Potency, selectivity, and consequences of nonselectivity of PDE inhibition

International Journal of Impotence Research

Volumn 16, Issue SUPPL. 1, 2004, Pages

  Bischoff, E ^a  

^a BAYER PHARMA AG   (Germany)

Author keywords

3 ,5 cyclic nucleotide phosphodiesterase; Phosphodiesterase inhibitors; Sildenafil; Tadalafil; Vardenafil

Indexed keywords

CYCLIC GMP DEPENDENT PROTEIN KINASE INHIBITOR; PHOSPHODIESTERASE; PHOSPHODIESTERASE III; PHOSPHODIESTERASE INHIBITOR; PHOSPHODIESTERASE V; PHOSPHODIESTERASE V INHIBITOR; PHOSPHODIESTERASE VI; PHOSPHODIESTERASE XI; SILDENAFIL; TADALAFIL; UNCLASSIFIED DRUG; VARDENAFIL;

ARTICLE; BRAIN; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; ENZYME INHIBITION; HEART MUSCLE; HEART RATE; HUMAN; IC 50; PRIORITY JOURNAL; RETINA; SIGNAL TRANSDUCTION; TACHYCARDIA; THROMBOCYTE AGGREGATION INHIBITION; VASCULAR SMOOTH MUSCLE; VASODILATATION; VISUAL DISORDER; VISUAL TRANSDUCTION;

3',5'-CYCLIC-GMP PHOSPHODIESTERASE; ANIMALS; CARBOLINES; HEART RATE; HUMANS; IMIDAZOLES; MALE; PHOSPHODIESTERASE INHIBITORS; PIPERAZINES; SUBSTRATE SPECIFICITY; SULFONES; TACHYCARDIA; TRIAZINES; VASODILATION; VISION;

EID: 3342991544     PISSN: 09559930     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.ijir.3901208     Document Type: Article

References (12)

1. Saenz de Tejada I et al. The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Int J Impot Res 2001; 13: 282-290.
2. Porst H. IC351 (tadalafil, Cialis): update on clinical experience. Int J Impot Res 2002; 14(Suppl 1): S57-S64.
3. Turko IV, Ballard SA, Francis SH, Corbin JD. Inhibition of cyclic GMP-binding cyclic GMP-specific phosphodiesterase (type 5) by sildenafil and related compounds. Mol Pharmacol 1999; 56: 124-130.
4. Saenz de Tejada I, Frutos JA, Gaudo M, Florio V. Comparative selectivity: profiles of tadalafil, sildenafil and vardenafil using an in vitro phosphodiesterase activity assay. Int J Impot Res 2002; 14(Suppl 4): S20-S32.
5. Corbin JD, Francis SH. Pharmacology of phosphodiesterase-5 inhibitors. Int J Clin Pract 2002; 277: 47581-47587.
6. Gbekor E et al. Selectivity of sildenafil and other phosphodiesterase type 5 (PDE5) inhibitors against all human phosphodiesterase families. Eur Urol 2002; 42(Suppl 1): 63.
7. Kim NN et al. Inhibition of cyclic GMP hydrolysis in human corpus cavernosum smooth muscle cells by vardenafil, a novel selective phosphodiesterase type 5 inhibitor. Life Sci 2001; 69: 2249-2256.
8. Bardou M et al. Hypoxic vasoconstriction of rat main pulmonary artery: role of endogenous nitric oxide, potassium channels, and phosphodiesterase inhibition. J Cardiovasc Pharmacol 2001; 38: 325-334.
9. Stief CG. Phosphodiesterase inhibitors in the treatment of erectile dysfunction. Drugs Today 2000; 36: 93-99.
10. Moreland RB, Goldstein II, Kim NN, Traish A. Sildenafil citrate, a selective phosphodiesterase type 5 inhibitor. Trends Endocrinol Metab 1999; 10: 97-104.
11. McGrouther C et al. Biochemical in situ hybridisation (ISH) and immunohistochemical (ICH) characterisation of phosphodiesterase type 5 (PDE5) expression in human corpus cavernosum (CC) and cardiac tissue. Int J Impot Res 2000; 12(Suppl 1): S27.
12. Burslem M, Harrow J, Lanfear I, Phillips SC. Modulation of PDE11A activity. Patent # EP 12 11 313 A2, 2002.