Table 3. Functional Data for New Compounds in Rat and Human 5-HT2A and 5-HT2C and Human 5-HT2B Receptorsa.
| r5-HT2A |
h5-HT2A |
h5-HT2B |
r5-HT2C |
h5HT2C |
||||||
|---|---|---|---|---|---|---|---|---|---|---|
| cmpd | pEC50 (EC50 nM) | Emax % | pEC50 (EC50 nM) | Emax % | pEC50 (EC50 nM) | Emax % | pEC50 (EC50 nM) | Emax % | pEC50 (EC50 nM) | Emax % |
| 5-HT | 8.3 ± 0.04 (5.4) | 100 ± 1.5 | 8.7 ± 0.05 (2.0) | 100 ± 1.6 | 9.31 ± 0.04 (0.49) | 99.9 ± 1.1 | 9.70 ± 0.03 (0.20) | 99.6 ± 0.73 | 9.52 ± 0.08 (0.30) | 98.5 ± 2.4 |
| 1 | 8.0 ± 0.04 (11) | 79.4 ± 1.1 | 8.4 ± 0.05 (4.2) | 86.4 ± 1.4 | 7.81 ± 0.09 (15) | 65 ± 2 | 7.02 ± 0.05 (95) | 104 ± 2 | 7.38 ± 0.12 (41.7) | 92 ± 0 |
| 4a | 7.6 ± 0.04 (27) | 51.7 ± 0.9 | 7.6 ± 0.03 (28) | 71.6 ± 0.9 | 7.4 ± 0.3 (38) | NAb | 6.88 ± 0.06 (133) | 91 ± 3 | 7.47 ± 0.36 (33.8) | 41 ± 6 |
| 4b | 7.3 ± 0.04 (50) | 53.8 ± 0.9 | 7.2 ± 0.03 (60) | 74.1 ± 0.8 | 7.1 ± 0.1 (87) | 38 ± 2 | 6.88 ± 0.05 (132) | 97 ± 2 | 7.36 ± 0.31 (43.2) | 50 ± 7 |
| 4c | 7.4 ± 0.06 (36) | 65.6 ± 1.6 | 7.4 ± 0.04 (42) | 88.0 ± 1.5 | 6.82 ± 0.07 (134) | 83 ± 3 | 6.98 ± 0.02 (105) | 104 ± 1 | 7.24 ± 0.13 (57.6) | 87 ± 5 |
| 4d | 7.8 ± 0.03 (14) | 68.5 ± 0.9 | 7.8 ± 0.04 (17) | 87.5 ± 1.3 | 7.05 ± 0.05 (85) | 90 ± 2 | 7.44 ± 0.05 (36) | 101 ± 2 | 7.28 ± 0.17 (57.6) | 74 ± 5 |
| 4e | 6.8 ± 0.03 (150) | 67.3 ± 0.9 | 6.8 ± 0.03 (170) | 88.0 ± 1.4 | 6.21 ± 0.04 (610) | 90 ± 2 | 6.54 ± 0.04 (290) | 105 ± 2 | 6.66 ± 0.14 (200) | 77 ± 5 |
| 5a | 7.7 ± 0.03 (21) | 80.9 ± 1.1 | 8.7 ± 0.05 (1.9) | 85.2 ± 1.4 | 8.2 ± 0.1 (6.7) | 52 ± 2 | 7.79 ± 0.04 (16) | 102 ± 2 | 7.24 ± 0.12 (57.1) | 119 ± 6 |
| 5b | 7.5 ± 0.04 (34) | 52.2 ± 0.9 | 8.2 ± 0.04 (6.2) | 70.0 ± 1.0 | 6.0 ± 0.4 (949) | NAb | 6.78 ± 0.05 (168) | 102 ± 2 | 6.75 ± 0.15 (178) | 65 ± 5 |
| 5c | 6.7 ± 0.03 (190) | 75.0 ± 1.3 | 7.4 ± 0.04 (42) | 84.1 ± 1.3 | 7.64 ± 0.04 (23) | 81 ± 1 | 7.73 ± 0.04 (19) | 102 ± 2 | 7.12 ± 0.11 (75.1) | 112 ± 5 |
| 5d | 6.3 ± 0.04 (450) | 49.7 ± 1.2 | 7.5 ± 0.05 (30) | 74.7 ± 1.5 | 6.8 ± 0.3 (168) | NAb | 6.05 ± 0.05 (898) | 104 ± 3 | 6.36 ± 0.09 (439) | 94 ± 5 |
| 5e | 6.9 ± 0.03 (130) | 65.5 ± 0.8 | 7.9 ± 0.04 (13) | 73.8 ± 1.1 | 7.5 ± 0.2 (29) | 20 ± 2 | 6.38 ± 0.04 (422) | 112 ± 3 | 6.49 ± 0.23 (321) | 64 ± 8 |
| 5f | 5.8 ± 0.04 (1500) | 77.6 ± 2.4 | 6.4 ± 0.02 (430) | 90.3 ± 1.2 | 6.54 ± 0.05 (290) | 90 ± 2 | 6.69 ± 0.03 (204) | 108 ± 2 | 6.28 ± 0.14 (529) | 83 ± 7 |
| 5g | 7.1 ± 0.04 (80) | 69.1 ± 1.3 | 8.0 ± 0.1 (10) | 89.3 ± 1.1 | 7.42 ± 0.08 (38) | 37 ± 1 | 7.34 ± 0.07 (46) | 100 ± 3 | 6.72 ± 0.13 (192) | 83 ± 5 |
| 5h | 7.1 ± 0.03 (83) | 70.1 ± 1.0 | 7.9 ± 0.04 (14) | 81.2 ± 1.3 | 7.3 ± 0.2 (50) | NAb | 6.54 ± 0.04 (286) | 105 ± 2 | 6.50 ± 0.13 (316) | 85 ± 6 |
| 5i | 6.9 ± 0.04 (120) | 73.4 ± 1.4 | 7.8 ± 0.04 (16) | 79.0 ± 1.1 | 7.4 ± 0.2 (43) | 31 ± 2 | 6.51 ± 0.05 (313) | 110 ± 3 | 6.35 ± 0.09 (445) | 94 ± 5 |
| 5j | 7.6 ± 0.04 (26) | 56.2 ± 0.9 | 8.2 ± 0.04 (6.5) | 73.3 ± 1.0 | NAb | 6.72 ± 0.04 (192) | 104 ± 2 | 6.54 ± 0.10 (289) | 75 ± 4 | |
| 5k | 6.1 ± 0.03 (770) | 69.6 ± 1.4 | 7.1 ± 0.04 (87) | 75.5 ± 1.2 | 6.97 ± 0.07 (107) | 51 ± 2 | 6.79 ± 0.03 (162) | 104 ± 2 | 6.29 ± 0.11 (512) | 75 ± 5 |
| 5l | 6.9 ± 0.05 (120) | 32.0 ± 0.7 | 7.5 ± 0.04 (32) | 46.9 ± 0.8 | NAb | 6.69 ± 0.05 (205) | 101 ± 2 | 6.55 ± 0.11 (283) | 60 ± 4 | |
a
Values are pEC50 ± SEM, with (EC50) values in nM and Emax given in percentage of the maximum response to 5-HT.
b
NA, not active; Emax ≤ 15%.