TABLE 4

Adenosine receptor affinities of antagonists

A few A_2B data are from functional (cAMP) studies.

		K_i
		A₁	A_2A	A_2B	A₃
		nM
Nonselective antagonists
32	Caffeine	10,700 (h)^{^a}	23,400 (h)^{^b}	33,800 (h)^{^c}	13,300 (h)^{^a}
		44,900 (h)^{^b}	9560 (h)^{^a}	10,400 (h)^{^d}	>100,000 (r)^{^e}
		41,000 (r)^{^f}	45,000 (r)^{^g}	20,500 (h)^{^h}
		44,000 (r)^{^g}	32,500 (r)^{^u}	30,000 (r)^{^j}
		47,000 (gp)^{^k}	48,000 (r)^{^a}	13,000 (m)^{^j}
		44,000 (c)^{^k}
33	Theophylline	6770 (h)^{^l}	1710 (h)^{^l}	9070 (h)^{^d}	22,300 (h)^{^a}
		14,000 (r)^{^m}	6700 (h)^{^a}	74,000 (h)^{^h} 15,100 (r)^{^d}	86,400 (h)^{^l}
		8740 (r)^{^a}	22,000 (r)^{^m}	5630 (m)^ⁿ	>100,000 (r)^{^e}
		7060 (gp)^{^o}	25,300 (r)^{^a}	11,000 (gp)^{^p}	85,000 (r)^{^q}
		4710 (rb)^{^o}		17,700 (rb)^ⁿ	>100,000 (d)^{^r}
		9050 (s)^{^o}		38,700 (d)^ⁿ
		6330 (c)^{^o}
34	CGS15943	3.5 (h)^{^s}	1.2 (h)^{^s}	32.4 (h)^ⁿ	35 (h)^{^s}
		6.4 (r)^{^s}		9.07 (m)^ⁿ
A₁-selective antagonists
35	DPCPX (CPX)	3.0 (h)^{^t}	129 (h)^{^l}	51 (h)^{^t}	795 (h)^{^u}
		0.50 (r)^{^t}	60 (h)^{^t}	63.8 (h)^{^d}	243 (h)^{^t}
		1.0 (r)^{^d}	157 (r)^{^u}	186 (r)^{^d}	509 (h)^{^r}
		0.18 (r)^{^o}	500 (r)^{^d}	200 (r)^{^p}	3960 (h)^{^l}
		1.06 (gp)^{^o}		86.2 (m)^ⁿ	>10,000 (r)^{^t}
		3.9 (gp)^{^k}		145 (gp)^{^p}	43,000 (r)^{^r}
		0.21 (rb)^{^o}		96.0 (rb)^ⁿ	708 (rb)^{^r}
		0.10 (s)^{^o}		147 (d)^ⁿ	115 (d)^{^c}
		0.05 (c)^{^o}		132 (d)^{^p}
		0.29 (c)^{^k}
		11.4 (d)^{^r}
36	CPFPX	1.26 (h)^{^v}	940 (h)^{^v}	nd^{^b}	N.D.
		0.63 (r)^{^v}	812 (r)^{^v}
		1.37(p)^{^v}
		0.18 (c)^{^v}
37	Rolofylline (KW-3902, NAX)	0.72 (h)^{^w}	108 (h)^{^w}	296 (h)^{^x}	4390 (h)^{^x}
		8.0 (h)^{^x}	673 (h)^{^x}
		0.19 (r)^{^y}	380 (r)^{^y}
		12.6 (r)^{^w}	510 (r)^{^w}
38	PSB-36	0.7 (h)^{^t}	980 (h)^{^t}	187 (h)^{^t}	2300 (h)^{^t}
		0.124 (r)^{^t}	552 (r)^{^t}		6500 (r)^{^t}
39	Toponafylline (BG-9928)	7.4 (h)^{^x}	6410 (h)^{^x}	90 (h)^{^x}	>10,000 (h)^{^x}
		3.9 (mk)^{^z}	943 (mk)^{^z}
		1.3 (r)^{^x}	2440 (r)^{^x}
		29 (d)^{^z}	4307 (d)^{^z}
40	FK-453	18 (h)^{^aa}	1300 (h)^{^aa}	980 (h)^{^aa}	>10,000 (h)^{^aa}
41	SLV320	1.00 (h)^{^bb}	398 (h)^{^bb}	3981 (h)^{^bb}	200 (h)^{^bb}
		2.51 (r)^{^bb}		501 (r)^{^bb}
42	LUF5981	0.90 (h)^{^cc}	194 (h)^{^cc}	>300 (h)^{^cc}	637 (h)^{^cc}
A_2A-selective antagonists
43	Istradefylline (KW6002)	841 (h)^{^dd}	12 (h)^{^ee}	>10,000 (h)^{^dd}	4470 (h)^{^dd}
		230 (r)^{^dd}	91.2 (h)^{^dd}
			2.2 (r)^{^ff}
			4.46 (r)^{^gg}
44	CSC (K_i MAO-B = 80.6 nM)^{^gg}	28,000 (r)^{^hh}	54 (r)^{^hh}	8200^ⁱⁱ	>10,000 (r)^{^e}
45	MSX-2	900 (r)^{^jj}	8.04 (r)^{^u}^,^{^jj}	>10,000 (h)^{^jj}	>10,000 (h)^{^jj}
		2500 (h)^{^jj}	5.38 (h)^{^jj}^,^{^kk}	2900 (h)^{^ll}
			14.5 (h)^{^jj}^,^{^mm}
46	SYN-115	N.D.	N.D.	N.D.	N.D.
47	BIIB014 (V2006)	68 (h)^ⁿⁿ	1.3 (h)^ⁿⁿ	63 (h)^ⁿⁿ	1005 (h)^ⁿⁿ
48	ZM-241385	774 (h)^{^aa}	1.6 (h)^{^aa}	75 (h)^{^aa}	743 (h)^{^aa}
49	ST-1535	71.8 (h)^{^oo}	6.6 (h)^{^oo}	352.3 (h)^{^oo}	>1000 (h)^{^oo}
50	SCH-58261	725 (h)^{^aa}	5.0 (h)^{^aa}	1110 (h)^{^aa}	1200 (h)^{^aa}
51	Preladenant (SCH-420814)	>1000 (h)^{^pp}	0.9 (h)^{^pp}	>1000 (h)^{^pp}	>1000 (h)^{^pp}
52	SCH-442416	1110 (h)^{^aa}	4.1 (h)^{^qq}	>10,000 (h)^{^aa}	>10,000 (h)^{^aa}
A_2B-selective antagonists
53	MRS1754	403 (h)^{^rr}	503 (h)^{^rr}	1.97 (h)^{^rr}	570 (h)^{^rr}
		16.8 (r)^{^rr}	612 (r)^{^rr}	12.8 (r)^{^rr}
				16.6 (r)^{^p}
				3.39 (m)^ⁿ
				9.12 (gp)^{^p}
				1.79 (rb)^ⁿ
				12.8 (d)^ⁿ
				12.3 (d)^{^p}
		nM
54	MRE-2029-F20	200 (h)^{^ss}	>1000 (h)^{^ss}	5.5 (h)^{^ss}	>1000 (h)^{^ss}
55	PSB-603	>10,000 (h)^{^tt}	>10,000 (h)^{^tt}	0.553 (h)^{^tt}	>10,000 (h)^{^tt}
		>10,000 (r)^{^tt}	>10,000 (r)^{^tt}	K_D 0.403 (h)^{^tt}
				K_D 0.351 (m)^{^tt}
56	CVT-6883	1940 (h)^{^uu}	3280 (h)^{^uu}	22 (h)^{^uu}	1070 (h)^{^uu}
57	PSB-1115	>10,000 (h)^{^u}	24,000 (r)^{^m}	53.4 (h)^{^u}	>10,000 (h)^{^u}
		2200 (r)^{^m}
58	ATL 802	369 (h)^{^rr}	654 (h)^{^rr}	2.36 (h)^{^rr}	>1000 (h)^{^rr}
		9583 (m)^{^rr}	8393 (m)^{^rr}	8.58 (m)^{^rr}	>10,000 (m)^{^rr}
59	LAS38096	2821 (h)^{^vv}	>1000 (h)^{^vv}	17 (h)^{^vv}	1043 (h)^{^vv}
A₃-selective antagonists
60	KF26777	1800 (h)^{^ww}	470 (h)^{^ww}	620 (h)^{^ww}	0.20 (h)^{^ww}
61	PSB-10	1700 (h)^{^xx}	2700 (h)^{^xx}	N.D.	0.441 (h)^{^yy}
		805 (r)^{^yy}	6040 (r)^{^yy}
62	PSB-11	1640 (h)^{^xx}	1280 (h)^{^xx}	2100 (m)^{^yy}	2.34 (h)^{^xx}
		440 (r)^{^xx}	2100 (r)^{^xx}		K_D 4.9 (h)^{^zz}
63	MRE-3008-F20	1200 (h)^{^aa}	141 (h)^{^aa}	2100 (h)^{^aa}	0.82 (h)^{^aa}
64	MRS1523	>10,000 (h)^{^aaa}	3660 (h)^{^aaa}	>10,000 (h)^{^aaa}	18.9 (h)^{^aa}
		15,600 (r)^{^aaa}	2050 (r)^{^aaa}	>10,000 (m)^{^aaa}	113 (r)^{^aaa}
					731 (m)^{^aaa}
65	MRS1191	>10,000 (h)^{^aaa}	>10,000 (h)^{^aaa}	>10,000 (h)^{^aaa}	31.4 (h)^{^aaa}
		40,100 (r)^{^aaa}	>10,000 (r)^{^aaa}		1850 (r)^{^aaa}
66	VUF-5574	≤10,000 (r)^{^bbb}	≤10,000 (r)^{^bbb}	N.D.	4.03 (h)^{^bbb}

h, human; c, cow; d, dog; gp, guinea pig; m, mouse; r, rat; rb, rabbit; N.D., no data available; LUF5981, 8-cyclohexyl-2,6-diphenyl-1-deazapurine; CSC, 8-(3-chlorostyryl)caffeine; KF26777, 2-(4-bromophenyl)-4-ethyl-4,5,7,8-tetrahydro-1H-imidazo[2.1-i]purin-5-one.
↵a Jacobson et al., 1999.
↵b Abo-Salem et al., 2004.
↵c Borrmann et al., 2009.
↵d Kim et al., 2002.
↵e van Galen et al., 1994.
↵f Grahner et al., 1994.
↵g Daly et al., 1991.
↵h Bertarelli et al., 2006.
↵u Müller et al., 2000.
↵j Brackett and Daly, 1994.
↵k Ukena et al., 1986b.
↵l Klotz et al., 1998.
↵m Müller et al., 1993b.
↵n Auchampach et al., 2009.
↵o Klotz et al., 1991.
↵p Fozard et al., 2003.
↵q Jacobson et al., 1995.
↵r Auchampach et al., 1997.
↵s Müller, 2000a.
↵t Weyler et al., 2006.
↵u Hayallah et al., 2002.
↵v Holschbach et al., 2002.
↵w Pfister et al., 1997.
↵x Kiesman et al., 2006b.
↵y Kiesman et al., 2006a.
↵z Doggrell, 2005.
↵aa Jacobson and Gao, 2006.
↵bb Kalk et al., 2007.
↵cc Chang et al., 2007.
↵dd Müller et al., unpublished data.
↵ee Kase et al., 2003.
↵ff Shimada et al., 1997.
↵gg Pretorius et al., 2008.
↵hh Jacobson et al., 1993a.
↵ii Daly and Jacobson, 1995.
↵jj Sauer et al., 2000.
↵kk Recombinant receptors (expressed in CHO cells).
↵ll Solinas et al., 2005.
↵mm Native receptors (post mortem brain).
↵nn Gillespie et al., 2009.
↵oo Minetti et al., 2005.
↵pp Müller and Ferré, 2007.
↵qq Kecskés et al., 2010.
↵rr Kim et al., 2000.
↵ss Baraldi et al., 2004.
↵tt Borrmann et al., 2009.
↵uu Elzein et al., 2008.
↵vv Vidal et al., 2007; Eastwood et al., 2010.
↵ww Saki et al., 2002.
↵xx Ozola et al., 2003.
↵yy Müller et al., 2002a.
↵zz Müller et al., 2002b.
↵aaa Liang et al., 2010.
↵bbb van Muijlwijk-Koezen et al., 2000.