(−)-MBP | Ki antagonist labeled | 20 (4.5) | 13 (5.2) | 12 (2.8) | 26 (2.3) | 11 (2.5) |
Ki agonist labeled | 77 (14) | 199 (35) | 9.1 (0.5) | Not tested | Not tested |
Function | pA2 = 2.64 (0.05) | IC50 = 112 (24) | EC50 = 19 (3) | No activation @ 10 μM | EC50 = 115 (4) |
Efficacy (%) | No activation @ 10 μM | 69 (5) (inverse agonist)b | 63 (13) (agonist)c | No activation @ 10 μM | 60 (1) (agonist)c |
(+)-MBP | Ki antagonist labeled | 332 (42.1) | 31 (7.1) | 200 (24.1) | 534 (63.0) | 969 (77.5) |
Function | EC50 > 1000 | EC50 > 1000 | EC50 > 1000 | EC50 > 1000 | EC50 = 122 (9.0) |
Efficacy (%) | 34 (4) (agonist)c | 42 (6) (agonist)c | 81 (8) (agonist)c | 30 (5) (agonist)c | 57 (10) (agonist)c |