|
|
|
α1D-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
5.5 – 7.4 |
pKi |
- |
7,14,16 |
|
⤷ |
pKi
5.5 – 7.4
[7,14,16]
|
α1D-adrenoceptor
|
|
|
Rn |
Agonist |
Full agonist |
6.3 |
pKi |
- |
10 |
|
⤷ |
pKi
6.3
[10]
|
β1-adrenoceptor
|
|
|
Hs |
Agonist |
Agonist |
5.5 – 6.0 |
pKi |
- |
1,5-6 |
|
⤷ |
pKi
5.5 – 6.0
[1,5-6]
|
α2C-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
4.5 – 6.8 |
pKi |
- |
8-9,11,13 |
|
⤷ |
pKi
4.5 – 6.8
[8-9,11,13]
|
α1A-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
4.8 – 6.4 |
pKi |
- |
2,4,7,14-16,18 |
|
⤷ |
pKi
4.8 – 6.4
[2,4,7,14-16,18]
|
α2A-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
3.6 – 7.4 |
pKi |
- |
8,11,13 |
|
⤷ |
pKi
3.6 – 7.4
[8,11,13]
|
β3-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
4.7 – 6.3 |
pKi |
- |
6,12,17 |
|
⤷ |
pKi
4.7 – 6.3
[6,12,17]
|
α1B-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
3.8 – 6.2 |
pKi |
- |
14,16 |
|
⤷ |
pKi
3.8 – 6.2
[14,16]
|
β2-adrenoceptor
|
|
|
Hs |
Agonist |
Agonist |
4.6 – 5.4 |
pKi |
- |
1,5-6 |
|
⤷ |
pKi
4.6 – 5.4
[1,5-6]
|
α2B-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
3.5 – 6.0 |
pKi |
- |
8,11,13 |
|
⤷ |
pKi
3.5 – 6.0
[8,11,13]
|
β3-adrenoceptor
|
|
|
Rn |
Agonist |
Full agonist |
4.2 |
pKi |
- |
12 |
|
⤷ |
pKi
4.2
[12]
|
β3-adrenoceptor
|
|
|
Mm |
Agonist |
Full agonist |
3.8 |
pKi |
- |
12 |
|
⤷ |
pKi
3.8
[12]
|
β1-adrenoceptor
|
|
|
Hs |
Agonist |
Agonist |
7.9 |
pEC50 |
- |
1 |
|
⤷ |
pEC50
7.9
[1]
|
α1B-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
5.9 – 9.2 |
pEC50 |
- |
14 |
|
⤷ |
pEC50
5.9 – 9.2
[14]
|
α2B-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
6.9 – 7.8 |
pEC50 |
- |
13 |
|
⤷ |
pEC50
7.8
[13]
Description: ERK1/2 phosphorylation
pEC50
6.9
[13]
Description: cAMP generation
|
α1D-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
6.6 – 7.8 |
pEC50 |
- |
14 |
|
⤷ |
pEC50
6.6 – 7.8
[14]
|
β3-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
7.2 |
pEC50 |
- |
1 |
|
⤷ |
pEC50
7.2
[1]
|
α1A-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
5.5 – 8.6 |
pEC50 |
- |
2,4,14 |
|
⤷ |
pEC50
5.5 – 8.6
[2,4,14]
|
α2C-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
6.0 – 7.7 |
pEC50 |
- |
9,13 |
|
⤷ |
pEC50
7.7
[13]
Description: ERK1/2 phosphorylation
pEC50
6.0 – 6.6
[9]
Description: 6.02 = value for β-arrestin recruitment and internalization
|
α2A-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
5.3 – 7.7 |
pEC50 |
- |
8,13 |
|
⤷ |
pEC50
7.7
[13]
Description: increased ERK1/2 phosphorylation
pEC50
6.7
[8]
Description: GTPγs binding
pEC50
5.3
[13]
Description: increased cAMP generation
|
β2-adrenoceptor
|
|
|
Hs |
Agonist |
Agonist |
6.4 |
pEC50 |
- |
1 |
|
⤷ |
pEC50
6.4
[1]
|
α2B-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
7.8 |
pIC50 |
- |
13 |
|
⤷ |
pIC50
7.8
[13]
Description: inhibition of forskolin stimulated cAMP generation
|
α2C-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
6.5 – 8.6 |
pIC50 |
- |
9,13 |
|
⤷ |
pIC50
6.5 – 8.6
[9,13]
Description: inhibition of cAMP production
|
α2A-adrenoceptor
|
|
|
Hs |
Agonist |
Full agonist |
6.6 |
pIC50 |
- |
13 |
|
⤷ |
pIC50
6.6
[13]
Description: inhibition of forskolin stimulated cAMP generation
|
|