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}	1.3^ⁱ
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	4.7^ⁿ	1.7^ⁿ	2700^ⁿ	1300^ⁿ
(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	0.16^ⁱ	3.4^{^f}	0.014^ⁱ	0.009^ⁱ
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.
↵a Coquelle et al. (2000). (S)-Br-HIBO is active; however, the racemic mixture was used for the determination of EC₅₀.
↵b Donevan et al. (1998).
↵c Banke et al. (1997).
↵d Dawson et al. (1990).
↵e Jin et al. (2002).
↵f Zhang et al. (2006b).
↵g Schiffer et al. (1997).
↵h Nakanishi et al. (1990).
↵i Vogensen et al. (2000).
↵j Holm et al. (2005).
↵k Kizelsztein et al. (2000).
↵l Jin et al. (2003).
↵m Greenwood et al. (2006).
↵n Bjerrum et al. (2003).
↵o Campiani et al. (2001).
↵p Stensbøl et al. (1999).
↵q Strange et al. (2006).
↵r Brehm et al. (2003).
↵s Stensbol et al. (2001).
↵t Jensen et al. (2007).