Therapeutic and pharmacokinetic characterizations of an anti-amyloidogenic bis-styrylbenzene derivative for Alzheimer's disease treatment

Title
Therapeutic and pharmacokinetic characterizations of an anti-amyloidogenic bis-styrylbenzene derivative for Alzheimer's disease treatment
Authors
변성림김현진전미진안영길김맹섭공재양김혜연김영수김동진
Keywords
amyloid; Alzheimer's disease; Alzheimer; 치매; 알츠하이머병; 아밀로이드; Aggregation inhibitor; Pharmacokinetics; Behavior test; Amyloid-β
Issue Date
2013-06
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 23, NO 11, 3467-3469
Abstract
Alzheimer’s disease drug discovery regarding exploration into the molecules and processes has focused on the intrinsic causes of the brain disorder correlated with the accumulation of amyloid-b. An anti-amyloidogenic bis-styrylbenzene derivative, KMS80013, showed excellent oral bioavailability (F = 46.2%), facilitated brain penetration (26%, iv) in mouse and target specific in vivo efficacy in acute AD mouse model attenuating the cognitive deficiency in Y-maze test. Acute toxicity (LD50 >2000 mg/kg) and hERG channel inhibition (14% at 10 lM) results indicated safety of KMS80013.
URI
http://pubs.kist.re.kr/handle/201004/46352
ISSN
0960894X
Appears in Collections:
KIST Publication > Article
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