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. Author manuscript; available in PMC: 2021 Mar 4.
Published in final edited form as: ACS Chem Neurosci. 2020 Feb 17;11(5):674–701. doi: 10.1021/acschemneuro.0c00003

Table 2.

Chemical structures and binding affinity data for analogues 4g,h,5b-d,6a,b and 7 at native iGluRs (rat synaptosomes) and homomeric recombinant rat iGluRs. All values in μM.a

graphic file with name nihms-1579919-t0022.jpg
Native iGluRs (synaptosomes)b Cloned homomeric iGluRsc
AMPA IC50 KA IC50 NMDA Ki GluK1 Ki GluK2 Ki GluK3 Ki
4g R1= NH2 >100 >100 >100 (70 ± 16)d (77 ± 5)d (64 ± 4)d
4h R1= CO2H >100 >100 1.3 [5.88 ± 0.06] >100 >100 >100
7 -- >100 >100 8.5 >100 >100 >100
5b R2= Br 26 [4.60 ± 0.04] 10 [4.99 ± 0.04] 2.4 [5.63 ±0.05] 5.88 ± 0.60 >100 2.42 ± 0.11
5c R2= CO2H 36 [4.45 ± 0.04] 63 [4.21 ± 0.05] 0.48 [6.32 ± 0.03] 12.5 ± 1.7 >100 15.7 ± 3.1
5d R2= triazole 21 [4.69 ±0.04] 20 [4.71±0.06] 0.83 [6.08±0.05] >50 >100 10–50
6a R2= Br >100 >100 1–10 ≥100 ≥100 ≥100
6b R2= CO2H >100 >100 0.16 [6.82 ± 0.08] ≥100 ≥100 >50
a

-,--: Values not determined, Radioligands used: AMPA, [3H]AMPA; KA, [3H]KA; [3H]CGP-39653; GluK1, [3H]NF608; GluK2 and GluK3, [3H]KA

b

Data are mean values of three to six individual experiments performed in triplicate. For AMPA and KA: pIC50 values with SEM in brackets. For NMDA: pKi values with SEM in brackets.

c

Mean values ± SEM of at least three experiments conducted in triplicate at 12–16 drug concentrations.

d

% specific binding mean values ± SD of three experiments at 10 μM ligand concentration.