Table 2.

In vitro data for CB1 antagonists - amides

#	R	Ke hCB1 (nM)	Ki hCB1 (nM)a	Ki hCB2 (nM)a	Selectivity Ki CB2/CB1	MDCK-mdr1 A to B (%)b
29	Me	120
30	CF3	0.4	1	130	130	500
31	n-Bu	0.6	6	400	67	0
32	MeOCH2CH2	72
33	MeCH2OCH2	20	11	>10000	>1000
34	MeSO2CH2CH2	3200
35	t-BuCH2	0.14	2	5000	>2500
36		200
37		410
38		2	2	530	265
39		1800
40		6	5	610	122	0
41	c-PenCH2	0.1	0.4	>10000	>25000
42		19	8	3000	375
43		36
44		34	21	5000	238	5
45		370
46		740
47	Ph(Me)CH	1.5	3	560	190

^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).