Sildenafil citrate (171599-83-0) is a potent and selective phosphodiesterase (PDE5) inhibitor, IC50=4 nM).1-3 Clinically useful agent for male erectile disfunction4 and pulmonary hypertension5.
1) Terrett et al. (1996), Sildenafil (VIAGRATM), a potent and selective inhibitor of type 5 cGMP phosphodiesterase with utility for the treatment of male erectile dysfunction; Bioorg. Med. Chem. Lett., 6 1819
2) Ballard et al. (1998), Effects of sildenafil on the relaxation of human corpus cavernosum tissue in vitro and on the activities of cyclic nucleotide phosphodiesterase isozymes; J. Urol., 159 2164
3) Turko et al. (1999), Inhibition of cyclic GMP-binding cyclic GMP-specific phosphodiesterase (Type 5) by sildenafil and related compounds; Mol. Pharmacol., 56 124
4) Teixeira et al. (2006), Differential effects of the phosphodiesterase type 5 inhibitors sildenafil, vardenafil, and tadalafil in rat aorta; J. Pharmacol. Exp. Therap., 316 654
5) Ghofrani et al. (2006), Sildenafil: from angina to erectile dysfunction to pulmonary hypertension and beyond; Nat. Rev. Drug Discov., 5 689