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. Author manuscript; available in PMC: 2014 Jan 7.
Published in final edited form as: Handb Exp Pharmacol. 2011;(200):10.1007/978-3-642-13443-2_6. doi: 10.1007/978-3-642-13443-2_6

Table 4.

Adenosine receptor affinities of 8-styrylxanthines and configurationally stable analogs

Ki (nM)a
A1 A2A A2B A3
Styrylxanthinesb
85 1,3-Dipropyl-8-stryrylX 22.2 (r)1 85.1 (r)1 nd nd
86 1-Methyl-3-propyl-8-styrylX 31.1 (r)1 46.5 (r)1 nd nd
87 Istradefylline (KW-6002) (Ki MAO-B = 28,000 nM)2 841 (h)c
230 (r)c 		12 (h)3
91.2 (h)c
2.2 (r)4
4.46 (r)5 		>10,000 (h)c 4,470 (h)c
88 8-Styrylcaffeine (Ki MAO-B = 2,864 nM)6 3890 (r)7 94 (r)7 nd nd
89 CSC (Ki MAO-B = 80.6 nM MAO-B)5 28,000 (r)7 54 (r)7 8,2008 >10,000 (r)9
90 KF17837 390 (r)10 7.9 (r)10 (E/Z)
1.0 (r)10 (E)		 1,500 (h)10 nd
91 Styryl-DMPX 1,100 (r)11 27 (r)11 nd nd
92 CS-DMPX 1,300 (r)11 13 (r)11 nd nd
93 BS-DMPX 1,200 (r)11 8.2 (r)11
10 (r)12 		>10,000 (h)13 >10,000 (h)13
94 m-Methoxystyryl-DMPX 1,280 (r)13 12 (r)13 nd nd
95 m-Hydroxystyryl-DMPX 940 (r)13 21 (r)13 nd nd
96 7-unsubst. analog of CS-DMPX 250 (r)11 410 (r)11 nd nd
97 3-Propyl analog of CS-DMPX 102 (r)11 5.1 (r)11 nd nd
98 p-SS-DMPX 4,900 (r)12 240 (r)12 nd nd
99 MSX-2 900 (r)14
2,500 (h)14 		8.04 (r)13,14
5.38 (h)14,d
14.5 (h) 14,e 		>10,000 (h)14
2,900 (h)15 		>10,000 (h)14
102 DMPTX (8-(3-thienylethenyl)-1,3-dipropylX) 561 (r)16 19 (r)16 nd nd
103 44 (r)17 >10,000 (r)17 nd nd
Analogs of Styrylxanthines
104 Phenylcyclopropyl-DMPX (trans, rac.) 4,600 (r)18 1,700 (r)18 nd nd
105 β-Naphthyl-DMPX 980 (r)18 380 (r)18 nd nd
106 3-Indolyl-DMPX 1,000 (r)18 300 (r)18 nd nd
107 Phenylethynyl-DMPX >3,000 (r)18 314 (h)c
300 (r)18 		nd 5,000 (h)c
108 PhenylbutadienylX (Ki MAO-B = 42.1 nM)5 nd 104 (r)18 nd nd
a

h = human; c = cow; d = dog; gp = guinea pig; m= mouse; mk = monkey; r = rat; rb = rabbit; a few A2B data are from functional (cAMP) studies; nd = no data available

b

most data probably represent data from mixture of E/Z isomers since in dilute solutions light-induced isomerization occurs very fast and is difficult to avoid under standard testing conditions

c

Müller et al., unpublished data

d

recombinant receptors expressed in CHO cells

e

native receptors (post-mortem human brain cortex)