Nomenclature |
ET
A receptor |
ET
B receptor |
HGNC, UniProt |
EDNRA, P25101
|
EDNRB, P24530
|
Family selective agonists |
– |
endothelin‐1 (EDN1, P05305) = endothelin‐2 (EDN2, P20800), endothelin‐3 (EDN3, P14138) |
Potency order of endogenous ligands |
endothelin‐1 (EDN1, P05305) = endothelin‐2 (EDN2, P20800) >endothelin‐3 (EDN3, P14138) [1242] |
– |
Selective agonists |
– |
sarafotoxin S6c [1062, 1690], BQ 3020 [1650], [Ala
1,3,11,15]ET‐1 [1354], IRL 1620 [2078] |
Sub/family‐selective antagonists |
SB209670 (pK
B 9.4) [502] – Rat, TAK 044 (pA2 8.4) [2081] – Rat, bosentan (pA2 7.2) [367] – Rat |
SB209670 (pK
B 9.4) [502] – Rat, TAK 044 (pA2 8.4) [2081] – Rat, bosentan (pK
i 7.1) [1405] |
Selective antagonists |
macitentan (pIC50 9.3) [177], sitaxsentan (pA2 8) [2135], FR139317 (Inverse agonist) (pIC50 7.3–7.9) [1242], BQ123 (pA2 6.9–7.4) [1242], ambrisentan (pA2 7.1) [178] |
A192621 (pK
d 8.1) [2043], BQ788 (pK
d 7.9–8) [1690], IRL 2500 (pK
d 7.2) [1690], Ro 46‐8443 (pIC50 7.2) [215] |
Labelled ligands |
[125
I]PD164333 (Antagonist) (pK
d 9.6–9.8) [416], [3
H]S0139 (Antagonist) (pK
d 9.2), [125
I]PD151242 (Antagonist) (pK
d 9–9.1) [417], [3
H]BQ123 (Antagonist) (pK
d 8.5) [858] |
[125
I]IRL1620 (Agonist) [1421], [125
I]BQ3020 (Agonist) [737, 1354, 1565], [125
I][Ala
1,3,11,15]ET‐1 (Agonist) [1354] |