Characterization of a novel phosphodiesterase type 5 inhibitor: JNJ-10258859

European Journal of Pharmacology

Volumn 472, Issue 1-2, 2003, Pages 73-80

  Qiu, Yuhong ^a   Bhattacharjee, Sheela ^a   Kraft, Patricia ^a   John, T Mathew ^a   Craig, Elizabeth ^a,b   Haynes Johnson, Donna ^a   Guan, Jihua ^a   Jiang, Weiqin ^a   Macielag, Mark ^a   Sui, Zhihua ^a   Clancy, Joanna ^a,c   Lundeen, Scott ^a  

^a Drug Discovery Raritan   (United States)

^b Serono   (United States)

^c Antex Biologics   (United States)

Author keywords

Corpus cavernosum; Erectile dysfunction; Phosphodiesterase; Phosphodiesterase type 5 inhibitor

Indexed keywords

3 (2,3 DIHYDROBENZOFURAN 5 YL) 2 [5 (4 METHOXYPHENYL)PYRIMIDIN 2 YL] 1,2,3,4 TETRAHYDROPYRROLO[3,4 B]QUINOLIN 9 ONE; CYCLIC GMP; JNJ 10258859; NITRIC OXIDE; PHOSPHODIESTERASE; PHOSPHODIESTERASE I; PHOSPHODIESTERASE INHIBITOR; PHOSPHODIESTERASE V; PHOSPHODIESTERASE VI; SILDENAFIL; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; AORTA PRESSURE; ARTICLE; ASSAY; CONTROLLED STUDY; DOG; DOSE RESPONSE; DRUG EFFECT; DRUG EFFICACY; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; ELECTROSTIMULATION; ENZYME INHIBITION; ENZYME PURIFICATION; ERECTILE DYSFUNCTION; HEART RATE; HUMAN; HUMAN TISSUE; IN VIVO STUDY; MALE; NONHUMAN; PELVIC NERVE; PRIORITY JOURNAL;

EID: 12444333500     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(03)01868-5     Document Type: Article

References (28)

1. Boolell M., Allen M.J., Ballard S.A., Gepi-Attee S., Muirhead G.J., Naylor A.M., Osterloh I.H., Gingell C. Sildenafil: an orally active type 5 cyclic GMP-specific phosphodiesterase inhibitor for the treatment of penile erectile dysfunction. Int. J. Impot. Res. 8:1996;47-52.
2. Burnett A.L., Lowenstein C.J., Bredt D.S., Chang T.S., Snyder S.H. Nitric oxide: a physiologic mediator of penile erection. Science. 257:1992;401-403.
3. Carter A.J., Ballard S.A., Naylor A.M. Effect of the selective phosphodiesterase type 5 inhibitor sildenafil on erectile function in the anesthetized dog. J. Urol. 160:1998;212-246.
4. Coste H., Grondin P. Characterization of a novel potent and specific inhibitor of type V phosphodiesterase. Biochem. Pharmacol. 50:1995;1577-1585.
5. Eardley I. The role of phosphodiesterase inhibitors in impotence. Exp. Opin. Invest. Drugs. 6:1997;1803-1810.
6. Feldman H., Goldstein A.I., Hatzichristou D.G., Krane R.J., Mckinlay J.B. Impotence and its medical and psychosocial correlates: results of Massachusetts male aging study. J. Urol. 151:1994;54-61.
7. Francis S.H., Turko I.V., Corbin J.D. Cyclic nucleotide phosphodiesterases: relating structure and function. Prog. Nucleic Acid Res. Mol. Biol. 65:2001;1-52.
8. Gillespie P.G., Beavo J.A. Characterization of a bovine cone photoreceptor phosphodiesterase purified by cyclic GMP-sepharose chromatography. J. Biol. Chem. 263:1988;8133-8141.
9. Hamet P., Coquil J.F. Cyclic GMP binding and cyclic GMP phosphodiesterase in rat platelets. J. Cyclic Nucleotide Res. 4:1978;281-290.
10. Hosogai N., Hamada K., Tomita M., Nagashima A., Takahashi T., Sekizawa T., Mizutani T., Urano Y., Kuroda A., Sawada K., Ozaki T., Seki J., Goto T. FR226807: a potent and selective phosphodiesterase type 5 inhibitor. Eur. J. Pharmacol. 428:2001;295-302.
11. Ignarro L.J., Bush P.A., Buga G.M., Wood K.S., Fukuto J.M., Rajfer J. Nitric oxide and cyclic GMP formation upon electrical field stimulation cause relaxation of corpus cavernosum smooth muscle. Biochem. Biophys. Res. Commun. 170:1990;843-850.
12. Kim N., Azadzoi K.M., Goldstein I., Saenz de Tejada I. A nitric oxide-like factor mediates nonadrenergic-noncholinergic neurogenic relaxation of penile corpus cavernosum smooth muscle. J. Clin. Invest. 88:1991;112-118.
13. Kotera J., Fujishige K., Michibata H., Yuasa K., Kubo A., Nakamura Y., Omori K. 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. 60:2000;1333-1341.
14. Kuthe A., Wiedenroth A., Magert H.J., Uckert S., Forssmann W.G., Stief C.G., Jonas U. Expression of different phosphodiesterase genes in human cavernous smooth muscle. J. Urol. 165:2001;280-283.
15. Ormrod D., Easthope S.E., Figgitt D.P. Vardenafil. Drugs Aging. 19:2002;217-227.
16. Qiu Y., Kraft P., Lombardi E., Clancy J. Rabbit corpus cavernosum smooth muscle shows a different phosphodiesterase profile than human corpus cavernosum. J. Urol. 164:2000;882-886.
17. Saenz de Tejada I., Angulo J., Cuevas P., Fernandez A., Moncada I., Allona A., Lledo E., Korschen H.G., Niewohner U., Haning H., Pages E., Bischoff E. The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Int. J. Impot. Res. 13:2001;282-290.
18. Schroder H., Leitman D., Hayward L., Bennet B., Murad F. Cultured rat lung fibroblasts as a model for organic nitrate-induced cyclic GMP accumulation and activation of guanylate cyclase. J. Appl. Cardiol. 2:1987;301-311.
19. Shahid M., van Amsterdam R.G., de Boer J., ten Berge R.E., Nicholson C.D., Zaagsma J. The presence of five cyclic nucleotide phosphodiesterase isoenzyme activities in bovine tracheal smooth muscle and the functional effects of selective inhibitors. Br. J. Pharmacol. 104:1991;471-477.
20. Silver P.J., Pagani E.D., Dundore R.L., de Garavilla L., Bode D.C., Bacon E.R. Cardiovascular activity of WIN 65579, a novel inhibitor of cyclic GMP phosphodiesterase 5. Eur. J. Pharmacol. 349:1998;263-268.
21. Sorbera L.A., Martin L., Leeson P.A., Castaner J. IC-351. Drugs Future. 26:2001;15-19.
22. Sui Z., Guan J., Macielag M.J., Jiang W., Zhang S., Qiu Y., Kraft P., Bhattacharjee S., John T.M., Haynes-Johnson D., Clancy J. Pyrimidinylpyrroloquinolones as highly potent and selective PDE5 inhibitors for treatment of erectile dysfunction. J. Med. Chem. 45:2002;4094-4096.
23. Taher A., Meyer M., Stief C.G., Jonas U., Forssmann W.G. Cyclic nucleotide phosphodiesterase in human cavernous smooth muscle. World J. Urol. 15:1997;32-35.
24. Thompson W.J., Appleman M.M. Multiple cyclic nucleotide phosphodiesterase activities from rat brain. Biochemistry. 10:1971;311-316.
25. Torphy T.J., Undem B.J., Cieslinski L.B., Luttmann M.A., Reeves M.L., Hay D.W.P. Identification, characterization and functional role of phosphodiesterase isozymes in human airway smooth muscle. J. Pharmacol. Exp. Ther. 265:1993;1213-1223.
26. Vardi Y., Padma-Nathan H., Siroky M.B. A canine model for hemodynamic study of isolated corpus cavernosum. J. Urol. 138:1987;663-666.
27. Walker D.K., Ackland M.J., James G.C., Muirhead G.J., Rance D.J., Wastall P., Wright P.A. Pharmacokinetics and metabolism of sildenafil in mouse, rat, rabbit, dog and man. Xenobiotica. 29:1999;297-310.
28. Wallis R.M., Corbin J.D., Francis S.H., Ellis P. Tissue distribution of phosphodiesterase families and the effects of sildenafil on tissue cyclic nucleotides, platelet function, and the contractile responses of trabeculae carneae and aortic rings in vitro. Am. J. Cardiol. 83:1999;3C-12C.