Effects of a newly developed tricyclic PARP‐1 inhibitor, on ischemic stroke | Zendy

Yoo A. Rum | Zendy; Koh SeongHo | Zendy; Noh Min Young | Zendy; Cho Goang Won | Zendy; Park JiSeon | Zendy; Kim Youngchul | Zendy; Lee HanChang | Zendy; Kim MyungHwa | Zendy; Kim Seung Hyun | Zendy

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Effects of a newly developed tricyclic PARP‐1 inhibitor, on ischemic stroke

Author(s) -

Yoo A. Rum,

Koh SeongHo,

Noh Min Young,

Cho Goang Won,

Park JiSeon,

Kim Youngchul,

Lee HanChang,

Kim MyungHwa,

Kim Seung Hyun

Publication year - 2010

Publication title -

drug development research

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.582

H-Index - 60

eISSN - 1098-2299

pISSN - 0272-4391

DOI - 10.1002/ddr.20368

Subject(s) - poly adp ribose polymerase , tricyclic , stroke (engine) , pharmacology , parp inhibitor , ischemic stroke , medicine , enzyme , ischemia , chemistry , polymerase , biochemistry , mechanical engineering , engineering

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 (IC 50 =7.8 nM in an enzyme‐based assay and=0.73 µM 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. Drug Dev Res 71: 253–260, 2010. © 2010 Wiley‐Liss, Inc.

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