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Table 4 In vitro plasma protein binding and brain tissue binding of GSK1034702

From: An evaluation of the brain distribution of [11C]GSK1034702, a muscarinic-1 (M1) positive allosteric modulator in the living human brain using positron emission tomography

Species Plasma protein binding (%) f P Brain tissue binding (%) f ND
Mouse 48.2 (±1.2) 0.52 86.7 (±0.6) 0.13
Rat (CD) 47.2 (±1.4) 0.53 87.7 (±0.5) 0.12
Rat (LH) 45.5 (±1.5) 0.55 84.9 (±1.0) 0.15
Dog 44.5 (±3.6) 0.56 81.8 (±1.8) 0.18
Monkey 41.7 (±2.7) 0.58 83.2 (±1.1) 0.17
Human 55.8 (±3.6) 0.44 N/A  
  1. Plasma protein binding and brain tissue binding of GSK1034702 evaluated by equilibrium dialysis over 5 h at concentration of 1 μg/mL. Values represent mean ± standard deviation from n = 6 determinations, fP = plasma-free fraction, fND = brain-free fraction. CD = Sprague Dawley rat and LH = Lister hooded rat.