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Chemical Compound Review

Cilostamida     N-cyclohexyl-N-methyl-4-[(2- oxo-1H...

Synonyms: ciloalamide, cilostamide, Cilostamidum, Lopac-C-7971, Tocris-0915, ...
 
 
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Disease relevance of Tocris-0915

  • These results indicate that cilostamide suppresses intimal hyperplasia both in the single- and double-injury models of rat, presumably by inhibiting proliferation rather than migration of VSMC [1].
  • The inhibitory potential of novel anti-platelet aggregatory cilostamide analogues on phosphodiesterase (PDE) isozyme activities was investigated with recombinant PDE isozymes expressed in a baculovirus/ Sf9 expression system [2].
 

High impact information on Tocris-0915

  • Incubation of intact rat fat cells with maximally effective concentrations of insulin (1 nM, 12 min) or isoprenaline (300 nM, 3 min) increased particulate cGMP- and cilostamide-inhibited, low-Km cAMP phosphodiesterase (cAMP-PDE) activity by about 50% and 100%, respectively [3].
  • Cilostamide, a PDE3-selective compound, did not affect either the antimigratory activity of forskolin or its ability to increase cAMP [4].
  • In F/B cells, IGF-1-induced phosphorylation of the apoptotic protein BAD was inhibited by the PDE3 inhibitor cilostamide [5].
  • As previously reported for insulin, induction of GVBD by Akt was prevented by incubating the oocytes with cilostamide, an inhibitor specific for the type 3 phosphodiesterase (PDE3), suggesting that the activity of a PDE is required for Akt action [6].
  • Specific PDE3 (cilostamide) and PDE4 (rolipram) inhibitors suppressed [3H]thymidine incorporation in TCC [7].
 

Biological context of Tocris-0915

 

Anatomical context of Tocris-0915

 

Associations of Tocris-0915 with other chemical compounds

 

Gene context of Tocris-0915

  • Indeed, PDE3 inhibitor cilostamide caused potentiation of 8-bromo-cAMP-elicited elevations of Cx43 expression that is similar to the effect of SNAP, and an elevation of intracellular cAMP was detected in SNAP-treated cells [19].
  • Selective inhibition of PDE3 by cilostamide and PDE4 by Ro 20-1724 potentiated beta1-AR cAMP signals, whereas Glu-R cAMP was augmented only by PD4 inhibition [20].
  • Suppression of arterial intimal hyperplasia by cilostamide, a cyclic nucleotide phosphodiesterase 3 inhibitor, in a rat balloon double-injury model [1].
  • Cilostamide treatment resulted in a marginal increase in the 50,000 mol. wt phosphorylation at concentrations (10-100 nM) which completely inhibited the STA2-induced aggregation [10].
  • Neither FSH, EGF nor FF-MAS caused any change in the meiotic status of CEO when meiotic arrest at the germinal vesicle (GV) stage was maintained by cilostamide [21].
 

Analytical, diagnostic and therapeutic context of Tocris-0915

References

  1. Suppression of arterial intimal hyperplasia by cilostamide, a cyclic nucleotide phosphodiesterase 3 inhibitor, in a rat balloon double-injury model. Inoue, Y., Toga, K., Sudo, T., Tachibana, K., Tochizawa, S., Kimura, Y., Yoshida, Y., Hidaka, H. Br. J. Pharmacol. (2000) [Pubmed]
  2. Potent effects of novel anti-platelet aggregatory cilostamide analogues on recombinant cyclic nucleotide phosphodiesterase isozyme activity. Sudo, T., Tachibana, K., Toga, K., Tochizawa, S., Inoue, Y., Kimura, Y., Hidaka, H. Biochem. Pharmacol. (2000) [Pubmed]
  3. Evidence that insulin and isoprenaline activate the cGMP-inhibited low-Km cAMP phosphodiesterase in rat fat cells by phosphorylation. Degerman, E., Smith, C.J., Tornqvist, H., Vasta, V., Belfrage, P., Manganiello, V.C. Proc. Natl. Acad. Sci. U.S.A. (1990) [Pubmed]
  4. Synergistic inhibition of vascular smooth muscle cell migration by phosphodiesterase 3 and phosphodiesterase 4 inhibitors. Palmer, D., Tsoi, K., Maurice, D.H. Circ. Res. (1998) [Pubmed]
  5. Cyclic nucleotide phosphodiesterase 3B is a downstream target of protein kinase B and may be involved in regulation of effects of protein kinase B on thymidine incorporation in FDCP2 cells. Ahmad, F., Cong, L.N., Stenson Holst, L., Wang, L.M., Rahn Landstrom, T., Pierce, J.H., Quon, M.J., Degerman, E., Manganiello, V.C. J. Immunol. (2000) [Pubmed]
  6. Protein kinase B/Akt induces resumption of meiosis in Xenopus oocytes. Andersen, C.B., Roth, R.A., Conti, M. J. Biol. Chem. (1998) [Pubmed]
  7. Differential expression of cyclic nucleotide phosphodiesterase 3 and 4 activities in human T cell clones specific for myelin basic protein. Ekholm, D., Hemmer, B., Gao, G., Vergelli, M., Martin, R., Manganiello, V. J. Immunol. (1997) [Pubmed]
  8. Complex effects of inhibitors on cyclic GMP-stimulated cyclic nucleotide phosphodiesterase. Yamamoto, T., Yamamoto, S., Osborne, J.C., Manganiello, V.C., Vaughan, M., Hidaka, H. J. Biol. Chem. (1983) [Pubmed]
  9. Antilipolytic action of insulin: role of cAMP phosphodiesterase activation. Elks, M.L., Manganiello, V.C. Endocrinology (1985) [Pubmed]
  10. Inhibition of platelet aggregation by the cAMP-phosphodiesterase inhibitor, cilostamide, may not be associated with activation of cAMP-dependent protein kinase. Nishikawa, M., Komada, F., Morita, K., Deguchi, K., Shirakawa, S. Cell. Signal. (1992) [Pubmed]
  11. Effect of type 3 and type 4 phosphodiesterase inhibitors on the maintenance of bovine oocytes in meiotic arrest. Mayes, M.A., Sirard, M.A. Biol. Reprod. (2002) [Pubmed]
  12. Inhibition of lipopolysaccharide-induced apoptosis by cilostazol in human umbilical vein endothelial cells. Kim, K.Y., Shin, H.K., Choi, J.M., Hong, K.W. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
  13. Purification of the putative hormone-sensitive cyclic AMP phosphodiesterase from rat adipose tissue using a derivative of cilostamide as a novel affinity ligand. Degerman, E., Belfrage, P., Newman, A.H., Rice, K.C., Manganiello, V.C. J. Biol. Chem. (1987) [Pubmed]
  14. Compartmentalization of cAMP signaling in mesangial cells by phosphodiesterase isozymes PDE3 and PDE4. Regulation of superoxidation and mitogenesis. Chini, C.C., Grande, J.P., Chini, E.N., Dousa, T.P. J. Biol. Chem. (1997) [Pubmed]
  15. Characterization of a liver low Michaelis-Menten constant 3',5'-cyclic adenosine monophosphate phosphodiesterase activity sensitive to thyroid status. Benelli, C., Geoffroy, V., Fouque, F., Lopez, S., Desbuquois, B. Endocrinology (1991) [Pubmed]
  16. Selective effects of phosphodiesterase inhibitors on different phosphodiesterases, adenosine 3',5'-monophosphate metabolism, and lipolysis in 3T3-L1 adipocytes. Elks, M.L., Manganiello, V.C. Endocrinology (1984) [Pubmed]
  17. Alterations in EDHF-type relaxation and phosphodiesterase activity in mesenteric arteries from diabetic rats. Matsumoto, T., Kobayashi, T., Kamata, K. Am. J. Physiol. Heart Circ. Physiol. (2003) [Pubmed]
  18. Selective inhibitor of platelet cyclic adenosine monophosphate phosphodiesterase, cilostamide, inhibits platelet aggregation. Hidaka, H., Hayashi, H., Kohri, H., Kimura, Y., Hosokawa, T., Igawa, T., Saitoh, Y. J. Pharmacol. Exp. Ther. (1979) [Pubmed]
  19. Nitric oxide-mediated regulation of connexin43 expression and gap junctional intercellular communication in mesangial cells. Yao, J., Hiramatsu, N., Zhu, Y., Morioka, T., Takeda, M., Oite, T., Kitamura, M. J. Am. Soc. Nephrol. (2005) [Pubmed]
  20. A specific pattern of phosphodiesterases controls the cAMP signals generated by different Gs-coupled receptors in adult rat ventricular myocytes. Rochais, F., Abi-Gerges, A., Horner, K., Lefebvre, F., Cooper, D.M., Conti, M., Fischmeister, R., Vandecasteele, G. Circ. Res. (2006) [Pubmed]
  21. Mouse oocyte meiotic resumption and polar body extrusion in vitro are differentially influenced by FSH, epidermal growth factor and meiosis-activating sterol. Coticchio, G., Rossi, G., Borini, A., Grøndahl, C., Macchiarelli, G., Flamigni, C., Fleming, S., Cecconi, S. Hum. Reprod. (2004) [Pubmed]
  22. Selective inhibition of cGMP-inhibited and cGMP-noninhibited cyclic nucleotide phosphodiesterases and relaxation of rat aorta. Lindgren, S., Rascón, A., Andersson, K.E., Manganiello, V., Degerman, E. Biochem. Pharmacol. (1991) [Pubmed]
  23. Activation of a cGMP-stimulated cAMP phosphodiesterase by protein kinase C in a liver Golgi-endosomal fraction. Geoffroy, V., Fouque, F., Nivet, V., Clot, J.P., Lugnier, C., Desbuquois, B., Benelli, C. Eur. J. Biochem. (1999) [Pubmed]
  24. Phosphodiesterase 3 inhibitors selectively block the spontaneous resumption of meiosis by macaque oocytes in vitro. Jensen, J.T., Schwinof, K.M., Zelinski-Wooten, M.B., Conti, M., DePaolo, L.V., Stouffer, R.L. Hum. Reprod. (2002) [Pubmed]
  25. Expression of cyclic nucleotide phosphodiesterase 3A in isolated rat submandibular acini. Shimizu, K., Murata, T., Hiramoto, K., Sugiyama, T., Nakagawa, T., Manganiello, V.C., Tagawa, T. Arch. Oral Biol. (2006) [Pubmed]
 
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