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. Author manuscript; available in PMC: 2012 May 1.
Published in final edited form as: Bioorg Med Chem Lett. 2010 Dec 1;21(9):2732–2735. doi: 10.1016/j.bmcl.2010.11.104

Table 5.

Key brain penetration and pharmacokinetic parameters.

Cmpds Drug concentration (μM)a Plasma/brain Clp (mL/min/kg)b t½b Oral AUC (μM.h)b %Fb
15 10.4/5.3 9.0 1.3 7.1 73
16 6.6/3.5 0.9 6.5 45 75
20 9.0/10.3 4.2 2.3 10 69
21 3.3/0.74 4.0 3.4 14.9 73
37 9.0/1.4 6.4 1.5 6 51
a

mouse; 10mg/kg IP, 2h

b

rat; 1mg/kg IV; 2mg/kg PO