. [1] It is possible to prevent cGMP hydrolysis by inhibiting PDE5 and therefore treat diseases associated with low cGMP levels, because of this, PDE5 is an ideal target for the development of ...
Inhibitors of PDE can prolong or enhance the effects of physiological processes mediated by cAMP or cGMP by inhibition of their degradation by PDE. [13] Sildenafil (Viagra) is an inhibitor of cGMP-specific phosphodiesterase type 5, which enhances the vasodilatory effects of cGMP in the corpus cavernosum and is used to treat erectile dysfunction.
Trodusquemine is an aminosterol (polyamine steroid conjugate) that inhibits protein tyrosine phosphatase 1B (PTP1B) activity. [1] The compound exhibits broad-spectrum antimicrobial activity [2] and numerous regenerative, neuroprotective, anti-atherosclerotic, antitumor, antiangiogenic, antiobesity, and anxiolytic properties. [3]
Dipyridamole inhibits the phosphodiesterase enzymes that normally break down cAMP (increasing cellular cAMP levels and blocking the platelet aggregation, response [3] to ADP) and/or cGMP. Dipyridamole inhibits the cellular reuptake of adenosine into platelets , red blood cells , and endothelial cells , leading to increased extracellular ...
Phosphodiesterase 9 inhibitors or PDE9 inhibitors are a class of drugs that work by inhibiting the activity of PDE9. The first compound with this effect, BAY 73-6691 , was reported in 2004. [ 1 ] PDE9 inhibitors are under investigation for the treatment of obesity, [ 2 ] hepatic fibrosis , [ 3 ] Alzheimer's disease , schizophrenia , other ...
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