Title : Vardenafil: structural basis for higher potency over sildenafil in inhibiting cGMP-specific phosphodiesterase-5 (PDE5).

Pub. Date : 2004 Nov

PMID : 15312980






6 Functional Relationships(s)
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Protein Name
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1 Vardenafil: structural basis for higher potency over sildenafil in inhibiting cGMP-specific phosphodiesterase-5 (PDE5). Sildenafil Citrate phosphodiesterase 5A Homo sapiens
2 Vardenafil: structural basis for higher potency over sildenafil in inhibiting cGMP-specific phosphodiesterase-5 (PDE5). Sildenafil Citrate phosphodiesterase 5A Homo sapiens
3 Two commercialized PDE5 inhibitors, sildenafil and vardenafil, are being used to treat erectile dysfunction. Sildenafil Citrate phosphodiesterase 5A Homo sapiens
4 Although these are the only two structural differences, vardenafil has more than 20-fold greater potency than sildenafil for inhibiting purified PDE5. Sildenafil Citrate phosphodiesterase 5A Homo sapiens
5 The IC50 of methyl-sildenafil for inhibiting PDE5 indicated that it was 64 times less potent than demethyl-vardenafil, which was similar to the finding that, based on IC50, sildenafil was 40 times less potent than vardenafil. Sildenafil Citrate phosphodiesterase 5A Homo sapiens
6 Similarly, the EC50 of methyl-sildenafil for inhibiting [3H]vardenafil binding to PDE5 indicated that it was 84 times less potent than demethyl-vardenafil, while the EC50 for sildenafil indicated that it was 31 times less potent than vardenafil. Sildenafil Citrate phosphodiesterase 5A Homo sapiens