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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 5.

Chemical structures and binding affinities of analogues 9a-e at native iGluRs (rat synaptosomes) and homomeric recombinant iGluRs. All values in μM.a

graphic file with name nihms-1579919-t0033.jpg
Native iGluRs (synaptosomes)b Cloned homomeric iGluRsc
AMPA IC50 KA IC50 NMDA Ki GluK1 Ki GluK2 Ki GluK3 Ki
9a 48 22 25 0.62 82 2.2
9b 69 [4.16 ± 0.02] >100 >100 ∼10 (50 ± 6)d >100 (99 ± 6)d >100 (83 ± 6)d
9c 15 [4.83 ± 0.05] 45 [4.72 ± 0.03] >100 2.98 ± 0.96 >100 (86 ± 6)d 2.46 ± 0.54
9d 35 [4.47 ± 0.007] 13 [4.89 ± 0.3] 61 [4.22 ± 0.03] >10 (60 ± 6)d >100 (93 ± 7)d >10 (57 ± 2)d
9e >100 >100 >100 >100 (93 ± 3)d >100 (97 ± 7)d >100 (95 ± 3)d
a

-,--: Values not determined, Radio ligands 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.