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. 2017 Oct 21;174(Suppl Suppl 1):S17–S129. doi: 10.1111/bph.13878
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]