. Author manuscript; available in PMC: 2011 Jan 1.

Published in final edited form as: Exp Eye Res. 2009 Oct 28;90(1):146–154. doi: 10.1016/j.exer.2009.10.001

Table 1.

Potency of a series of agonists and agonist-derived antagonists at the four subtypes of human adenosine receptors.

Action	Drug	Potency, nM				Source (Ref.)
Action	Drug	A₁	A_2A	A_2B	A₃	Source (Ref.)
Nonselective agonist	Adenosine	310	700	24,000	290	(Fredholm et al., 2001)
A₃ agonist	Cl-IB-MECA	222±22	5360 ± 2470	>10,000	1.4 ± 0.3	(Gao et al., 2002; Tchilibon et al., 2005)
A₃ antagonist	MRS 3771	6,220±640	>10,000	>10,000	29.0±4.9	(Gao et al., 2006)
A₃ antagonist	LJ 979	>10,000	>10,000	>10,000	15.5±3.1	(Gao et al., 2006)
A₃ antagonist	MRS 3826	>10,000	>10,000	ND	910±330	(Besada et al., 2006)
A₃ antagonist	MRS 3827	ND	ND	ND	ND	-
A₃ antagonist	LJ 1251	2,490±940	341±75	>10,000	4.16±0.50	(Jeong et al., 2007)

ND: not determined because MRS 3827 is not a pure compound, but a mixture of two isomers (in a 3:2 ratio) of MRS 3771. In MRS 3827, the two free OH groups in MRS3771 were incompletely acetylated. The completely acetylated form is MRS3826.