Table 3.

In vitro data for CB1 antagonists - ureas

#	R	Ke hCB1 (nM)	Ki hCB1 (nM)a	Ki hCB2 (nM)a	Selectivity Ki CB2/CB1	MDCK-mdr1 A to B (%)b
48		66	13
49		670
50	i-BuNH	100
51	c-PenNH	54	5	740	150	3
52		17	24	1300	54
53	c-HexNH	41	1.4	620	440
54		2200
55		4900
56	c-HexCH2NH	35	43	740	17
57		5900
58		3200
59	PhNH	3	6	2400	400	1.0
60		8	6	7100	1200	1.2
61		2	6	1300	220	5.0
62		10	5	3200	640	1.4
63		5	5	4200	840	0
64		2	19	2000	110	0
65		13	4	>10000	>1000	1.1
66		150
67		1000
68		1200
69		420	250

^aDisplacement was measured using [³H]CP55940 in CHO cell membrane preparations overexpressing hCB1 or hCB2 receptors.

^b% transported from the apical side (A) to the basal side (B).