. 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 1.

Generalized iGluR antagonist compound classes 1–4 and binding affinities of selected antagonists UBP304 (2a), LY466195 (3a), and 4a-e at native AMPA, KA, and NMDA receptors (rat synaptosomes) and cloned homomeric receptors GluK1–3. All values in μM^a



				Native iGluRs			Homomeric GluK receptors^b
	R₁	R₂	R₃	AMPA^a (IC₅₀)	KA^a (IC₅₀)	NMDA^b (K_i)	GluK1 (K_i)	GluK2 (K_i)	GluK3 (K_i)
2a^28,37	--	--	--				0.012	>100	111
3a⁷	--	--	--				0.05	--	8.9
4a³⁶	H	H	H	51	22	6	4.3	>100	8.1
4b³⁸	OH	H	H	2	1.4	1	4.8	10–100	0.87
4c³⁹	Me	H	H	>100	>100	17	>100	>100	>100
4d³⁹	F	H	H	> 100	59	4.6	12	>100	11
4e³⁹	Cl	H	H	>100	>100	0.63	154	>100	131
4f³⁹	Br	H	H	>100	>100	0.62	> 100	> 100	> 100
5a³⁸	H	OH	H	6.3	6.7	4.1	3.7	32	2.1
9a³⁸	H	H	n-Pr	48	22	25	0.62	81	2.2

Radioligands: AMPA, [³H]AMPA; KA, [³H]KA; NMDA, [³H]CGP-39653; GluK1, [³H]NF608; GluK2 and GluK3, [³H]KA.