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