Table 1 Functional selectivity profile of Nitro-I, Met-I, OTV1, and OTV2 from BRET assays in the agonist mode

From: G protein-specific mechanisms in the serotonin 5-HT2A receptor regulate psychosis-related effects and memory deficits

 

5-HT

Nitro-I

Met-I

OTV1

OTV2

pEC50

Emax

logτ/KA

pEC50

Emax

logτ/KA

pEC50

Emax

logτ/KA

pEC50

Emax

logτ/KA

pEC50

Emax

logτ/KA

Gαq

9.75 ± 0.23

101.10 ± 2.37

9.70 ± 0.15

9.65 ± 0.19

102.50 ± 9.81

9.67 ± 0.20

9.55 ± 0.31

98.16 ± 12.19

9.57 ± 0.39

5.38 ± 0.08

86.62 ± 3.72

5.28 ± 0.11

8.35 ± 0.19

75.20 ± 5.12

8.24 ± 0.14

Gα11

10.26 ± 0.08

98.03 ± 3.46

9.46 ± 0.06

9.96 ± 0.23

78.67 ± 6.99

9.13 ± 0.13

8.88 ± 0.11

79.73 ± 3.08

8.60 ± 0.12

5.41 ± 0.10

127.30 ± 11.26

5.93 ± 0.15

9.56 ± 0.12

80.31 ± 3.35

8.92 ± 0.12

Gα14

9.30 ± 0.10

98.44 ± 5.21

9.14 ± 0.09

8.72 ± 0.15

102.90 ± 5.67

8.73 ± 0.14

8.72 ± 0.11

98.77 ± 4.13

8.72 ± 0.13

5.72 ± 0.13

94.48 ± 5.94

5.64 ± 0.15

9.18 ± 0.25

90.79 ± 6.32

9.13 ± 0.14

Gα15

8.10 ± 0.08

99.36 ± 3.22

8.03 ± 0.09

7.61 ± 0.13

107.80 ± 4.62

7.66 ± 1.03

7.22 ± 0.27

98.48 ± 5.40

7.21 ± 0.10

NA

NA

NA

7.55 ± 0.33

60.05 ± 6.63

7.68 ± 0.04

Gαi1

8.12 ± 0.17

99.92 ± 6.02

8.16 ± 0.15

6.78 ± 0.09

73.92 ± 2.88

6.42 ± 0.15

7.73 ± 0.15

87.12 ± 4.55

7.56 ± 0.15

6.71 ± 0.28

23.21 ± 2.96

5.59 ± 0.44

7.96 ± 0.25

76.81 ± 6.93

7.65 ± 0.18

Gαi2

6.71 ± 0.08

99.95 ± 3.55

6.70 ± 0.15

7.69 ± 0.22

54.55 ± 4.28

6.73 ± 0.61

7.75 ± 0.16

50.40 ± 2.84

6.90 ± 0.60

NA

8.50 ± 0.38

25.05 ± 3.43

7.23 ± 0.70

Gαi3

7.16 ± 0.10

100 ± 3.89

7.20 ± 0.10

7.91 ± 0.15

54.48 ± 3.07

7.07 ± 0.18

7.47 ± 0.13

56.76 ± 2.50

6.88 ± 0.17

NA

8.45 ± 0.31

42.55 ± 4.58

7.70 ± 0.23

GαoA

7.02 ± 0.08

99.99 ± 3.33

7.01 ± 0.15

7.27 ± 0.24

51.01 ± 4.45

6.64 ± 0.51

7.14 ± 0.19

47.38 ± 3.50

6.25 ± 0.33

NA

8.35 ± 0.25

29.67 ± 2.68

7.76 ± 0.51

GαoB

6.98 ± 0.08

99.85 ± 3.46

7.05 ± 0.11

7.25 ± 0.23

45.76 ± 3.87

6.57 ± 0.24

7.12 ± 0.16

47.46 ± 2.89

6.63 ± 0.23

NA

8.04 ± 0.45

40.55 ± 6.64

7.18 ± 0.27

Gαz

8.00 ± 0.08

94.48 ± 3.32

8.13 ± 0.08

7.36 ± 0.14

100.30 ± 5.06

8.69 ± 0.13

7.20 ± 0.13

82.95 ± 4.19

8.55 ± 0.10

8.12 ± 1.81

16.44 ± 1.52

4.67 ± 0.90

8.12 ± 0.21

61.83 ± 5.17

7.89 ± 0.31

β-arrestin1

6.71 ± 0.06

99.31 ± 2.59

6.88 ± 0.05

6.65 ± 0.09

46.59 ± 1.95

6.32 ± 0.14

6.44 ± 0.08

38.18 ± 1.40

6.04 ± 0.17

NA

4.80 ± 0.17

76.65 ± 9.22

4.37 ± 0.10

β-arrestin2

6.75 ± 0.04

99.70 ± 1.85

6.84 ± 0.05

6.55 ± 0.11

43.78 ± 2.15

6.15 ± 0.12

6.02 ± 0.05

44.96 ± 1.10

5.63 ± 0.12

NA

6.32 ± 0.15

45.50 ± 3.22

5.44 ± 0.13

  1. NA no activity. Data represent mean ± SEM of 3 independent experiments.
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