Referenced in: none

Automatically associated channels: Kv11.1

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

Authors: Seong Rim Byeon, Hyunjin Vincent Kim, Mijin Jeon, Young Gil Ahn, Maeng Sup Kim, Jae Yang Kong, Hye Yun Kim, Young Soo Kim, Dong Jin Kim

Journal, date & volume: Bioorg. Med. Chem. Lett., 2013 Jun 1 , 23, 3467-9

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/23601707

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-β. 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 μM) results indicated safety of KMS80013.