Table 2.

Adenosine receptor affinities of antagonists.

		Ki (nM)a
		A1	A2A	A2B	A3
Non-selective antagonists
38	Caffeine	10,700 (h) [145]	23,400 (h) [67]	33,800 (h) [14]	13,300 (h) [145]
		44,900 (h) [67]	9560 (h) [145]	10,400 (h) [149]	>100,000 (r) [133]
		41,000 (r) [146]	45,000 (r) [147]	20,500 (h) [150]
		44,000 (r) [147]	32,500 (r) [148]	30,000 (r) [131]
		47,000 (gp) [20]	48,000 (r) [145]	13,000 (m) [131]
		44,000 (c) [20]
39	Theophylline	6770 (h) [127]	1710 (h) [127]	9070 (h) [149]	22,300 (h) [145]
		14,000 (r) [151]	6700 (h) [145]	74,000 (h) [150]	86,400 (h) [127]
		8740 (r) [145]	22,000 (r) [151]	15,100 (r) [149]	>100,000 (r) [133]
		7060 (gp) [152]	25,300 (r) [145]	5630 (m) [141]	85,000 (r) [154]
		4710 (rb) [152]		11,000 (gp) [153]	>100,000 (d) [155]
		9050 (s) [152]		17,700 (rb) [141]
		6330 (c) [152]		38,700 (d) [141]
A1-selective antagonists
40	DPCPX (CPX)	3.0 (h) [25]	129 (h) [127]	51 (h) [25]	795 (h) [156]
		0.50 (r) [25]	60 (h) [25]	63.8 (h) [149]	243 (h) [25]
		1.0 (r) [149]	157 (r) [148]	186 (r) [149]	509 (h) [155]
		0.18 (r) [152]	500 (r) [149]	200 (r) [153]	3960 (h) [127]
		1.06 (gp) [152]		86.2 (m) [141]	>10,000 (r) [25]
		3.9 (gp) [20]		145 (gp) [153]	43,000 (r) [155]
		0.21 (rb) [152]		96.0 (rb) [141]	708 (rb) [155]
		0.10 (s) [152]		147 (d) [141]	115 (d) [155]
		0.05 (c) [152]		132 (d) [153]
		0.29 (c) [20]
		11.4 (d) [155]
41	Rolofylline (KW3902, NAX)	0.72 (h) [61]	108 (h) [61]	296 (h) [157]	4390 (h) [157]
		8.0 (h) [157]	673 (h) [157]
		0.19 (r) [158]	380 (r) [158]
		12.6 (r) [61]	510 (r) [61]
42	Toponafylline (BG-9928)	7.4 (h) [157]	6410 (h) [157]	90 (h) [157]	>10,000 (h) [157]
		3.9 (mk) [159]	943 (mk) [159]
		1.3 (r) [157]	2440 (r) [157]
		29 (d) [159]	4307 (d) [159]
43	Naxifylline (BG9719, CVT-124)	0.45 (h) [61]	1100 (h) [61]	611 (h) [158]	4810 (h) [158]
		12 (h) [158]	1660 (h) [158]	1010 (m) [141]
		0.67 (r) [61]	1250 (r) [61]	470 (rb) [141]
				742 (d) [141]
44	PSB-36	0.7 (h) [25]	980 (h) [25]	187 (h) [25]	2300 (h) [25]
		0.124 (r) [25]	552 (r) [25]		6500 (r) [25]
45	FK-453	18 (h) [109]	1300 (h) [109]	980 (h) [109]	>10,000 (h) [109]
46	SLV320	1.00 (h) [160]	398 (h) [160]	3981 (h) [160]	200 (h) [160]
		2.51 (r) [160]		501 (r) [160]
47	Thiazole derivative	57.4 (h) [63]	6250 (h) [63]	>1000 (r) [63]	2160 (h) [63]
		4.83 (r) [63]	> 1000 (r) [63]
48	L-97-1	580 (h) [161]	> 100,000 (h) [161]	>100,000 (h) [161]	ndb
A2A-selective antagonists
49	Istradefylline (KW6002)	841 (h)c	12 (h) [162]	>10,000 (h)c	4470 (h)c
		230 (r)c	91.2 (h)c
			2.2 (r) [163]
			4.46 (r) [164]
50	CSC (Ki MAO-B=80.6 nM) [164]	28,000 (r) [165]	54 (r) [165]	8200 [165]	>10,000 (r) [133]
51	MSX-2	900 (r) [26]	8.04 (r) [26,148]	>10,000 (h) [26]	>10,000 (h) [26]
		2500 (h) [26]	5.38 (h)d, [26]
			14.5 (h)e, [26]
52	CGS15943	3.5 (h) [18]	1.2 (h) [18]	32.4 (h) [141]	35 (h) [18]
		6.4 (r) [18]		9.07 (m) [141]
53	ZM-241385	774 (h) [109]	1.6 (h) [109]	75 (h) [109]	743 (h) [109]
54	Vipadenant (BIIB014, V2006)	68 (h) [166]	1.3 (h) [166]	63 (h) [166]	1005 (h) [166]
55	SCH-442416	1110 (h) [109]	4.1 (h) [32]	>10,000 (h) [109]	>10,000 (h) [109]
56		2720 (r) [72]	18.3 (r) [72]	3420 (h) [72]	489 (h) [72]
57	SCH-58261	725 (h) [109]	5.0 (h) [109]	1110 (h) [109]	1200 (h) [109]
58	Preladenant (SCH-420814)	>1000 (h) [65]	0.9 (h) [65]0	>1000 (h) [65]	>1000 (h) [65]
59	ST-1535	71.8 (h) [167]	6.6 (h) [167]9	352.3 (h) [167]	>1000 (h) [167]
60	SYN-115	nd	nd	nd	nd
61		2.8 (h) [75]	0.0038 (h) [75]	nd	nd
			0.14 (h) cAMP [75]
62		228.4 (h) [76]	0.38 (h) [76]	nd	nd
A2B-selective antagonists
63	MRS1754	403 (h) [168]	503 (h) [168]	1.97 (h) [168]	570 (h) [168]
		16.8 (r) [168]	612 (r) [168]	12.8 (r) [168]
				16.6 (r) [153]
				3.39 (m) [141]
				9.12 (gp) [153]
				1.79 (rb) [141]
				12.8 (d) [141]
				12.3 (d) [153]
66	MRE-2029-F20	200 (h) [169]	> 1000 (h) [169]	5.5 (h) [169]	>1000 (h) [169]
65	PSB-603	>10,000 (h) [14]	> 10,000 (h) [14]	0.553 (h) [14]	>10,000 (h) [14]
		>10,000 (r) [14]	> 10,000 (r) [14]	KD 0.403 (h) [14]
				KD 0.351 (m) [14]
67	GS 6201 (CVT-6883)	1940 (h) [170]	3280 (h) [170]	22 (h) [170]	1070 (h) [170]
64	PSB-1115	>10,000 (h) [156]	24,000 (r) [151]	53.4 (h) [156]	>10,000 (h) [156]
		2200 (r) [151]
68	ATL 802	369 (h) [168]	654 (h) [168]	2.36 (h) [168]	>1000 (h) [168]
		9583 (m) [168]1	8393 (m) [168]	8.58 (m) [168]	>10,000 (m) [168]
69	LAS38096	2821 (h) [171,172]	> 1000 (h) [171,172]	17 (h) [171,172]	1043 (h) [171,172]
70		nd	965 (h) [173]	3.5 (h) [173]	nd
71		100 (h) [174]	51 (h) [174]	8 (h) [174]	nd
				21 (h) cAMP [174]
72		931 (h) [174]	239 (h) [174]	4 (h) [174]	3754 (h) [174]
73		2444 (h) [175]	2126 (h) [175]	11 (h) [175]	>1000 (h) [175]
74	OSIP	37 (h) [176]	328 (h) [176]	0.41 (h) [176]	450 (h) [176]
75	QAF805	186 (h) [177]	1775 (h) [177]	3.4 (h) [177]	10.2 (h) [177]
A3-selective antagonists
76	MRS1523	>10,000 (h) [134]	3660 (h) [134]	>10,000 (h) [134]	18.9 (h) [109]
		15,600 (r) [134]	2050 (r) [134]		113 (r) [134]
				>10,000 (m) [134]	731 (m) [134]
77	MRE3008-F20	1200 (h) [109]	141 (h) [109]	2100 (h) [109]	0.82 (h) [109]
78		562 (h) [178]	778 (h) [178]	>10,000 (h) [178]	0.108 (h) [178]
79	VUF-5574	≥10,000 (r) [179]	≥10,000 (r) [179]	nd	4.03 (h) [179]
80	KF26777	1800 (h) [180]	470 (h) [180]	620 (h) [180]	0.20 (h) [180]
81	PSB-10	1700 (h) [181]	2700 (h) [181]	nd	0.441 (h) [28]
		805 (r) [28]	6040 (r) [28]
82	PSB-11	1640 (h) [181]	1280 (h) [181]	2100 (m) [28]	2.34 (h) [181]
		440 (r) [181]	2100 (r) [181]		KD 4.9 (h) [182]
83		>1000 (h) [183]	> 1000 (h) [183]	>1000 (h) [183]	1.2 (h) [183]
84	MRS5147	1760 (h) [55]	1600 (h) [55]	nd	0.73 (h) [55]
85	MRS5127	3040 (h) [55]	1080 (h) [55]	nd	1.44 (h) [55]
86	LJ1251	2490 (h) [184]	341 (h) [184]	nd	4.16 (h) [184]
87	OT7999	>10,000 (h) [50]	> 10,000 (h) [50]	>10,000 (h) [50]	0.95 (h) [50]

^ah = human; c = cow; d = dog; gp = guinea pig; m = mouse; r = rat; rb = rabbit; s = sheep; a few A_2B data are from functional (cAMP) studies.

^bnd = no data available.

^cUnpublished data (Müller et al.).

^dRecombinant receptors (expressed in CHO cells).

^eNative receptors (post-mortem brain).