Differential vasoactive effects of sildenafil and tadalafil on cerebral arteries

European Journal of Pharmacology

Volumn 674, Issue 2-3, 2012, Pages 345-351

  Kruuse, Christina ^a   Gupta, Saurabh ^a   Nilsson, Elisabeth ^b   Kruse, Lars ^a   Edvinsson, Lars ^a,b  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

^b LUND UNIVERSITY HOSPITAL   (Sweden)

Author keywords

Cerebral artery; Migraine; PDE5; Phosphodiesterase; Sildenafil; Tadalafil

Indexed keywords

5 [2 ETHOXY(MORPHOLINYLACETATE)PHENYL] 1,6 DIHYDRO 1 METHYL 3 PROPYL 7H PYRAZOLO[4,3 D]PYRIMIDIN 7 ONE METHANESULPHANATE; PHOSPHODIESTERASE V; PHOSPHODIESTERASE V INHIBITOR; SILDENAFIL; TADALAFIL; UK 114542; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ANTIHYPERTENSIVE ACTIVITY; ARTERY CONSTRICTION; ARTERY DIAMETER; ARTERY DILATATION; ARTERY TONE; ARTICLE; BRAIN ARTERY; CONCENTRATION RESPONSE; CONTROLLED STUDY; DOSE RESPONSE; DRUG EFFECT; IC 50; IN VITRO STUDY; IN VIVO STUDY; MALE; MIDDLE CEREBRAL ARTERY; MIDDLE MENINGEAL ARTERY; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT; SINGLE DRUG DOSE;

ANIMALS; BLOOD PRESSURE; CARBOLINES; CYCLIC NUCLEOTIDE PHOSPHODIESTERASES, TYPE 5; GENE EXPRESSION REGULATION, ENZYMOLOGIC; MALE; MIDDLE CEREBRAL ARTERY; MORPHOLINES; PHOSPHODIESTERASE 5 INHIBITORS; PIPERAZINES; PURINES; PYRAZOLES; PYRIMIDINES; RATS; RATS, SPRAGUE-DAWLEY; SULFONES; VASODILATOR AGENTS;

EID: 84855551681     PISSN: 00142999     EISSN: 18790712     Source Type: Journal    
DOI: 10.1016/j.ejphar.2011.10.037     Document Type: Article

References (48)

1. Ahern, G.P., Klyachko, V.A., Jackson, M.B., 2002. cGMP and S-nitrosylation: two routes for modulation of neuronal excitability by NO. Trends Neurosci. 25, 510-517. (Pubitemid 35246321)
2. Asghar, M.S., Hansen, A.E., Kapijimpanga, T., van der Geest, R.J., van der Koning, P., Larsson, H.B., Olesen, J., Ashina, M., 2010. Dilation by CGRP of middle meningeal artery and reversal by sumatriptan in normal volunteers. Neurology 75, 1520-1526.
3. Asghar, M.S., Hansen, A.E., Amin, F.M., van der Geest, R.J., Koning, P.V., Larsson, H.B., Olesen, J., Ashina, M., 2011. Evidence for a vascular factor in migraine. Ann. Neurol. 69, 635-645.
4. Atalay, B., Caner, H., Cekinmez, M., Ozen, O., Celasun, B., Altinors, N., 2006. Systemic administration of phosphodiesterase V inhibitor, sildenafil citrate, for attenuation of cerebral vasospasm after experimental subarachnoid hemorrhage. Neurosurgery 59, 1102-1107 discussion 1107-1108.
5. Black, K.L., Yin, D., Ong, J.M., Hu, J., Konda, B.M., Wang, X., Ko, M.K., Bayan, J.A., Sacapano, M.R., Espinoza, A., Irvin, D.K., Shu, Y., 2008. PDE5 inhibitors enhance tumor permeability and efficacy of chemotherapy in a rat brain tumor model. Brain Res. 1230, 290-302.
6. Boolell, M., Allen, M.J., Ballard, S.A., Gepi Attee, S., Muirhead, G.J., Naylor, A.M., Osterloh, I.H., Gingell, C., 1996. Sildenafil: an orally active type 5 cyclic GMP-specific phosphodiesterase inhibitor for the treatment of penile erectile dysfunction. Int. J. Impot. Res. 8, 47-52.
7. Brennan, K.C., Charles, A., 2010. An update on the blood vessel in migraine. Curr. Opin. Neurol. 23, 266-274.
8. Bryan Jr., R.M., Eichler, M.Y., Swafford, M.W., Johnson, T.D., Suresh, M.S., Childres, W.F., 1996. Stimulation of alpha 2 adrenoceptors dilates the rat middle cerebral artery. Anesthesiology 85, 82-90. (Pubitemid 26234698)
9. Corbin, J.D., Francis, S.H., 2002. Pharmacology of phosphodiesterase-5 inhibitors. Int. J. Clin. Pract. 56, 453-459. (Pubitemid 34855305)
10. Curran, M., Keating, G., 2003. Tadalafil. Drugs 63, 2203-2212 discussion 2213-2204.
11. Ghofrani, H.A., Osterloh, I.H., Grimminger, F., 2006. Sildenafil: from angina to erectile dysfunction to pulmonary hypertension and beyond. Nat. Rev. Drug Discov. 5, 689-702. (Pubitemid 44151606)
12. Gokce, C., Gulsen, S., Yilmaz, C., Guven, G., Caner, H., Altinors, N., 2010. The effect of the sildenafil citrate on cerebral vasospasm and apoptosis following experimental subarachnoid hemorrhage in rats. J. Neurosurg. Sci. 54, 29-37.
13. Iversen, H.K., 2001. Human migraine models. Cephalalgia 21, 781-785. (Pubitemid 34621550)
14. Juhl, L., Edvinsson, L., Olesen, J., Jansen-Olesen, I., 2007. Effect of two novel CGRP-binding compounds in a closed cranial window rat model. Eur. J. Pharmacol. 567, 117-124. (Pubitemid 46782825)
15. Kraus, M.M., Prast, H., 2002. Involvement of nitric oxide, cyclic GMP and phosphodiesterase 5 in excitatory amino acid and GABA release in the nucleus accumbens evoked by activation of the hippocampal fimbria. Neuroscience 112, 331-343. (Pubitemid 34607017)
16. Kruse, L.S., Sandholdt, N.T., Gammeltoft, S., Olesen, J., Kruuse, C., 2006. Phosphodiesterase 3 and 5 and cyclic nucleotide-gated ion channel expression in rat trigeminovascular system. Neurosci. Lett. 404, 202-207. (Pubitemid 44041797)
17. Kruse, L.S., Moller, M., Tibaek, M., Gammeltoft, S., Olesen, J., Kruuse, C., 2009. PDE9A, PDE10A, and PDE11A expression in rat trigeminovascular pain signalling system. Brain Res. 1281, 25-34.
18. Kruuse, C., Rybalkin, S.D., Khurana, T.S., Jansen-Olesen, I., Olesen, J., Edvinsson, L., 2001. The role of cGMP hydrolysing phosphodiesterases 1 and 5 in cerebral artery dilatation. Eur. J. Pharmacol. 420, 55-65. (Pubitemid 32539095)
19. Kruuse, C., Thomsen, L.L., Jacobsen, T.B., Olesen, J., 2002. The phosphodiesterase 5 inhibitor sildenafil has no effect on cerebral blood flow or blood velocity, but nevertheless induces headache in healthy subjects. J. Cereb. Blood Flow Metab. 22, 1124-1131. (Pubitemid 35006805)
20. Kruuse, C., Thomsen, L.L., Birk, S., Olesen, J., 2003. Migraine can be induced by sildenafil without changes in middle cerebral artery diameter. Brain 126, 241-247. (Pubitemid 36068573)
21. Kruuse, C., Frandsen, E., Schifter, S., Thomsen, L., Birk, S., Olesen, J., 2004. Plasma levels of cAMP, cGMP and CGRP in sildenafil-induced headache. Cephalalgia 24, 547-553. (Pubitemid 39272955)
22. Kruuse, C., Khurana, T.S., Rybalkin, S.D., Birk, S., Engel, U., Edvinsson, L., Olesen, J., 2005. Phosphodiesterase 5 and effects of sildenafil on cerebral arteries of man and guinea pig. Eur. J. Pharmacol. 521, 105-114. (Pubitemid 41427797)
23. Kruuse, C., Hansen, A.E., Larsson, H.B., Lauritzen, M., Rostrup, E., 2009. Cerebral haemodynamic response or excitability is not affected by sildenafil. J. Cereb. Blood Flow Metab. 29, 830-839.
24. Li, L., Jiang, Q., Zhang, L., Ding, G., Gang Zhang, Z., Li, Q., Ewing, J.R., Lu, M., Panda, S., Ledbetter, K.A., Whitton, P.A., Chopp, M., 2007. Angiogenesis and improved cerebral blood flow in the ischemic boundary area detected by MRI after administration of sildenafil to rats with embolic stroke. Brain Res. 1132, 185-192. (Pubitemid 46096440)
25. Michelakis, E.D., Tymchak, W., Noga, M., Webster, L., Wu, X.C., Lien, D., Wang, S.H., Modry, D., Archer, S.L., 2003. Long-term treatment with oral sildenafil is safe and improves functional capacity and hemodynamics in patients with pulmonary arterial hypertension. Circulation 108, 2066-2069. (Pubitemid 37337580)
26. Moncada, S., Higgs, E.A., 2006. Nitric oxide and the vascular endothelium. Handb. Exp. Pharmacol. 213-254.
27. Nichols, D.J., Muirhead, G.J., Harness, J.A., 2002. Pharmacokinetics of sildenafil after single oral doses in healthy male subjects: absolute bioavailability, food effects and dose proportionality. Br. J. Clin. Pharmacol. 53, 5S-12S.
28. Olesen, J., Burstein, R., Ashina, M., Tfelt-Hansen, P., 2009. Origin of pain in migraine: evidence for peripheral sensitisation. Lancet Neurol. 8, 679-690.
29. Pagani, S., Mirtella, D., Mencarelli, R., Rodriguez, D., Cingolani, M., 2005. Postmortem distribution of sildenafil in histological material. J. Anal. Toxicol. 29, 254-257. (Pubitemid 40827573)
30. Parsons, A.A., Strijbos, P.J., 2003. The neuronal versus vascular hypothesis of migraine and cortical spreading depression. Curr. Opin. Pharmacol. 3, 73-77. (Pubitemid 36131330)
31. Pelligrino, D., Wang, Q., 1998. Cyclic nucleotide crosstalk and the regulation of cerebral vasodilation. Prog. Neurobiol. 56, 1-18. (Pubitemid 28351159)
32. Petersen, K.A., Dyrby, L., Williamson, D., Edvinsson, L., Olesen, J., 2005. Effect of hypotension and carbon dioxide changes in an improved genuine closed cranial window rat model. Cephalalgia 25, 23-29. (Pubitemid 40143789)
33. Rosen, R.C., Kostis, J.B., 2003. Overview of phosphodiesterase 5 inhibition in erectile dysfunction. Am. J. Cardiol. 92, 9M-18M. (Pubitemid 37386271)
34. Royl, G., Balkaya, M., Lehmann, S., Lehnardt, S., Stohlmann, K., Lindauer, U., Endres, M., Dirnagl, U., Meisel, A., 2009. Effects of the PDE5-inhibitor vardenafil in a mouse stroke model. Brain Res. 1265, 148-157.
35. Salom, J.B., Burguete, M.C., Perez-Asensio, F.J., Castello-Ruiz, M., Torregrosa, G., Alborch, E., 2006. Relaxant effect of sildenafil in the rabbit basilar artery. Vascul. Pharmacol. 44, 10-16. (Pubitemid 41796965)
36. Schankin, C.J., Kruse, L.S., Reinisch, V.M., Jungmann, S., Kristensen, J.C., Grau, S., Ferrari, U., Sinicina, I., Goldbrunner, R., Straube, A., Kruuse, C., 2010. Nitric oxide-induced changes in endothelial expression of phosphodiesterases 2, 3, and 5. Headache 50, 431-441.
37. Shimizu-Albergine, M., Rybalkin, S.D., Rybalkina, I.G., Feil, R., Wolfsgruber, W., Hofmann, F., Beavo, J.A., 2003. Individual cerebellar Purkinje cells express different cGMP phosphodiesterases (PDEs): in vivo phosphorylation of cGMP-specific PDE (PDE5) as an indicator of cGMP-dependent protein kinase (PKG) activation. J. Neurosci. 23, 6452-6459. (Pubitemid 36909870)
38. Shin, H.S., Bae, S.K., Lee, M.G., 2006. Pharmacokinetics of sildenafil after intravenous and oral administration in rats: hepatic and intestinal first-pass effects. Int. J. Pharm. 320, 64-70. (Pubitemid 44128707)
39. Silver, B., McCarthy, S., Lu, M., Mitsias, P., Russman, A.N., Katramados, A., Morris, D.C., Lewandowski, C.A., Chopp, M., 2009. Sildenafil treatment of subacute ischemic stroke: a safety study at 25-mg daily for 2 weeks. J. Stroke Cerebrovasc. Dis. 18, 381-383.
40. Stepien, A., Chalimoniuk, M., 1998. Level of nitric oxide-dependent cGMP in patients with migraine. Cephalalgia 18, 631-634. (Pubitemid 29009493)
41. Teixeira, C.E., Priviero, F.B., Webb, R.C., 2006. Differential effects of the phosphodiesterase type 5 inhibitors sildenafil, vardenafil, and tadalafil in rat aorta. J. Pharmacol. Exp. Ther. 316, 654-661. (Pubitemid 43130992)
42. Toque, H.A., Priviero, F.B., Zemse, S.M., Antunes, E., Teixeira, C.E., Webb, R.C., 2009. Effect of the phosphodiesterase 5 inhibitors sildenafil, tadalafil and vardenafil on rat anococcygeus muscle: functional and biochemical aspects. Clin. Exp. Pharmacol. Physiol. 36, 358-366.
43. Wallis, R.M., 1999. The pharmacology of sildenafil, a novel and selective inhibitor of phosphodiesterase (PDE) type 5. Nippon Yakurigaku Zasshi 114 (Suppl. 1), 22P-26P.
44. Wong, D., Dorovini-Zis, K., Vincent, S.R., 2004. Cytokines, nitric oxide, and cGMP modulate the permeability of an in vitro model of the human blood-brain barrier. Exp. Neurol. 190, 446-455. (Pubitemid 39504999)
45. You, J., Johnson, T.D., Childres, W.F., Bryan Jr., R.M., 1997. Endothelial-mediated dilations of rat middle cerebral arteries by ATP and ADP. Am. J. Physiol. 273, H1472-H1477.
46. Zhang, R., Wang, Y., Zhang, L., Zhang, Z., Tsang, W., Lu, M., Chopp, M., 2002. Sildenafil (Viagra) induces neurogenesis and promotes functional recovery after stroke in rats. Stroke 33, 2675-2680. (Pubitemid 35266440)
47. Zhang, L., Zhang, R.L., Wang, Y., Zhang, C., Zhang, Z.G., Meng, H., Chopp, M., 2005. Functional recovery in aged and young rats after embolic stroke. Treatment with a phosphodiesterase type 5 inhibitor. Stroke.
48. Zhang, L., Zhang, Z., Zhang, R.L., Cui, Y., LaPointe, M.C., Silver, B., Chopp, M., 2006. Tadalafil, a long-acting type 5 phosphodiesterase isoenzyme inhibitor, improves neurological functional recovery in a rat model of embolic stroke. Brain Res. 1118, 192-198. (Pubitemid 44633866)