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. Author manuscript; available in PMC: 2011 Nov 1.
Published in final edited form as: Bioorg Med Chem. 2010 Sep 29;18(21):7548–7564. doi: 10.1016/j.bmc.2010.08.049

Table 2a.

Affinities (Ki=nM) of 3-substituted β-carbolines at αxβ3γ2(x=1–3,5,6) receptor subtypes

graphic file with name nihms243911u2.jpg
Ligands R6 R3 α1 α2 α3 α4 α5 α6
BCCE H CO2Et 1.2 4.9 5.7 1000 26.8 2700
15 H CO2CH2CF3 3.0 24.5 41.7 >500 125.7 >2000
16(WYB09-1) H CO2CH(CF3)2 3.99 8 32 1000 461 2000
17(WYB23-1) H CO2CH2CCl3 10 33 43 1000 189 2000
18(WYB17) H CO2CH(CH3)CCl3 2000 2000 2000 3000 2000 5000
19(CMA64) H CO2CH(CH3)C2H5 18 60 116 NA 216 >2000
20(CMA69) H CO2CH(CF3)C2H5 1000 1000 1000 NA 1000 >2000
25(WY-B-24) graphic file with name nihms243911t14.jpg 22.0 177 44.8 3000 422 3000
26(CM-A-77) graphic file with name nihms243911t15.jpg 33.5 1000 1000 1000 1000 3000

The affinity of compounds at GABAA/BzR recombinant subtypes was measured by competition for [3H]flunitrazepam binding to HEK cell membranes expressing human receptors of composition α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2.119 Data represent the average of at least three determinations with a SEM of ±5%.