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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).
PDE enzymes are composed of 3 functional domains: an N-terminal cyclin fold domain, a linker helical domain and a C-terminal helical bundle domain (see figure 3). [9] The active site is a deep pocket at the junction of the 3 subdomains and is lined with highly conserved residues between isotypes of PDE. [14]
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.
Chemical structure of sildenafil (Viagra), the prototypical PDE5 inhibitor. A phosphodiesterase type 5 inhibitor (PDE5 inhibitor) is a vasodilating drug that works by blocking the degradative action of cGMP-specific phosphodiesterase type 5 (PDE5) on cyclic GMP in the smooth muscle cells lining the blood vessels supplying various tissues.
8654 242202 Ensembl ENSG00000138735 ENSMUSG00000053965 UniProt O76074 Q8CG03 RefSeq (mRNA) NM_033437 NM_001083 NM_033430 NM_153422 RefSeq (protein) NP_001074 NP_236914 NP_246273 NP_700471 Location (UCSC) Chr 4: 119.49 – 119.63 Mb Chr 3: 122.52 – 122.65 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Cyclic guanosine monophosphate-specific phosphodiesterase type 5 is an enzyme (EC ...
The phosphate atom in cAMP binds to PDE active site, using an arginine residue and a water molecule, which was initially associated with Mg 2+. A second arginine residue and the Mg 2+ may also play roles during binding and/or play roles in the next step; S N 2 attack of phosphorus by H 2 O with formation of a trigonal bipyramid transition state
Older PDE 10A inhibitors such as papaverine have been shown to produce antipsychotic effects in animal models, [3] and more potent and selective PDE 10A inhibitors are a current area of research for novel antipsychotic drugs which act through a different pathway to conventional dopamine or 5-HT 2A antagonist drugs and may have a more favourable ...
The Authority was established under Act 13 of 2002, ... Act. [2] The Authority began collecting Serious Events (events that harm the patient) and Incidents ...