Table 2.
compd | TPSA | Ke CB1 (nM) | Ki CB1 (nM) [3H] CP55940 | Ki CB2 (nM) [3H] CP55940 | CB2/CB1 Ki ratio | MDCK-mdr1 A to B (%)a |
---|---|---|---|---|---|---|
10 | 85 | 3.9 | 7.1 | 13947 | 1959 | <1 |
11 | 73 | 15.9 | 11 | 1657 | 151 | <1 |
12 | 101 | 2.9 | 6.2 | 948 | 153 | <1 |
13a | 88 | 19.2 | 25.5 | 20000 | 784 | <1 |
13b | 88 | 443 | 195 | 4645 | 24 | |
13c | 88 | 46 | 337 | 8946 | 27 | |
13d | 88 | 99 | 220 | 7779 | 35 | |
13e | 88 | 62 | 269 | >20000 | >74 | |
13f | 114 | 171 | ||||
13g | 88 | 199 |
Compound’s permeability was measured from apical to basal (A to B) sides of the membrane.