The selective rho-kinase inhibitor azaindole-1 has long-lasting erectile activity in the rat

Urology

Volumn 81, Issue 2, 2013, Pages 465.e7-465.e14

  Lasker, George F ^a   Pankey, Edward A ^a   Allain, Alexander V ^a   Murthy, Subramanyam N ^a   Stasch, Johannes Peter ^b,c   Kadowitz, Philip J ^a  

^a TULANE UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b BAYER AG   (Germany)

^c MARTIN LUTHER UNIVERSITY HALLE WITTENBERG   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

1H 1,2,4 OXADIAZOLO[4,3 A]QUINOXALIN 1 ONE; 4 (1 AMINOETHYL) N (4 PYRIDYL)CYCLOHEXANECARBOXAMIDE; 7 NITROINDAZOLE; ATROPINE; AZAINDOLE 1; CYCLIC GMP; FASUDIL; GUANYLATE CYCLASE; MUSCARINIC RECEPTOR; NEURONAL NITRIC OXIDE SYNTHASE; NITRIC OXIDE; NITROPRUSSIDE SODIUM; RHO KINASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CAVERNOSAL NERVE CRUSH INJURY; CHOLINERGIC TRANSMISSION; CONTROLLED STUDY; CRUSH TRAUMA; DRUG EFFECT; DRUG MEGADOSE; ENZYME ACTIVATION; INTRACAVERNOUS PRESSURE; MALE; MEAN ARTERIAL PRESSURE; NERVE INJURY; NERVE STIMULATION; NEUROTRANSMISSION; NONADRENERGIC NONCHOLINERGIC NERVE; NONHUMAN; PENIS ERECTION; PRESSURE; PRIORITY JOURNAL; RAT;

EID: 84873309139     PISSN: 00904295     EISSN: 15279995     Source Type: Journal    
DOI: 10.1016/j.urology.2012.10.039     Document Type: Article

References (30)

1. V. Sauzeau, H. Le Jeune, and C. Cario-Toumaniantz Cyclic GMP-dependent protein kinase signaling pathway inhibits RhoA-induced Ca2+ sensitization of contraction in vascular smooth muscle J Biol Chem 275 2000 21722 21729
2. T.M. Mills, K. Chitaley, and C.J. Wingard Effect of Rho-kinase inhibition on vasoconstriction in the penile circulation J Appl Physiol 91 2001 1269 1273
3. T.J. Bivalacqua, H.C. Champion, and M.F. Usta RhoA/Rho-kinase suppresses endothelial nitric oxide synthase in the penis: a mechanism for diabetes-associated erectile dysfunction Proc Natl Acad Sci U S A 101 2004 9121 9126
4. K. Chitaley, C.J. Wingard, and R. Clinton Webb Antagonism of Rho-kinase stimulates rat penile erection via a nitric oxide-independent pathway Nat Med 7 2001 119 122
5. C. Breitenlechner, M. Gassel, and H. Hidaka Protein kinase A in complex with Rho-kinase inhibitors Y-27632, Fasudil, and H-1152P: structural basis of selectivity Structure 11 2003 1595 1607
6. R. Kast, H. Schirok, and S. Figueroa-Perez Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase Br J Pharmacol 152 2007 1070 1080
7. E.A. Pankey, R.J. Byun, and W.B. Smith 2nd The Rho kinase inhibitor azaindole-1 has long-acting vasodilator activity in the pulmonary vascular bed of the intact chest rat Can J Physiol Pharmacol 90 2012 825 835
8. F. Guagnini, M. Ferazzini, and M. Grasso Erectile properties of the Rho-kinase inhibitor SAR407899 in diabetic animals and human isolated corpora cavernosa J Transl Med 10 2012 59
9. C.E. Teixeira, Z. Ying, and R.C. Webb Proerectile effects of the Rho-kinase inhibitor (S)-(+)-2-methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl] homopiperazine (H-1152) in the rat penis J Pharmacol Exp Ther 315 2005 155 162
10. Y. Zhao, P.E. Brandish, and M. DiValentin Inhibition of soluble guanylate cyclase by ODQ Biochemistry 39 2000 10848 10854
11. E.A. Pankey, M. Bhartiya, and A.M. Badejo Jr. Pulmonary and systemic vasodilator responses to the soluble guanylyl cyclase activator, BAY 60-2770, are not dependent on endogenous nitric oxide or reduced heme Am J Physiol Heart Circ Physiol 300 2011 H792 H802
12. G.C. Hsieh, A.B. O'Neill, and R.B. Moreland YC-1 potentiates the nitric oxide/cyclic GMP pathway in corpus cavernosum and facilitates penile erection in rats Eur J Pharmacol 458 2003 183 189
13. J.P. Stasch, P.M. Schmidt, and P.I. Nedvetsky Targeting the heme-oxidized nitric oxide receptor for selective vasodilatation of diseased blood vessels J Clin Invest 116 2006 2552 2561
14. H.H. Schmidt, P.M. Schmidt, and J.P. Stasch NO- and haem-independent soluble guanylate cyclase activators Handb Exp Pharmacol 191 2009 309 339
15. M.E. Sullivan, C.S. Thompson, and M.R. Dashwood Nitric oxide and penile erection: is erectile dysfunction another manifestation of vascular disease? Cardiovasc Res 43 1999 658 665
16. T.J. Bivalacqua, M.F. Usta, and H.C. Champion Endothelial dysfunction in erectile dysfunction: role of the endothelium in erectile physiology and disease J Androl 24 6 suppl 2003 S17 S37
17. K. Park, S.W. Kim, K.S. Rhu, and J.S. Paick Chronic administration of an oral Rho kinase inhibitor prevents the development of vasculogenic erectile dysfunction in a rat model J Sex Med 3 2006 996 1003
18. N. Murat, B.C. Soner, and O. Demir Contractility of diabetic human corpus cavernosum smooth muscle in response to serotonin mediated via Rho-kinase Pharmacology 84 2009 24 28
19. F.B. Priviero, R. Leite, R.C. Webb, and C.E. Teixeira Neurophysiological basis of penile erection Acta Pharmacol Sin 28 2007 751 755
20. J. Rajfer, W.J. Aronson, and P.A. Bush Nitric oxide as a mediator of relaxation of the corpus cavernosum in response to nonadrenergic, noncholinergic neurotransmission N Engl J Med 326 1992 90 94
21. F. Trigo-Rocha, W.J. Aronson, and M. Hohenfellner Nitric oxide and cGMP: mediators of pelvic nerve-stimulated erection in dogs Am J Physiol 264 1993 H419 H422
22. R. Maas, E. Schwedhelm, J. Albsmeier, and R.H. Boger The pathophysiology of erectile dysfunction related to endothelial dysfunction and mediators of vascular function Vasc Med 7 2002 213 225
23. J.Y. Jeremy, S.A. Ballard, and A.M. Naylor Effects of sildenafil, a type-5 cGMP phosphodiesterase inhibitor, and papaverine on cyclic GMP and cyclic AMP levels in the rabbit corpus cavernosum in vitro Br J Urol 79 1997 958 963
24. C. Gratzke, T.D. Strong, and M.A. Gebska Activated RhoA/Rho kinase impairs erectile function after cavernous nerve injury in rats J Urol 184 2010 2197 2204
25. T.J. Bivalacqua, W. Deng, and H.C. Champion Gene therapy techniques for the delivery of endothelial nitric oxide synthase to the corpora cavernosa for erectile dysfunction Methods Mol Biol 279 2004 173 185
26. H. Shimokawa, and A. Takeshita Rho-kinase is an important therapeutic target in cardiovascular medicine Arterioscler Thromb Vasc Biol 25 2005 1767 1775
27. M.F. Usta, T.J. Bivalacqua, and I.T. Koksal The protective effect of aminoguanidine on erectile function in diabetic rats is not related to the timing of treatment BJU Int 94 2004 429 432
28. Y. Rikitake, H.H. Kim, and Z. Huang Inhibition of Rho kinase (ROCK) leads to increased cerebral blood flow and stroke protection Stroke 36 2005 2251 2257
29. M.F. Usta, T.J. Bivalacqua, and Z. Tokatli Stratification of penile vascular pathologies in patients with Peyronie's disease and in men with erectile dysfunction according to age: a comparative study J Urol 172 2004 259 262
30. B.K. Dahal, D. Kosanovic, and P.K. Pamarthi Therapeutic efficacy of azaindole-1 in experimental pulmonary hypertension Eur Respir J 36 2010 808 818