Table 1 Maximal binding capacities (Bmax) and binding affinities (Kd) of [Sar1,Ile8]Ang II, irbesartan and losartan to AT1 wild-type (WT) and mutants receptors

From: A small difference in the molecular structure of angiotensin II receptor blockers induces AT1 receptor-dependent and -independent beneficial effects

  

Kd (n M)

Receptor

B max (pmol mg − 1 protein)

[Sar 1 ,Ile 8 ]Ang II

Irbesartan

Losartan

WT

0.62±0.07

0.8±0.3 (1.0)

1.9±1.1 (1.0)

11±3 (1.0)

V108A

0.60±0.11

0.7±0.4 (0.9)

19±5 (10)

416±149 (38)

S109A

0.51±0.03

0.9±0.6 (1.1)

2.1±0.6 (1.1)

33±13 (3.0)

L112A

0.57±0.04

0.8±0.3 (1.0)

10±1 (5.3)

593±88 (54)

Y113F

0.71±0.12

1.8±1.0 (2.3)

4.6±0.7 (2.4)

179±18 (10)

Y113A

0.30±0.02

0.8±0.2 (1.0)

49±5 (26)

1455±431 (132)

Y184F

0.65±0.04

0.9±0.4 (1.1)

3.0±1.3 (1.6)

40±17 (3.6)

Y184A

0.56±0.03

0.9±0.3 (1.1)

2.1±1.1 (1.1)

21±3 (1.9)

K199Q

0.25±0.04

2.0±0.9 (2.5)

2.0±1.0 (1.1)

21±9 (1.9)

N200A

0.29±0.02

1.8±1.2 (2.3)

1.8±0.2 (0.9)

26±13 (2.4)

F204A

0.15±0.02

24±9 (30)

—

—

H256A

0.29±0.09

0.8±0.4 (1.0)

2.4±1.4 (1.3)

41±17 (3.7)

Q257A

0.15±0.07

5.0±2.1 (6.3)

3.2±0.7 (1.7)

148±29 (13)

M284G

0.43±0.01

0.6±0.1 (0.8)

0.7±0.1 (0.4)

7.8±2.3 (0.7)

M284A

0.41±0.03

1.3±0.7 (1.6)

0.5±0.1 (0.3)

9.0±0.9 (0.8)

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