Phosphodiesterase 5 enzyme and its inhibitors: Update on pharmacological and therapeutical aspects

Methods and Findings in Experimental and Clinical Pharmacology

Volumn 26, Issue 10, 2004, Pages 789-799

  Kulkarni, S K ^a   Patil, C S ^a  

^a PANJAB UNIVERSITY   (India)

Author keywords

[No Author keywords available]

Indexed keywords

CAFFEINE; CYCLIC AMP; CYCLIC AMP DEPENDENT PROTEIN KINASE; CYCLIC GMP; CYCLIC GMP DEPENDENT PROTEIN KINASE; CYCLIC NUCLEOTIDE; DIPYRIDAMOLE; GLYCERYL TRINITRATE; HYDROLASE; ISOBUTYLMETHYLXANTHINE; NITRIC OXIDE; PHOSPHODIESTERASE; PHOSPHODIESTERASE I; PHOSPHODIESTERASE III; PHOSPHODIESTERASE IV; PHOSPHODIESTERASE IX; PHOSPHODIESTERASE V; PHOSPHODIESTERASE V INHIBITOR; PHOSPHODIESTERASE VI; PHOSPHODIESTERASE VII; PHOSPHODIESTERASE VIII; PHOSPHODIESTERASE X; PHOSPHODIESTERASE XI; SILDENAFIL; SPLEEN EXONUCLEASE; TADALAFIL; THEOPHYLLINE; UNCLASSIFIED DRUG; UNINDEXED DRUG; VARDENAFIL; ZAPRINAST;

AMINO ACID SEQUENCE; ANGINA PECTORIS; AORTA MEDIA; BACKACHE; CEREBELLUM; CLINICAL TRIAL; COMORBIDITY; DRUG EFFECT; DRUG EFFICACY; DRUG MECHANISM; DRUG SAFETY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG TARGETING; DYSPEPSIA; ENZYME ACTIVITY; ENZYME ANALYSIS; ENZYME INHIBITION; ENZYME LOCALIZATION; ENZYME MECHANISM; ENZYME PHOSPHORYLATION; ERECTILE DYSFUNCTION; FLUSHING; HEADACHE; HEART; HUMAN; HYPERTENSION; IMMUNOHISTOCHEMISTRY; INOTROPISM; KIDNEY; LIVER; LUNG; MOLECULAR CLONING; MYALGIA; NONHUMAN; NOSE CONGESTION; PANCREAS; PHARMACOKINETICS; PLACENTA; PROTEIN DOMAIN; REGULATORY MECHANISM; REVERSE TRANSCRIPTION POLYMERASE CHAIN REACTION; REVIEW; SECOND MESSENGER; SEQUENCE HOMOLOGY; SIDE EFFECT; SIGNAL TRANSDUCTION; SKELETAL MUSCLE; SMOOTH MUSCLE CONTRACTILITY; THROMBOCYTE; THROMBOCYTE AGGREGATION INHIBITION; TISSUE DISTRIBUTION; TRACHEA MUSCLE; VASCULAR TISSUE; VASODILATATION; VISUAL IMPAIRMENT;

3',5'-CYCLIC-GMP PHOSPHODIESTERASE; HUMANS; PHOSPHODIESTERASE INHIBITORS;

EID: 13244258565     PISSN: 03790355     EISSN: None     Source Type: Journal    
DOI: 10.1358/mf.2004.26.10.872561     Document Type: Review

References (52)

1. Francis, S.H. Lincoln, T.M., Corbin, J.D. Characterization of a novel cGMP binding protein from rat lung. J Biol Chem 1980. 255(2): 620-6.
2. McAllister-Lucas, L.M., Sonnenburg, W.K., Kadlecek, A. et al. The structure of a bovine lung cGMP-binding, cGMP-specific phosphodiesterase deduced from a cDNA clone. J Biol Chem 1993, 268(30): 22863-73.
3. Rascon, A. Cyclic nucleotide phosphodiesterases: Diversity, classification, structure and function. Acta Cient Venez 1997, 48(3): 145-53.
4. Corbin, J.D., Francis, S.H. Cyclic GMP phosphodiesterase-5: Target for sildenafil. J Biol Chem 1999, 274(20): 13729-32.
5. Degerman, E., Belfrage, P., Manganiello, V.C. Structure, localization, and regulation of cGMP-inhibited phosphodiesterase (PDE3). J Biol Chem 1997, 272(11): 6823-6.
6. Lin, C.S., Chow, S., Lau, A., Tu, R., Lue, T.F. Human PDE5A encodes three PDE5 isoforms from two alternate promoters. Int J Impot Res 2002, 14: 15-24.
7. Loughney, K., Hill, T.R., Florio, V.R. et al. Isolation and characterization of cDNAs encoding PDE5A, a human cGMP-binding, cGMP-specific 3′,5′-cyclic nucleotide phosphodiesterase. Gene 1998, 216(1): 139-47.
8. Yanaka, N., Kotera, J., Ohtsuka, A. et al. Expression, structure and chromosomal localization of the human cGMP-binding cGMP-specific phosphodiesterase PDE5A gene. Eur J Biochem 1998, 255 (2): 391-9.
9. Wyatt, T.A., Naftilan, A.J., Francis, S.H., Corbin, J.D. ANF elicits phosphorylation of the cGMP phosphodiesterase in vascular smooth muscle cells. Am J Physiol 1998, 274(2 Pt 2): H448-55.
10. Turko, I.V., Haik, T.L., McAllister-Lucas, L.M., Burns, F., Francis, S.H., Corbin, J.D. Identification of key amino acids in a conserved cGMP-binding site of cGMP-binding phosphodiesterases. A putative NKXnD motif for cGMP binding. J Biol Chem 1996, 271(36): 22240-4.
11. Corbin, J.D., Francis, S.H. Pharmacology of phosphodiesterase-5 inhibitors. Int J Clin Pract 2002, 56(6): 453-9.
12. Bischoff, E., Niewoehner, U., Haning, H., Es-Sayed, M., Schenke, T., Schlemmer, K.H. The oral efficacy of vardenafil hydrochloride for inducing penile erection in a conscious rabbit model. J Urol 2001, 165(4): 1316-8.
13. Padma-Nathan, H., McMurray, J.G., Pullman, W.E. et al. On-demand IC351 (Cialis) enhances erectile function in patients with erectile dysfunction. Int J Impot Res 2001, 13(1): 2-9.
14. Lue, T.F. Erectile dysfunction. N Engl J Med 2000, 324: 1802-13.
15. Broughton, B.J., Chaplen, P., Knowles, P. et al. New inhibitor of reagin-mediated anaphylaxis. Nature 1974, 251(5476): 650-2.
16. Bergstrand, H., Kristoffersson, J., Lundquist, B., Schurmann, A. Effects of antiallergic agents, compound 48/80, and some reference inhibitors on the activity of partially purified human lung tissue adenosine cyclic 3′,5′-monophosphate and guanosine cyclic 3′,5′- monophosphate phosphodiesterases. Mol Pharmacol 1977, 13(1): 38-43.
17. Vitezic, D. A risk-benefit assessment of sildenafil in the treatment of erectile dysfunction. Drug Saf 2001, 24(4): 255-65.
18. Olsson, A.M., Persson, C.A. Efficacy and safety of sildenafil citrate for the treatment of erectile dysfunction in men with cardiovascular disease. Int J Clin Pract 2001, 55(3): 171-6.
19. Moreland, R.B., Gupta, S., Goldstein, I., Traish, A. Cyclic AMP modulates TGF-β 1-induced fibrillar collagen synthesis in cultured human corpus cavernosum smooth muscle cells. Int J Impot Res 1998, 10(3): 159-63.
20. Bischoff, E., Schneider, K. A conscious rabbit model is able to demonstrate the efficacy of vardenafil and sildenafil on penile erection. Int J Impot Res 2000, 12(Suppl. 3): Abst. A17.
21. Saenz de Tejada, I., Angulo, J., Cuevas, P. 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(5): 282-90.
22. Patterson, B., Bedding A., Jewell H. Dose-normalized pharmacokinetic of Tadalafil (IC 351) administered as a single dose to a healthy volunteers. Poster, presented at ESSIR, Rome 2001.
23. Milligan, P.A., Marshall, S.F., Karlsson, M.O. A population pharmacokinetic analysis of sildenafil citrate in patients with erectile dysfunction. Br J Clin Pharmacol 2002, 53(Suppl 1): 45S-52S.
24. Sachse, R., Rohde, G. Safety, Tolerability and pharmacokinetic of BAY 38-9456 in patients with erectile dysfunction. Poster, presented at AUA, Atlanta 2000.
25. Nichols, D.J., Muirhead, G.J., Harness, J.A. Pharmacokinetics of sildenafil after single oral doses in healthy male subjects: Absolute bioavailability, food effects and dose proportionality. Br J Clin Pharmacol 2002, 53(Suppl 1): 5S-12S.
26. Eichelbaum, M., Burk, O. CYP3A genetics in drug metabolism. Nat Med 2001, 7(3): 285-7.
27. Baxendale, R.W., Burslem, F., Phillips, S.C. Phosphodiesterase type II (PDE II) cellular localization: Progress towards defining a physiological role in testis and/ or reproduction. Poster, presented at AUA, Anaheim 2001.
28. Porst H. Die tagliche oder bedarforientierte Veraberichung von IC351 zur Bechandlung der erektilen Dysfunktion. Poster, presented at DAU, Hamburg 2000.
29. Muirhead, G.J., Wulff, M.B., Fielding, A., Kleinermans, D., Buss, N. Pharmacokinetic interactions between sildenafil and saquinavir/ ritonavir. Br J Clin Pharmacol 2000, 50(2): 99-107.
30. Augulo, J., Gadau, M., Fernandez, A. IC 351 enhances NO mediated relaxation of human arterial and trabecular penile smooth muscle. Poster presented at ESSIR, Rome 2001.
31. Gresser, U., Gleiter, C.H. Erectile dysfunction: Comparison of efficacy and side effects of the PDE-5 inhibitors sildenafil, vardenafil and tadalafil-review of the literature. Eur J Med Res 2002, 7(10): 435-46.
32. Rotella, D.P. Phosphodiesterase 5 inhibitors: Current status and potential applications. Nat Rev Drug Discov 2002, 1(9): 674-82.
33. Kotera, J., Fujishige, K., Michibata, H. et al. Characterization and effects of methyl-2-(4-aminophenyl)-1,2-dihydro-1-oxo-7-(2-pyridinylmethoxy)-4- (3,4,5-trimethoxyphenyl)-3-isoquinoline carboxylate sulfate T-1032), a novel potent inhibitor of cGMP-binding cGMP-specific phosphodiesterase (PDE5). Biochem Pharmacol 2000, 60(9): 1333-41.
34. NIH Consensus Conference. Impotence. NIH Consensus Development Panel on Impotence. JAMA 1993, 270(1): 83-90.
35. Andersson, K.E. Pharmacology of penile erection. Pharmacol Rev 2001, 53(3): 417-50.
36. Archer, S.L. Potassium channels and erectile dysfunction. Vascul Pharmacol 2002, 38(1): 61-71.
37. Jackson, G. Phosphodiesterase 5 inhibition: Effects on the coronary vasculature. Int J Clin Pract 2001, 55(3): 183-8.
38. Hakim, L.S., Goldstein, I. Diabetic sexual dysfunction. Endocrinol Metab Clin North Am 1996, 25(2): 379-400.
39. Nehra, A., Moreland, R.B. Neurologic erectile dysfunction. Urol Clin North Am 2001, 28(2): 289-308.
40. Tao, Y.X., Hassan, A., Haddad, E., Johns, R.A. Expression and action of cyclic GMP-dependent protein kinase 1alpha in inflammatory hyperalgesia in rat spinal cord. Neuroscience 2000, 95(2): 525-33.
41. Jain, N.K., Paul, C.S., Singh, A., Kulkarni, S.K. Sildenafil-induced peripheral analgesia and activation of the nitric oxide-cyclic GMP pathway. Brain Res 2001, 909(1-2): 170-8.
42. Moncada, S., Higgs, A. The L-arginine-nitric oxide pathway. N Engl J Med 1993, 329(27): 2002-12.
43. Furness, J.B., Johnson, P.J., Pompolo, S., Bornstein, J.C. Evidence that enteric motility reflexes can be initiated through entirely intrinsic mechanisms in the guinea-pig small intestine. Neurogastroenterol Motil 1995, 7(2): 89-96.
44. Murthy, K.S. Activation of phosphodiesterase 5 and inhibition of guanylate cyclase by cGMP-dependent protein kinase in smooth muscle. Biochem J 2001, 360(Pt 1): 199-208.
45. Watkins, C.C., Sawa, A., Jaffrey, S. et al. Insulin restores neuronal nitric oxide synthase expression and function that is lost in diabetic gastropathy. J Clin Invest 2000, 106(3): 373-84.
46. Bortolotti, M., Mari, C., Giovannini, M., Pinna, S., Miglioli, M., Pandolfo, N. Effects of sildenafil on esophageal motility of normal subjects. Dig Dis Sci 2001, 46(11): 2301-6.
47. Prickaerts, J., De Vente, J., Honig, W., Steinbusch, H.W.M., Blockland, A. Cyclic GMP, but not cyclic AMP, in rat hippocampus is involved in early stages of object memory consolidation. Eur J Pharmacol 2002, 436: 83-7.
48. Kotera, J., Fujishige, K., Omori, K. Immunohistochemical localization of cGMP-binding cGMP-specific phosphodiesterase (PDE5) in rat tissues. J Histochem Cytochem 2000, 48(5): 685-93.
49. Baratti, C.M., Boccia, M.M. Effects of sildenafil on long-term retention of an inhibitory avoidance response in mice. Behav Pharmacol 1999, 10(8): 731-7.
50. Bortolotti, M., Mari, C., Lopilato, C. Effects of sildenafil on esophageal motility of patients with idiopathic achalasia. Gastroenterology 2000, 118: 253-7.
51. McPherson, M.A., Pereira, M.M., Lloyd Mills, C., Murray, K.J., Dormer, R.L. A cyclic micleotide PDE5 inhibitor corrects defective mucin secretion in submandibular cells containing antibody directed against the cystic fibrosis transmembrane conductance regulator protein. FEBS Lett 1999, 464(1-2): 48-52.
52. Wang, X., Robinson, P.J. Cyclic GMP-dependent protein kinase and cellular signaling in the nervous system. J Neurochem 1997, 68(2): 443-56.