TABLE 4.

Adenosine receptor affinities of antagonists

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

		Ki
		A1	A2A	A2B	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	ndb	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
A2A-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 (Ki MAO-B = 80.6 nM)gg	28,000 (r)hh	54 (r)hh	8200ii	>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
A2B-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	KD 0.403 (h)tt
				KD 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		KD 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.