Nomenclature |
β1-adrenoceptor |
β2-adrenoceptor |
β3-adrenoceptor |
HGNC, UniProt |
ADRB1, P08588
|
ADRB2, P07550
|
ADRB3, P13945
|
Principal transduction |
Gs
|
Gs
|
Gs
|
Rank order of potency |
(-)-noradrenaline > (-)-adrenaline |
(-)-adrenaline > (-)-noradrenaline |
(-)-noradrenaline = (-)-adrenaline |
Endogenous agonists (pKi) |
noradrenaline (6.0) 356
|
– |
– |
Selective agonists (pKi) |
(-)-Ro 363 (8.0) 380, xamoterol (Partial agonist) (7.0) 364, denopamine (Partial agonist) (5.8) 364,400
|
formoterol (pEC50 10.08) 334, salmeterol (pEC50 9.9) 334, zinterol (pEC50 9.48) 334, procaterol (pEC50 8.43) 334
|
carazolol (8.7) 376, BRL 37344 (6.4–7.0) 338,348,362,376, CGP 12177 (Partial agonist) (6.1–7.3) 338,373,376,380, CL316243 (5.2) 411, L 755507 (pEC50 10.1) 334, L742791 (pEC50 8.8) 408, SB251023 (pEC50 7.14 - Mouse) 363
|
Selective antagonists (pKi) |
CGP 20712A (8.5–9.2) 332,341,373, betaxolol (8.8) 373, atenolol (6.7–7.6) 332,366,373
|
ICI 118551 (Inverse agonist) (9.2–9.5) 332,335,373
|
L-748337 (8.4) 341, SR59230A (6.9–8.4) 341,347,362
|
Radioligands (Kd) |
[125I]ICYP (Antagonist, it is necessary to use an excess of a β2-AR-selective ligand such as ICI 118551 to allow visualisation of β1-AR binding in native tissue) (4.99x10-12–3.28x10-11 M) 373,395
|
[125I]ICYP (Antagonist, it is necessary to use an excess of a β1-AR-selective ligand such as CGP20712A to allow visualisation of β2-AR binding in native tissues) (7.9x10-12 M) 373,395
|
[125I]ICYP (Agonist, Partial agonist) (1.58x10-10–6.31x10-10 M) 373,380,385,395,399
|
Comment |
The agonists indicated have less than two orders of magnitude selectivity 334. |
– |
Agonist SB251023 has a pEC50 of 6.9 for the splice variant of the mouse β3 receptor, β3b
363. |