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 3 Regional V _T , K ₁ values and GSK1034702 injected mass (μg) and [ ¹¹ C]GSK1034702 injected dose in MBq for each scan in the human brain

ROI	Subject 1		Subject 2				Subject 4
	Scan 1 (baseline)		Scan 1 (baseline)		Scan 2 (post dose)		Scan 1(baseline)		Scan 2 (post dose)
	K ₁	V _T	K ₁	V _T	K ₁	V _T	K ₁	V _T	K ₁	V _T
MTL	0.33	7.81	0.19	13.3	0.16	8.30	0.24	7.11	0.25	6.91
Cerebellum	0.23	5.33	0.19	4.75	0.15	3.69	0.19	5.17	0.19	4.56
White matter	0.13	4.63	0.10	4.38	0.08	4.01	0.11	5.04	0.11	4.49
Cortex	0.19	5.37	0.16	5.00	0.12	4.03	0.16	5.57	0.17	4.81
Striatum	0.20	5.59	0.16	5.05	0.13	5.29	0.18	5.83	0.18	4.93
Thalamus	0.29	6.29	0.19	5.44	0.15	4.39	0.20	5.74	0.20	5.11
GSK1034702 injected mass	38.48		34.17		49.35		46.02		44.19
[¹¹C]GSK1034702 injected dose	284.19		322.12		263.02		300.50		325.50

Regions of interest: MTL = medial temporal lobe (ROI defined above), cerebellum, thalamus and striatum and cortex = sum of cortical regions (includes grey and white matter); white matter = all cerebral white matter. K₁ = rate constant for transfer from arterial plasma to tissue (mL.cm⁻³.min⁻¹). V_T = volume of distribution (mL.cm⁻³). GSK1034702 injected mass in microgrammes. [¹¹C]GSK1034702 injected dose in megabecquerel.