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

EJNMMI Research

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

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

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, f_P = plasma-free fraction, f_ND = brain-free fraction. CD = Sprague Dawley rat and LH = Lister hooded rat.