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Table 1 Compounds selected for functional studies in view of their agonistic properties for the 25 TAS2R receptors identified in humans to date

From: The expression and relaxant effect of bitter taste receptors in human bronchi

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

    
  1. The most recent nomenclature was adopted [5, 2024]. 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.