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. 2013 Nov 22;14(1):134. doi: 10.1186/1465-9921-14-134

Table 1.

Compounds selected for functional studies in view of their agonistic properties for the 25 TAS2R receptors identified in humans to date

hTAS2R 1 3 4 5 7 8 9 10 13 14 16 19 20 30 31 38 39 40 41 42 43 45 46 50 60
Chloroquine
 
10 and 172 ± 29
 
 
+
 
 
10000
 
 
 
 
 
 
 
 
100
 
 
 
 
 
 
 
 
Quinine
 
 
10
 
10
 
 
10
 
10
 
 
 
 
10
 
10
10
 
 
10
 
10
 
 
Denatonium
 
 
300
 
 
1000
 
3 and 120 ± 56
30
 
 
 
 
0.03 and 0.27 ± 0.06
 
 
100
 
 
 
300
 
30 and 240 ± 192
 
 
Colchicine
 
 
100 and 1025 ± 121
 
 
 
 
 
 
 
 
 
 
 
 
 
3000
 
 
 
 
 
300 and 1580 ± 170
 
 
Strychnine
 
 
 
 
+
 
 
3 and 21.8 ± 7.5
 
 
 
 
 
 
 
 
 
 
 
 
 
 
0.1 and 0.43 ± 0.02
 
 
Diphenidol
100
 
100
 
10
 
 
30
30
10
100
 
100
100
3
100
100
30
 
 
30
 
30
 
 
Caffeine
 
 
 
 
300
 
 
300
 
300
 
 
 
 
 
 
 
 
 
 
300
 
300
 
 
Saccharin
 
 
 
 
 
+
 
 
 
 
 
 
 
 
170 ± 10
 
 
 
 
 
80 ± 60
 
 
 
 
Ofloxacin
 
 
 
 
 
 
EC50 ≈200
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
Phenanthroline
 
 
 
100
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
Erythromycin
 
 
 
 
 
 
 
300
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
Dapsone
 
 
100
 
 
 
 
100
 
 
 
 
 
 
 
 
 
30
 
 
 
 
 
 
 
Flufenamic acid
 
 
 
 
 
 
 
 
 
0.01 and 0.14 ± 0.02
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
Carisoprodol
 
 
 
 
 
 
 
 
 
100
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
Malvidin-3-glucoside
 
 
 
 
6 and 12.6 ± 0.7
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
Sodium cromoglycate         3000 and 4500 ± 1600               10 and 45 ± 25               3000        

The most recent nomenclature was adopted [5,20-24]. Unless otherwise stated, single values (without SEM) represent the threshold concentration, defined as the lowest concentration (μM) that elicited a calcium response in transfected HEK-293 T cells, whereas values presented as mean ± SEM represent the EC50 (μM) [5]. When both threshold concentration and EC50 were available, both values were reported in this order. When no quantitative indicator was available, the symbol “+” indicates agonist property of the compound to the receptor.