. 2011 Mar;63(1):1–34. doi: 10.1124/pr.110.003285

TABLE 3.

Adenosine receptor affinities of agonists

Most data for A_2B are from functional studies.

		K_i
		A₁	A_2A	A_2B	A₃
		nM
Nonselective agonists
1	Adenosine^a	∼100 (h)^b	310 (h)^b	15,000 (h)^b	290 (h)^b
		73 (r)^b	150 (r)^b	5100 (r)^b	6500 (r)^b
2	2-Chloro-adenosine	6.7 (r)^c	76 (r)^c	24,000 (h)^d	1890 (r)^e
3	NECA	14 (h)^b	20 (h)^b	140 (h)^b	25 (h)^b
		5.1 (r)^f	9.7 (r)^f	1890 (h)^g	113 (r)^f
				1900 (m)^f
A₁-selective agonists
4	R-PIA	2.04 (h)^h	220 (r)^c	150,000 (h)^d	33 (h)^u
		1.2 (r)^c		19,000 (m)^j	158 (r)^e
5	GW493838	N.D.	N.D.	N.D.	N.D.
6	CHA	0.85 (r)^c	460 (r)^c	160,000 (h)^d	1025 (h)^k
					176 (r)^e
7	CPA	2.3 (h)^l	794 (h)^l	18,600 (h)^l	72 (h)^l
8	CCPA	0.83 (h)^l	2270 (h)^l	18,800 (h)^l	38 (h)^l
		1.3 (r)^m	950 (r)^m		237 (r)^m
		0.1 (rb)^m			37.7 (rb)^m
9	TCPA	2.8 (h)ⁿ	210 (h)ⁿ	>10,000 (h)ⁿ	600 (h)ⁿ
10	2′-Me-CCPA	1.8 (c)^o	3900 (c)^o	N.D.	5000 (r)^o
11	Selodenoson (DTI-0009)	N.D.	N.D.	N.D.	N.D.
12	GR79236	3.1 (r)^l	1300 (h)^l	N.D.	N.D.
13	Tecadenoson	6.5 (p)^l	2315 (h)^l	N.D.	N.D.
14	GS9667 (CVT-3619)	55 (h)^p	>10,000 (h)^p	>50,000 (h)^p	>1000 (h)^p
15	Capadenoson (BAY 68-4986)	N.D.	N.D.	N.D.	N.D.
A_2A-selective agonists
16	CGS21680	289 (h)^l	27 (h)^l	>10,000 (h)^l	67 (h)^l
		1800 (r)^m	19 (r)^m	>10,000 (r)^m	584 (r)^m
		120 (rb)^m			673 (rb)^m
17	Apadenoson (ATL-146e)	77 (h)^l	0.5 (h)^l	N.D.	45 (h)^l
18	ATL-313	N.D.	N.D.	N.D.	N.D.
19	UK-432097	N.D.	4 (h)	N.D.	N.D.
20	Sonedenoson (MRE-0094)	N.D.	N.D.	N.D.	N.D.
21	Binodenoson (WRC-0470)	48,000 (h)^l	270 (h)^l	430,000 (h)^l	903 (h)^l
22	Regadenoson (CV-3146)	>10,000 (h)^l	290 (h)^l	>10,000 (h)^l	>10,000 (h)^l
A_2B-selective agonists
23	A_2B agonist	1050 (h)^q	1550 (h)^q	82 (h)^q	>5000 (h)^q
24	BAY 60-6583	>10,000 (h)^a,r	>10,000 (h)^a,r	3–10 (h)^r	>10,000 (h)^a,r
				330 (m)^s
				750 (d)^s
				340 (rb)^s
A₃-selective agonist
25	IB-MECA (CF101)	51 (h)^l	2900 (h)^l	11,000 (h)^l	1.8 (h)^l
26	Cl-IB-MECA	220 (h)^l	5360 (h)^l	>10,000 (h)^m	1.4 (h)^l
	CF102	280 (r)^m	470 (r)^m	>10,000 (m)^m	0.33 (r)^m
		35 (m)^m	∼10,000 (m)^m		0.18 (m)^m
27	CP608,039	7300 (h)^t	N.D.	N.D.	5.8 (h)^t
		1750 (rb)^t			83 (rb)^t
28	HEMADO	330 (h)^u	1200 (h)^u	>30,000 (h)^u	1.10 (h)^u
29	2-Phenylethynyl-adenosine derivative	32,800 (h)^v	41,700 (h)^v	>30,000 (h)^v	0.44 (h)^v
30	MRS3558 (CF502)	260 (h)^l	2330 (h)^l	>10,000 (h)^l	0.29 (h)^l
		105 (r)^m	1080 (r)^m		1.0 (r)^m
		15.8 (m)^m	10,400 (m)^m		1.49 (m)^m
31	MRS5151	14,900 (h)^w	∼10,000 (h)^w	N.D.	2.38 (h)^w
		10,500 (m)^w	>10,000 (m)^w		24.4 (m)^w

h, human; c, cow; d, dog; m, mouse; p, pig; r, rat; rb, rabbit; R-PIA, (R)-N⁶-phenylisopropyladenosine; N.D., no data available; CHA, N⁶-cyclohexyladenosine; CCPA, 2-chloro-N⁶-cyclopentyladenosine; TCPA, N⁶-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine; ATL-313, 4-{3-[6-amino-9-(5-cyclopropylcarbamoyl-3,4-dihydroxytetrahydrofuran-2-yl)-9H-purin-2-yl]prop-2-y nyl}piperidine-1-carboxylic acid methyl ester; CP608,039, (2S,3S,4R,5R)-3-amino-5-{6-[5-chloro-2-(3-methylisoxazol-5-ylmethoxy)benzylamino]purin-9-yl}-4-hydroxytetrahydrofuran-2-carboxylic acid methylamide; HEMADO, 2-(1-hexynyl)-N-methyladenosine; MRS3558, (1′S,2′R,3′S,4′R,5′S)-4′-{2-chloro-6-[(3-chlorophenylmethyl)amino]purin-9-yl}-1-(methylaminocarbonyl)bicyclo[3.10.0]hexane-2,3-diol; MRS5151, (1′S,2′R,3′S,4′R,5′S)-4′-[6-(3-chlorobenzylamino)-2-(5-hydroxycarbonyl-1-pentynyl)-9-yl]-2′,3′-dihydroxybicyclo[3.10.0]hexane-1′-carboxylic acid N-methylamide.