Nomenclature |
ETA
receptor
|
ETB
receptor
|
HGNC, UniProt |
EDNRA, P25101
|
EDNRB, P24530
|
Family selective
agonists |
endothelin‐1
(EDN1, P05305) =
endothelin‐2
(EDN2, P20800)
>endothelin‐3
(EDN3, P14138)
[1178] |
endothelin‐1
(EDN1, P05305) =
endothelin‐2
(EDN2, P20800),
endothelin‐3
(EDN3, P14138) |
Selective
agonists |
– |
sarafotoxin S6c
(pK
d 8.8–9.8) [1016, 1616], BQ 3020
(pK
i 9.7) [1576], [Ala1,3,11,15]ET‐1 (pK
d 8.7–9.2) [1300], IRL 1620
(pK
i 8.7) [1991] |
(Sub)family‐selective antagonists |
SB209670
(pK
B 9.4) [474] – Rat,
TAK 044
(pA2 8.4) [1993] – Rat,
bosentan
(pA2 7.2) [354] – Rat |
SB209670
(pK
B 9.4) [474] – Rat,
TAK 044
(pA2 8.4) [1993] – Rat,
bosentan
(pK
i 7.1) [1349] |
Selective
antagonists |
atrasentan
(pA2 9.2–10.5) [1446], PD‐156707
(pK
d 9–9.8) [1180], macitentan
(pIC50 9.3) [174], sitaxsentan
(pA2 8) [2047], FR139317
(Inverse agonist) (pIC50 7.3–7.9) [1178], ambrisentan
(pIC50 7.7) [175], BQ123
(pA2 6.9–7.4) [1178], avosentan
(pIC50 7.3) [210], ambrisentan
(pA2 7.1) [175] |
A192621
(pK
d 8.1) [2145], BQ788
(pK
d 7.9–8) [1616], IRL 2500
(pK
d 7.2) [1616], Ro 46‐8443
(pIC50 7.2) [209] |
Labelled
ligands |
[125I]PD164333 (Antagonist)
(pK
d 9.6–9.8) [398], [3H]S0139 (Antagonist) (pK
d 9.2), [125I]PD151242 (Antagonist)
(pK
d 9–9.1) [399], [3H]BQ123 (Antagonist) (pK
d 8.5) [817] |
[125I]IRL1620 (Agonist) (pK
d 9.9–10.1) [1362], [125I]BQ3020 (Agonist) (pK
d 8.3–10) [702, 1300, 1495], [125I][Ala1,3,11,15]ET‐1
(Agonist) (pK
d 9.7) [1300] |