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. 2015 Dec 9;172(24):5744–5869. doi: 10.1111/bph.13348
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]