General Description
A cell-permeable, potent, fast-acting, and selective inhibitor of prolyl oligopeptidase (PREP) (K
i = 23 pM). Reported to cross the blood-brain barrier. Inhibits about 85% PREP activity within 10 minutes of administration and exhibits a half-life of about 4.8 hours. Exhibits higher lipophilicity that increases its penetration across biological membranes
in vivo. Maximum plasma and brain levels are achieved within 10 minutes following its
i.p. administration. Shown to block oxidative-stress induced α-synuclein aggregation and clearance in cellular and animal models of Parkinson′s disease. Also shown to improve cognitive performance in young rats (1-5 mg/kg) in a dose-dependent manner.
