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 2 GSK1034702 plasma concentration at start of PET scan and GSK1034702 plasma free fraction ( f _P )

			f _P
	Time between oral dose of GSK1034702 and start of post-dose PET scan (hours)	GSK1034702 plasma concentration at start of post-dose PET scan (ng/mL)	Baseline	Post-dose
Subject 1	-	-	0.42	-
Subject 2	3.2	7.9	0.43	0.41
Subject 3	4.4	13.2	0.43	0.43
Subject 4	3.8	10.4	0.51	0.48
Average			0.45	0.44

The dose for all subjects was 5 mg of GSK1034702. Time given is the time in hours post oral dose of GSK1034702 at which the PET scan acquisition started. GSK1034702 PK concentrations were taken between results from the start of the scan are taken between 4 and 50 min before the PET scan. In vivo plasma-free fractions were measured from plasma samples acquired from the four subjects during each PET scan. f_P = plasma-free fraction.