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. 2020 Oct 31;16(4):543–559. doi: 10.1007/s11302-020-09732-z

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)