Table 5.
Affinities of AST-004, 2-methylthioadenosine, or NECA at adenosine receptors determined in radioligand binding studies
Human A3AR | Rat A3AR |
Mouse A3AR |
Human A1AR | Rat A1AR |
Mouse A1AR |
|
---|---|---|---|---|---|---|
Agonist | Ki ± SEM (nM) | |||||
AST-004 | 1490 ± 410 | 10,800 ± 1200 | 4940 ± 974 | 1590 ± 853 | 1880 ± 507 | 3690 ± 877 |
2-Methylthio-adenosineb | 720 ± 280 | - | - | 1900 ± 770 | - | - |
NECA | 6.18 (KD) a | 48.6 (KD)a | 15.1 (KD) a | 14a | 5.1a | 2.49a |
Human A2AAR |
Rat A2AAR |
Mouse A2AAR |
Human A2BAR |
Rat A2BAR |
Mouse A2BAR |
|
---|---|---|---|---|---|---|
Agonist | Ki ± SEM (nM) | |||||
AST-004 | 16,000 ± 6170 | 10,200 ± 1990 | 9040 ± 4290 | > 10,000 | > 10,000 | 10,000 |
2-Methylthio-adenosineb | 11,600 ± 1000 | - | - | > 30,000 | - | - |
NECA | 20a | 9.7a | 43.4a | 1890a | 1110a | 656a |
aData from Alnouri et al. (2015)
bMethods from Gao et al. (2003)