. 2010 Sep;62(3):405–496. doi: 10.1124/pr.109.002451

TABLE 5.

AMPA receptor agonist EC₅₀ values in micromolar

EC₅₀ values for GluA1, GluA3, or GluA4 coexpressed with GluA2 can be found in Stein et al. (1992), Coquelle et al. (2000), Nakanishi et al. (1990), and Vogensen et al. (2000).

Agonist	GluA1	GluA2	GluA3	GluA4
	μM
l-Glutamate	3.4–22^a–d	6.2–296^a,e,f	1.3–35^a–c	560^g
AMPA	1.3–8.7^c,h,i	66^f	1.4–130^c,h,i	1.3ⁱ
Kainate	32–34^d,h	130–170^j	31–36^c,h
Willardiine	11.5^k	6.3^l
F-Willardiine	0.47^k	0.2–0.5^l,m	20.9^m	11.9^m
Br-Willardiine	2.8^k	0.84^l
I-Willardiine	33.6^k	1.5^l
Br-HIBO	14^a	5.4^a	202^a	39^a
Cl-HIBO	4.7ⁿ	1.7ⁿ	2700ⁿ	1300ⁿ
(S)-CPW399	24.9^o	13.9^o	224^o	34.3^o
(S)-ATPA	22^p		7.9^p	7.6^p
ACPA	1.1–11^c,q	15^q	0.1–5^c,q	1.1^q
(S)-4-AHCP	4.5^r		7.2^r	15^r
(S)-Thio-ATPA	5.2^s	13–40^s	32^s	20^s
2-Et-Tet-AMPA	42^t	52^t	18^t	4^t
(S)-2-Me-Tet-AMPA	0.16ⁱ	3.4^f	0.014ⁱ	0.009ⁱ
SYM2081	132^b		453^b
Domoic Acid	1.3^d 0.97^b		21^b

ACPA, (R,S)-2-amino-3-(3-carboxy-5-methyl-4-isoxazolyl)propionic acid; (S)-4-AHCP, (R,S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid; 2-Et-Tet-AMPA, (R,S)-2-amino-3-[3-hydroxy-5-(2-ethyl-2H-5-tetrazolyl)-4-isoxazolyl]propionic acid; (S)-2-Me-Tet-AMPA, (S)-2-amino-3-[3-hydroxy-5-(2-methyl-2H-tetrazol-5-yl)isoxazol-4-yl]propionic acid; (S)-ATPA, (S)-2-amino-3-(5-tert-butyl-3-hydroxyisoxazol-4-yl)propionic acid; (S)-thio-ATPA, (S)-2-amino-3-(5-tert-butyl-3-hydroxy-4-isothiazolyl)propionic acid; (S)-CPW399, (S)-1-(2-amino-2-carboxyethyl)-6,7-dihydro-1H-cyclopentapyrimidine-2,4(1H,3H)dione; Br-HIBO, (R,S)-4-bromo-HIBO; Cl-HIBO, (R,S)-4-chloro-HIBO.