. Author manuscript; available in PMC: 2020 May 9.

Published in final edited form as: J Med Chem. 2019 Apr 18;62(9):4467–4482. doi: 10.1021/acs.jmedchem.8b01986

Table 3.

Binding of 4-hydroxy-1,2,3-triazole Glu analogues to AMPA receptor subtypes.

Ligand	GluA1_o		GluA2(R)_o		GluA3_o		GluA4_o		GluA2_o-ABD
Ligand	K_i (μM)	n_H	K_i (μM)	n_H	K_i (μM)	n_H	K_i (μM)	n_H	K_i (μM)	n_H
(S)-2	0.022	n.d.	0.017	n.d.	0.021	n.d.	0.040	n.d.	n.d.	n.d.
5a	0.0052	n.d.	0.0039	n.d.	0.0022	n.d.	0.0027	n.d.	n.d.	n.d.
5b	7.7	n.d.	0.75	n.d.	0.39	n.d.	0.20	n.d.	n.d.	n.d.
6a	15.7 ± 1.1^#	1.02 ± 0.17	1.87 ± 0.72^#	0.95 ± 0.09	4.98 ± 0.58	0.95 ± 0.25	4.08 ± 1.66	0.89 ± 0.07	n.d.	n.d.
6b	9.02 ± 2.27^##	0.62 ± 0.04	0.71 ± 0.22^**^,##	0.99 ± 0.04	1.91 ± 0.44	0.99 ± 0.03	9.47 ± 1.95	0.72 ± 0.03	0.32 ± 0.03^**	1.01 ± 0.15
6c	54.1 ± 8.6^###	0.81 ± 0.07	3.25 ± 0.47^###	1.55 ± 0.65	11.9 ± 2.9	0.75 ± 0.09	≈ 100	n.d.	n.d.	n.d.
7a	73 ± 34	0.97 ± 0.17	4.38 ± 2.18^*	0.80 ± 0.06	4.89 ± 0.51	0.82 ± 0.05	11.6 ± 2.1	0.91 ± 0.24	1.97 ± 0.17^*	0.92 ± 0.05
7b	> 100	n.d.	> 100	n.d.	≈ 100	n.d.	> 100	n.d.	n.d.	n.d.
7c	> 100	n.d.	> 100	n.d.	> 100	n.d.	> 100	n.d.	n.d.	n.d.

Shown are means ± SEM from n ≥ 3 experiments conducted in triplicate at 12-15 ligand concentrations. n.d., not determined.

GluA2 not statistically significantly different from GluA2-ABD (p > 0.05, t-test).

^**

GluA2 not statistically significantly different from GuA2-ABD (p > 0.05, t-test).

^#,##,###

K_i at GluA1 statistically significantly different from GluA2 (p < 0.05, t-test).