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Effects of a Newly Developed Tricyclic PARP-1 Inhibitor, on Ischemic Stroke
- Authors
- Yoo, A. Rum; Koh, Seong-Ho; Noh, Min Young; Cho, Goang Won; Park, Ji-Seon; Kim, Youngchul; Lee, Han-Chang; Kim, Myung-Hwa; Kim, Seung Hyun
- Issue Date
- Jun-2010
- Publisher
- John Wiley & Sons Inc.
- Keywords
- PARP; inhibitor; stroke
- Citation
- Drug Development Research, v.71, no.4, pp 253 - 260
- Pages
- 8
- Indexed
- SCI
SCIE
SCOPUS
- Journal Title
- Drug Development Research
- Volume
- 71
- Number
- 4
- Start Page
- 253
- End Page
- 260
- ISSN
- 1098-2299
0272-4391
- Abstract
- Poly(ADP-ribose) polymerase (PARP)-1 plays an important role in the pathogenic mechanism of ischemic stroke. A number of studies have been undertaken to develop PARP-1 inhibitors for clinical use. We report on the newly developed PARP-1 inhibitors, among which 12a showed good activity (IC50) = 7.8 nM in an enzyme-based assay and = 0.73 mu M in a cell-based assay) and pharmacokinetic profiles. Treatment of the middle cerebral artery (MCA) occluded rats with 3 mg/kg 12a reduced infarct volume suggesting that, may be a good candidate for the treatment of ischemic stroke.
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Collections - 서울 의과대학 > 서울 신경과학교실 > 1. Journal Articles
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Related Researcher
- Koh, Seong-Ho
- 서울 의과대학 (DEPARTMENT OF NEUROLOGY)