TABLE 3

Effect of Ketanserin and SB742457 on ¹¹C-GSK215083 BP_ND in Putamen, Caudate, and Frontal Cortex at 5 Hours and 7 Days After Administration

	FRTM BP, ketanserin			FRTM BP, SB-742457		% occupancy
Subject no.	Baseline	5 h	% occupancy, 5 h	5 h	Day 7	5 h	Day 7
Putamen (5HT6)
Subject 5	0.865	0.882	0	0.419	∼	52	∼
Subject 6^*	1.196	0.359	70	0.292	∼	76	∼
Subject 7^*	1.466	0.306	79	0.378	∼	74	∼
Subject 8	1.449	1.355	6	0.437	∼	70	∼
Subject 9	1.020	∼	∼	0.407	0.376	60	63
Subject 10	0.837	∼	∼	0.387	0.430	54	49
Mean			3			64	56
Caudate (5HT6)
Subject 5	0.655	0.594	9	0.226	∼	65	∼
Subject 6^*	0.768	0.190	75	0.160	∼	79	∼
Subject 7^*	0.546	0.075	86	0.098	∼	82	∼
Subject 8	1.839	1.413	23	0.114	∼	94	∼
Subject 9	0.955	∼	∼	0.163	0.198	83	79
Subject 10	0.713	∼	∼	0.005	0.045	99	94
Mean			16			84	87
Frontal cortex (5HT2A)
Subject 5	0.212	0.185	13	0.052	∼	75	∼
Subject 6^*	0.272	Poor fit	∼	0.050	∼	81	∼
Subject 7^*	0.390	0.281	28	0.175	∼	55	∼
Subject 8	0.277	0.178	36	0.145	∼	48	∼
Subject 9	0.202	∼	∼	0.059	0.136	71	33
Subject 10	0.326	∼	∼	0.163	0.249	50	24
Mean			25			63	29

↵* Subjects who received SB742457 before ketanserin.