Table 1.
Compound | 5-HT2A |
5-HT2B |
5-HT2c |
2C/2A | ||||||
---|---|---|---|---|---|---|---|---|---|---|
Ki (nM) a | pEC50b | Efficacy c | Ki (nM) | pEC50 | Efficacy | Ki (nM) | pEC50 | Efficacy | ||
5-HT2ARs | ||||||||||
TCB-2d | 0.73 | 6.8 | – | – | – | – | – | – | – | – |
MDL11,939e | 2.8 | – | – | 1419 | – | – | 853 | – | – | – |
M100,907f | 1.9e | 8.9 | – | 261e | 6 | – | 88e | 7.7 | – | 0.06 |
5-HT2CRs | ||||||||||
CP-809,101g | 6 | 6.8 | 0.67 | 64 | 7.2 | 0.57 | 1.6 | 10 | 0.93 | 1585 |
Lorcaserinh | 159 | 6.7 | 1 | 190 | 6.0 | 1 | 29 | 7.9 | 1 | 16 |
SB242084f | 851 | 6.8 | – | 45 | 7.0 | – | 7.0 | 9 | – | 158 |
Ki: binding affinity.
pEC50, potency: negative logarithm of the EC50 (half-maximal effective concentration).
Efficacy relative to response to a supramaximal 5-HT concentration.
Modified from (Higgins et al., 2013a).