Table 1.

Ligand binding affinity at adenosine receptors.

K_i, nM (or % inhibition at 10 µM)

	A1AR	Mouse A2AAR	A3AR	A1AR	Human A2AAR	A3AR
Agonists
IB-MECAa,b	5.9	~1000	0.087	51	2900	1.8
Cl-IB-MECAa,b	35	~10,000	0.18	220	5400	1.4
MRS5474c,d	3.20±0.05	34±9%	1056±251	50	3950	470
MRS5698e,e	14%	27%	3.1	6%	41%	3.5
MRS5841f,f	15%	1%	11	16%	7%	1.9
MRS5980g,g	38%	7%	36	6%	24%	0.70
CCPAh,i	0.27	988	16	0.83	2270	43
CPAc,i	0.22±0.01	808±89	534±14	2.3	794	43
CHAc,j	2.15±0.37	1695±60	611±12	2.4	1390	73
SPAc,c	1.08±0.04	33±2%	3111±183	7.92±1.55	3778±890	246±21
Cl-ENBAc,k	0.20±0.01	3985±358	2414±325	0.51	1340	1290
CGS21680c,i	193±38	10±2	48±11	289	27	67
Antagonists
MRS1523n,l	5,330	0%	702	>10,000	3660	19
MRS1191c,l	0%	0%	32±3%	>10,000	>10,000	31
SCH442416c,m	765±36	1.27±0.04	6±2%	35%	4.1	67%
DPCPXn,i	1.5	598	0%	3.9	129	3960

Bold indicates a K_i ≥100-fold lower than the other two receptors of the same species. Superscripts indicate the references for literature data (mouse, human). SEMs are included for experimental results.

^a(Ge et al, 2006)

^b(Tchilibon et al, 2005)

^ccurrent results

^d(Tosh et al, 2012b)

^e(Tosh et al, 2012a)

^f(Paoletta et al, 2013)

^g(Tosh et al, 2014)

^h(Alnouri et al, 2015)

ⁱ(Klotz et al, 1998)

^j(Ferkany et al, 1986; Gao et al, 2003; Stone et al, 1988)

^k(Franchetti et al, 2009)

^l(Liang et al, 2010)

^m(Kumar et al, 2011)

ⁿ(Kreckler et al, 2006)