DY-9760e, a novel calmodulin antagonist, reduces infarction after permanent focal cerebral ischemia in rats

Pharmacology

Volumn 71, Issue 1, 2004, Pages 38-45

  Sato, Toshiyuki ^a   Takamori, Hideo ^a   Shirasaki, Yasufumi ^a  

^a DAIICHI SANKYO CO   (Japan)

Author keywords

Calmodulin; DY 9760e; Infarct volume; Middle cerebral artery occlusion; Permanent focal ischemia; Therapeutic time window

Indexed keywords

3 [2 [4 (3 CHLORO 2 METHYLPHENYL) 1 PIPERAZINYL]ETHYL] 5,6 DIMETHOXY 1 (4 IMIDAZOLYLMETHYL) 1H INDAZOLE; CALCIUM ION; CALMODULIN INHIBITOR; DY 9760E; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BRAIN INFARCTION SIZE; BRAIN ISCHEMIA; BRAIN PROTECTION; CELL PROTECTION; CONTROLLED STUDY; DRUG DOSE REGIMEN; DRUG EFFECT; DRUG EFFICACY; DRUG INDICATION; MALE; MIDDLE CEREBRAL ARTERY OCCLUSION; NEUROPROTECTION; NONHUMAN; PRIORITY JOURNAL; RAT;

ANIMALS; BRAIN ISCHEMIA; CALMODULIN; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG ADMINISTRATION SCHEDULE; DRUG EVALUATION, PRECLINICAL; INDAZOLES; INFARCTION, MIDDLE CEREBRAL ARTERY; INFUSIONS, INTRAVENOUS; JAPAN; MALE; MIDDLE CEREBRAL ARTERY; NEUROPROTECTIVE AGENTS; RATS; RATS, INBRED F344; RECOVERY OF FUNCTION; TIME FACTORS;

EID: 1642619558     PISSN: 00317012     EISSN: None     Source Type: Journal    
DOI: 10.1159/000076260     Document Type: Article

References (48)

1. Choi DW: Glutamate neurotoxicity and diseases of the nervous system. Neuron 1988;1:623-634.
2. Choi DW: Calcium: Still center-stage in hypoxic-ischemic neuronal death. Trends Neurosci 1995;18:58-60.
3. Meldrum B, Garthwaite J: Excitatory amino acid neurotoxicity and neurodegenerative disease. Trends Pharmacol Sci 1990;11:379-387.
4. 2+ elevation induced by in vitro ischemia-like condition in hippocampal slices. Brain Res 1993;601:103-110.
5. James P, Vorherr T, Carafoli E: Calmodulin-binding domains: Just two faced or multifaceted? Trends Biochem Sci 1995;20:38-42.
6. Zhou LW, Moyer JA, Muth EA, Clark B, Palkovits M, Weiss B: Regional distribution of calmodulin activity in rat brain. J Neurochem 1985;44:1657-1662.
7. Picone CM, Grotta JC, Earls R, Strong R, Dedman J: Immunohistochemical determination of calcium-calmodulin binding predicts neuronal damage after global ischemia. J Cereb Blood Flow Metab 1989;9:805-811.
8. Palfi A, Simonka JA, Pataricza M, Tekulics P, Lepran I, Papp G, Gulya K: Postischemic calmodulin gene expression in the rat hippocampus. Life Sci 2001;68:2373-2381.
9. Sun X, Shin C, Windebank AJ: Calmodulin in ischemic neurotoxicity of rat hippocampus in vitro. Neuroreport 1997;8:415-418.
10. Sugimura M, Sato T, Nakayama W, Morishima Y, Fukunaga K, Omitsu M, Miyamoto E, Shirasaki Y: DY-9760e, a novel calmodulin antagonist with cytoprotective action. Eur J Pharmacol 1997;336:99-106.
11. Sato T, Morishima Y, Sugimura M, Uchida T, Shirasaki Y: DY-9760e, a novel calmodulin antagonist, reduces brain damage induced by transient focal cerebral ischemia. Eur J Pharmacol 1999;370:117-123.
12. Sato T, Morishima Y, Shirasaki Y: 3-[2-[4-(3-chloro-2-methylphenyl)-1- piperazinyl]ethyl]-5,6-dimethoxy-1-(4-imidazolylmethyl)-1H-indazole dihydrochloride 3.5 hydrate (DY-9760e), a novel calmodulin antagonist, reduces brain edema through the inhibition of enhanced blood-brain barrier permeability after transient focal ischemia. J Pharmacol Exp Ther 2003;304:1042-1047.
13. Tamura A, Graham DI, McCulloch J, Teasdale GM: Focal cerebral ischaemia in the rat: 1. Description of technique and early neuropathological consequences following middle cerebral artery occlusion. J Cereb Blood Flow Metab 1981;1:53-60.
14. Takagi K, Sato T, Shirasaki Y, Narita K, Tamura A, Sano K: Post-ischemic administration of DY-9760e, a novel calmodulin antagonist, reduced infarct volume in the permanent focal ischemia model of spontaneously hypertensive rat. Neurol Res 2001;23:662-668.
15. Stroke Therapy Academic Industrial Roundtable II (STAIR II): Recommendations for clinical trial evaluation of acute stroke therapies. Stroke 2001;32:1598-1606.
16. Nagafuji T, Matsui T, Koide T, Asano T: Blockade of nitric oxide formation by N([omega])-nitro-L-arginine mitigates ischemic brain edema and subsequent cerebral infarction in rats. Neurosci Lett 1992;147:159-162.
17. Dawson VL, Dawson TM, Bartley DA, Uhl GR, Snyder SH: Mechanisms of nitric oxide-mediated neurotoxicity in primary brain cultures. J Neurosci 1993;13:2651-2661.
18. Buisson A, Margaill I, Callebert J, Plotkine M, Boulu RG: Mechanisms involved in the neuroprotective activity of a nitric oxide synthase inhibitor during focal cerebral ischemia. J Neurochem 1993;61:690-696.
19. Fukunaga K, Ohmitsu M, Miyamoto E, Sato T, Sugimura M, Uchida T, Shirasaki Y: Inhibition of neuronal nitric oxide synthase activity by 3-[2-[4-(3-chloro-2-methylphenyl)-1-piperazinyl] ethyl]-5, 6-dimethoxy-1-(4- imidazolylmethyl)-1H-indazole dihydrochloride 3.5 hydrate (DY-9760e), a novel neuroprotective agent, in vitro and in cultured neuroblastoma cells in situ. Biochem Pharmacol 2000;60:693-699.
20. Sharkey J, Butcher SP: Immunophilins mediate the neuroprotective effects of FK506 in focal cerebral ischaemia. Nature 1994;371:336-339.
21. Ide T, Morikawa E, Kirino T: An immunosuppressant, FK506, protects hippocampal neurons from forebrain ischemia in the Mongolian gerbil. Neurosci Lett 1996;204:157-160.
22. Dawson TM, Steiner JP, Dawson VL, Dinerman JL, Uhl GR, Snyder SH: Immunosuppressant FK506 enhances phosphorylation of nitric oxide synthase and protects against glutamate neurotoxicity. Proc Natl Acad Sci USA 1993;90:9808-9812.
23. Velentza AV, Schumacher AM, Watterson DM: Death associated protein kinase as a potential therapeutic target. Expert Opin Ther Targets 2002;6:497-506.
24. Hajimohammadreza I, Probert AW, Coughenour LL, Borosky SA, Marcoux FW, Boxer PA, Wang KK: A specific inhibitor of calcium/calmodulin-dependent protein kinase-II provides neuroprotection against NMDA-and hypoxia/hypoglycemia- induced cell death. J Neurosci 1995;15:4093-4101.
25. Takano H, Fukushi H, Morishima Y, Shirasaki Y: Calmodulin and calmodulin-dependent kinase II mediate neuronal cell death induced by depolarization. Brain Res 2003;962:41-47.
26. Memezawa H, Smith ML, Siesjo BK: Penumbral tissues salvaged by reperfusion following middle cerebral artery occlusion in rats. Stroke 1992;23:552-559.
27. Fisher M, Takano K: The penumbra, therapeutic time window and acute ischaemic stroke. Baillieres Clin Neurol 1995;4:279-295.
28. Saunders DE, Clifton AG, Brown MM: Measurement of infarct size using MRI predicts prognosis in middle cerebral artery infarction. Stroke 1995;26:2272-2276.
29. Heiss WD, Huber M, Fink GR, Herholz K, Pietrzyk U, Wagner R, Wienhard K: Progressive derangement of periinfarct viable tissue in ischemic stroke. J Cereb Blood Flow Metab 1992;12:193-203.
30. DeGraba TJ, Ostrow PT, Grotta JC: Threshold of calcium disturbances after focal cerebral ischemia in rats. Implications of the window of therapeutic opportunity. Stroke 1993;24:1212-1217.
31. Reith W, Hasegawa Y, Latour LL, Dardzinski BJ, Sotak CH, Fisher M: Multislice diffusion mapping for 3-D evolution of cerebral ischemia in a rat stroke model. Neurology 1995;45:172-177.
32. Takahashi M, Ni JW, Kawasaki-Yatsugi S, Toya T, Ichiki C, Yatsugi SI, Koshiya K, Shimizu-Sasamata M, Yamaguchi T: Neuroprotective efficacy of YM872, an alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptor antagonist, after permanent middle cerebral artery occlusion in rats. J Pharmacol Exp Ther 1998;287:559-566.
33. Graham SH, Chen J, Lan J, Leach MJ, Simon RP: Neuroprotective effects of a use-dependent blocker of voltage-dependent sodium channels, BW619C89, in rat middle cerebral artery occlusion. J Pharmacol Exp Ther 1994;269:854-859.
34. Furuichi Y, Katsuta K, Maeda M, Ueyama N, Moriguchi A, Matsuoka N, Goto T, Yanagihara T: Neuroprotective action of tacrolimus (FK506) in focal and global cerebral ischemia in rodents: Dose dependency, therapeutic time window and long-term efficacy. Brain Res 2003;965:137-145.
35. Hatfield RH, Gill R, Brazell C: The dose-response relationship and therapeutic window for dizocilpine (MK-801) in a rat focal ischaemia model. Eur J Pharmacol 1992;216:1-7.
36. Danton GH, Dietrich WD: Inflammatory mechanisms after ischemia and stroke. J Neuropathol Exp Neurol 2003;62:127-136.
37. Gong C, Qin Z, Betz AL, Liu XH, Yang GY: Cellular localization of tumor necrosis factor alpha following focal cerebral ischemia in mice. Brain Res 1998;801:1-8.
38. Jander S, Schroeter M, Stoll G: Role of NMDA receptor signaling in the regulation of inflammatory gene expression after focal brain ischemia. J Neuroimmunol 2000;109:181-187.
39. Legos JJ, Whitmore RG, Erhardt JA, Parsons AA, Tuma RF, Barone FC: Quantitative changes in interleukin proteins following focal stroke in the rat. Neurosci Lett 2000;282:189-192.
40. Zhu DY, Deng Q, Yao HH, Wang DC, Deng Y, Liu GQ: Inducible nitric oxide synthase expression in the ischemic core and penumbra after transient focal cerebral ischemia in mice. Life Sci 2002;71:1985-1996.
41. 2+/calmodulin. Mol Cell Biol 2003;23:1418-1427.
42. Lilienbaum A, Israel A: From calcium to NF-kappa B signaling pathways in neurons. Mol Cell Biol 2003;23:2680-2698.
43. Qin C, Nguyen T, Stewart J, Samudio I, Burghardt R, Safe S: Estrogen up-regulation of p53 gene expression in MCF-7 breast cancer cells is mediated by calmodulin kinase IV-dependent activation of a nuclear factor kappaB/CCAAT-binding transcription factor-1 complex. Mol Endocrinol 2002;16:1793-1809.
44. Shibasaki F, Hallin U, Uchino H: Calcineurin as a multifunctional regulator. J Biochem (Tokyo) 2002;131:1-15.
45. Sola C, Barron S, Tusell JM, Serratosa J: The Ca2+/calmodulin system in neuronal hyperexcitability. Int J Biochem Cell Biol 2001;33: 439-455.
46. Muthalif MM, Benter IF, Uddin MR, Malik KU: Calcium/calmodulin-dependent protein kinase IIalpha mediates activation of mitogen-activated protein kinase and cytosolic phospholipase A2 in norepinephrine-induced arachidonic acid release in rabbit aortic smooth muscle cells. J Biol Chem 1996;271:30149-30157.
47. Muthalif MM, Hefner Y, Canaan S, Harper J, Zhou H, Parmentier JH, Aebersold R, Gelb MH, Malik KU: Functional interaction of calcium-/calmodulin- dependent protein kinase II and cytosolic phospholipase A(2). J Biol Chem 2001;276:39653-39660.
48. Tachibana S, Fukano A, Sudo K, Tanaka M: Determination of a novel calmodulin antagonist, 3-[2-[4-(3-chloro-2-methylphenyl)-1-piperazinyl] ethyl]-5,6-dimethoxy-1-(4-imidazolylmethyl)-1H-indazole dihydrochloride 3.5 hydrate, DY-9760e, in human plasma using solidphase extraction and high-performance liquid chromatography with fluorescence detection. J Chromatogr B Biomed Sci Appl 1999;734:39-45.