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.
↵a Data are from functional studies.
↵b Yan et al., 2003.
↵c Daly et al., 1993.
↵d Bruns, 1980.
↵e van Galen et al., 1994.
↵f Müller and Stein, 1996.
↵g Data from radioligand binding studies versus the antagonist radioligand [³H]PSB-603 (S. Hinz and C. E. Müller, unpublished data).
↵h Klotz et al., 1998.
↵u Salvatore et al., 1993.
↵j Brackett and Daly, 1994.
↵k Sajjadi et al., 1996.
↵l Jacobson and Gao, 2006.
↵m Liang et al., 2010.
↵n Beukers et al., 2003.
↵o Franchetti et al., 1998.
↵p Elzein and Zablocki, 2008.
↵q Baraldi et al., 2007.
↵r Kuno et al., 2007.
↵s Data from radioligand binding studies versus the antagonist radioligand [³H]MRS1754 (Auchampach et al., 2009).
↵t Tracey et al., 2003.
↵u Volpini et al., 2002; Klotz et al., 2007.
↵v Volpini et al., 2009.
↵w Melman et al., 2008.