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Chemical Compound Review

Fasudil     5-(1,4-diazepan-1- ylsulfonyl)isoquinoline

Synonyms: Fasudilum, zlchem 7, Tocris-0541, SureCN4674, CHEMBL38380, ...
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Disease relevance of Fasudil


Psychiatry related information on Fasudil


High impact information on Fasudil


Chemical compound and disease context of Fasudil


Biological context of Fasudil


Anatomical context of Fasudil


Associations of Fasudil with other chemical compounds


Gene context of Fasudil

  • PKN1 kinase activity is not necessary for this translocation, and in fact the PKN inhibitor HA1077 is also shown to induce PKN1 vesicle accumulation [27].
  • Treatment with fasudil suppressed the production and transcription of collagen and TIMP, stimulated the production and transcription of MMP-1, and enhanced collagenase activity [28].
  • Moreover, Rho-kinase inhibitors, Y-27632 and fasudil, suppressed the synthesis of PAI-1 in this culture system [29].
  • Phosphorylation was inhibited by the calmodulin (CaM) inhibitor W-7, but not by the Rho kinase inhibitor HA-1077, i.e. it is exclusively regulated by Ca2+/CaM-dependent MLC kinase [30].
  • Fasudil increased AngII-induced relaxation in SHRSP vessels [31].

Analytical, diagnostic and therapeutic context of Fasudil


  1. Rho-kinase inhibition with intracoronary fasudil prevents myocardial ischemia in patients with coronary microvascular spasm. Mohri, M., Shimokawa, H., Hirakawa, Y., Masumoto, A., Takeshita, A. J. Am. Coll. Cardiol. (2003) [Pubmed]
  2. Involvements of Rho-kinase and TGF-beta pathways in aldosterone-induced renal injury. Sun, G.P., Kohno, M., Guo, P., Nagai, Y., Miyata, K., Fan, Y.Y., Kimura, S., Kiyomoto, H., Ohmori, K., Li, D.T., Abe, Y., Nishiyama, A. J. Am. Soc. Nephrol. (2006) [Pubmed]
  3. Hydroxyfasudil, an active metabolite of fasudil hydrochloride, relaxes the rabbit basilar artery by disinhibition of myosin light chain phosphatase. Nakamura, K., Nishimura, J., Hirano, K., Ibayashi, S., Fujishima, M., Kanaide, H. J. Cereb. Blood Flow Metab. (2001) [Pubmed]
  4. The novel and specific Rho-kinase inhibitor (S)-(+)-2-methyl-1-[(4-methyl-5-isoquinoline)sulfonyl]-homopiperazine as a probing molecule for Rho-kinase-involved pathway. Sasaki, Y., Suzuki, M., Hidaka, H. Pharmacol. Ther. (2002) [Pubmed]
  5. Evaluation of fasudil hydrochloride treatment for wandering symptoms in cerebrovascular dementia with 31P-magnetic resonance spectroscopy and Xe-computed tomography. Kamei, S., Oishi, M., Takasu, T. Clinical neuropharmacology. (1996) [Pubmed]
  6. Chronic administration of an oral rho kinase inhibitor prevents the development of vasculogenic erectile dysfunction in a rat model. Park, K., Kim, S.W., Rhu, K.S., Paick, J.S. The journal of sexual medicine (2006) [Pubmed]
  7. Enhanced myosin light chain phosphorylations as a central mechanism for coronary artery spasm in a swine model with interleukin-1beta. Katsumata, N., Shimokawa, H., Seto, M., Kozai, T., Yamawaki, T., Kuwata, K., Egashira, K., Ikegaki, I., Asano, T., Sasaki, Y., Takeshita, A. Circulation (1997) [Pubmed]
  8. Agonist-induced regulation of myosin phosphatase activity in human platelets through activation of Rho-kinase. Suzuki, Y., Yamamoto, M., Wada, H., Ito, M., Nakano, T., Sasaki, Y., Narumiya, S., Shiku, H., Nishikawa, M. Blood (1999) [Pubmed]
  9. Fasudil, a Rho-kinase inhibitor, attenuates glomerulosclerosis in Dahl salt-sensitive rats. Nishikimi, T., Akimoto, K., Wang, X., Mori, Y., Tadokoro, K., Ishikawa, Y., Shimokawa, H., Ono, H., Matsuoka, H. J. Hypertens. (2004) [Pubmed]
  10. Fasudil prevents KATP channel-induced improvement in postischemic functional recovery. Nishizawa, K., Wolkowicz, P.E., Yamagishi, T., Guo, L.L., Pike, M.M. Am. J. Physiol. Heart Circ. Physiol. (2005) [Pubmed]
  11. Inhibition of Rho-kinase by fasudil attenuated angiotensin II-induced cardiac hypertrophy in apolipoprotein E deficient mice. Wang, Y.X., da Cunha, V., Martin-McNulty, B., Vincelette, J., Li, W., Choy, D.F., Halks-Miller, M., Mahmoudi, M., Schroeder, M., Johns, A., Light, D.R., Dole, W.P. Eur. J. Pharmacol. (2005) [Pubmed]
  12. Effects of isoquinoline derivatives, HA1077 and H-7, on cytosolic Ca2+ level and contraction in vascular smooth muscle. Takizawa, S., Hori, M., Ozaki, H., Karaki, H. Eur. J. Pharmacol. (1993) [Pubmed]
  13. Transforming Growth Factor-{beta}2 and Connective Tissue Growth Factor in Proliferative Vitreoretinal Diseases: Possible Involvement of Hyalocytes and Therapeutic Potential of Rho Kinase Inhibitor. Kita, T., Hata, Y., Kano, K., Miura, M., Nakao, S., Noda, Y., Shimokawa, H., Ishibashi, T. Diabetes (2007) [Pubmed]
  14. Rho-kinase inhibition blunts renal vasoconstriction induced by distinct signaling pathways in vivo. Cavarape, A., Endlich, N., Assaloni, R., Bartoli, E., Steinhausen, M., Parekh, N., Endlich, K. J. Am. Soc. Nephrol. (2003) [Pubmed]
  15. Rho-kinase/ROCK is involved in cytokinesis through the phosphorylation of myosin light chain and not ezrin/radixin/moesin proteins at the cleavage furrow. Kosako, H., Yoshida, T., Matsumura, F., Ishizaki, T., Narumiya, S., Inagaki, M. Oncogene (2000) [Pubmed]
  16. Effect of fasudil on Rho-kinase and nephropathy in subtotally nephrectomized spontaneously hypertensive rats. Kanda, T., Wakino, S., Hayashi, K., Homma, K., Ozawa, Y., Saruta, T. Kidney Int. (2003) [Pubmed]
  17. Protective effect of fasudil, a Rho-kinase inhibitor, on chemokine expression, leukocyte recruitment, and hepatocellular apoptosis in septic liver injury. Thorlacius, K., Slotta, J.E., Laschke, M.W., Wang, Y., Menger, M.D., Jeppsson, B., Thorlacius, H. J. Leukoc. Biol. (2006) [Pubmed]
  18. Phosphorylation of collapsin response mediator protein-2 by Rho-kinase. Evidence for two separate signaling pathways for growth cone collapse. Arimura, N., Inagaki, N., Chihara, K., Ménager, C., Nakamura, N., Amano, M., Iwamatsu, A., Goshima, Y., Kaibuchi, K. J. Biol. Chem. (2000) [Pubmed]
  19. Fluvastatin ameliorates podocyte injury in proteinuric rats via modulation of excessive Rho signaling. Shibata, S., Nagase, M., Fujita, T. J. Am. Soc. Nephrol. (2006) [Pubmed]
  20. Calyculin-A induces focal adhesion assembly and tyrosine phosphorylation of p125(Fak), p130(Cas), and paxillin in Swiss 3T3 cells. Leopoldt, D., Yee, H.F., Rozengurt, E. J. Cell. Physiol. (2001) [Pubmed]
  21. Platelet shape change is mediated by both calcium-dependent and -independent signaling pathways. Role of p160 Rho-associated coiled-coil-containing protein kinase in platelet shape change. Paul, B.Z., Daniel, J.L., Kunapuli, S.P. J. Biol. Chem. (1999) [Pubmed]
  22. Androgens potentiate renal vascular responses to angiotensin II via amplification of the Rho kinase signaling pathway. Song, J., Kost, C.K., Martin, D.S. Cardiovasc. Res. (2006) [Pubmed]
  23. Attenuation of pressure-induced myogenic contraction and tyrosine phosphorylation by fasudil, a cerebral vasodilator, in rat cerebral artery. Masumoto, N., Tanabe, Y., Saito, M., Nakayama, K. Br. J. Pharmacol. (2000) [Pubmed]
  24. Inhibition of HIV-1 Nef-induced apoptosis of uninfected human blood cells by serine/threonine protein kinase inhibitors, fasudil hydrochloride and M3. Okada, H., Takei, R., Tashiro, M. FEBS Lett. (1998) [Pubmed]
  25. Nef protein of HIV-1 induces apoptotic cytolysis of murine lymphoid cells independently of CD95 (Fas) and its suppression by serine/threonine protein kinase inhibitors. Okada, H., Takei, R., Tashiro, M. FEBS Lett. (1997) [Pubmed]
  26. Amelioration of crescentic glomerulonephritis by RhoA kinase inhibitor, Fasudil, through podocyte protection and prevention of leukocyte migration. Hidaka, T., Suzuki, Y., Yamashita, M., Shibata, T., Tanaka, Y., Horikoshi, S., Tomino, Y. Am. J. Pathol. (2008) [Pubmed]
  27. Hyperosmotic-induced protein kinase N 1 activation in a vesicular compartment is dependent upon Rac1 and 3-phosphoinositide-dependent kinase 1. Torbett, N.E., Casamassima, A., Parker, P.J. J. Biol. Chem. (2003) [Pubmed]
  28. Fasudil hydrochloride hydrate, a Rho-kinase (ROCK) inhibitor, suppresses collagen production and enhances collagenase activity in hepatic stellate cells. Fukushima, M., Nakamuta, M., Kohjima, M., Kotoh, K., Enjoji, M., Kobayashi, N., Nawata, H. Liver Int. (2005) [Pubmed]
  29. Inhibition of Rho/Rho-kinase signaling downregulates plasminogen activator inhibitor-1 synthesis in cultured human monocytes. Ishibashi, T., Nagata, K., Ohkawara, H., Sakamoto, T., Yokoyama, K., Shindo, J., Sugimoto, K., Sakurada, S., Takuwa, Y., Teramoto, T., Maruyama, Y. Biochim. Biophys. Acta (2002) [Pubmed]
  30. P2X1-mediated ERK2 activation amplifies the collagen-induced platelet secretion by enhancing myosin light chain kinase activation. Toth-Zsamboki, E., Oury, C., Cornelissen, H., De Vos, R., Vermylen, J., Hoylaerts, M.F. J. Biol. Chem. (2003) [Pubmed]
  31. Negative regulation of RhoA/Rho kinase by angiotensin II type 2 receptor in vascular smooth muscle cells: role in angiotensin II-induced vasodilation in stroke-prone spontaneously hypertensive rats. Savoia, C., Tabet, F., Yao, G., Schiffrin, E.L., Touyz, R.M. J. Hypertens. (2005) [Pubmed]
  32. Involvement of Rho-kinase in cold ischemia-reperfusion injury after liver transplantation in rats. Shiotani, S., Shimada, M., Suehiro, T., Soejima, Y., Yosizumi, T., Shimokawa, H., Maehara, Y. Transplantation (2004) [Pubmed]
  33. Long-term inhibition of Rho kinase suppresses intimal thickening in autologous vein grafts in rabbits. Furuyama, T., Komori, K., Shimokawa, H., Matsumoto, Y., Uwatoku, T., Hirano, K., Maehara, Y. J. Vasc. Surg. (2006) [Pubmed]
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