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. 2016 Sep;108:292–304. doi: 10.1016/j.neuropharm.2016.04.016

Table 1.

Selectivity profile of 5-HT2A/2C drugs used in the studyi.

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
a

Ki: binding affinity.

b

pEC50, potency: negative logarithm of the EC50 (half-maximal effective concentration).

c

Efficacy relative to response to a supramaximal 5-HT concentration.

i

Modified from (Higgins et al., 2013a).