Table 1.

In vitro data for CB1 antagonists – sulfonamides, carbamates & imines

#	R	Ke hCB1 (nM)	Ki hCB1 (nM)a	Ki hCB2 (nM)a	Selectivity Ki CB2/CB1	MDCK-mdr1 A to B (%)b
2	Otenabantc	0.2	0.7	7700	11000
5	Me	120	3d
9	MeSO2	3	24	1700	68	14
10	EtSO2	17	3	980	330	18
11	i-PrSO2	1	1.4	980	700	11
12	c-PrSO2	17	5	2300	460	4
13	n-PrSO2	2	1.2	850	710	6
14	CF3CH2CH2SO2	15	1.2	500	420
15	i-BuSO2	0.5	2	2800	1400	0
16	n-BuSO2	0.9	0.6	500	830	5
17	MeOCH2CH2SO2	50
18	c-HexCH2SO2	0.6	1.7	91	54
19		4	3	3000	1000	9
20	MeO2C	98
21	t-BuO2C	4	5	3400	680	3
22	MeOCH2CH2O2C	54
23	c-BuO2C	10	3	3400	1100
24		95
25		105
26	c-BuCH2O2C	12	3	4600	1500	0
27	4-F-Ph(HN=)C	4000
28	4-F-PhNH(HN=)C	510				0.4

^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).

^cSee reference [24].

^dSee reference [18].