. Author manuscript; available in PMC: 2007 Jan 1.

Published in final edited form as: Recent Pat Cardiovasc Drug Discov. 2006 Jan;1(1):95–108. doi: 10.2174/157489006775244263

Table 2.

Examples of Recently Published and Commercially Available ET Receptor Agonists and Antagonists and Their Selectivity to ET Receptor Subtypes

Compound	Chemistry	Receptor Specificity	US Patent
Agonists
ET₁ ET₂ ET₃	Cys-Ser-Cys-Ser-Ser-Leu-Met-Asp-Lys-Glu-Cys-Val-Tyr- Phe- Cys-His-Leu-Asp-Ile-Ile-Trp	ET_A, ET_B ET_A, ET_B ET_B	5468623 [87] 5230999 [88]
IRL 1620	Suc-Asp-Glu-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp	ET_B	20050084872^* [89]
S6c	Cys-Thr-Cys-Asn-Asp-Met-Thr-Asp-Glu-Glu-Cys-Leu-Asn-Phe- Cys-His-Gln-Asp-Val-Ile-Trp	ET_B	20050090514^* [90]
Antagonists
A127722	2-(4-methoxyphenyl)-4-(1,3-benzodioxol-5-yl)-1-(((dibutyl amino)carbonyl) methyl)pyrrolidine-3-carboxylic acid	ET_A	6573285 [91]
ABT 627	(2R,3R,4S)-1-[(dibutyl carbamoyl)methyl]-2-(p-methoxyphenyl)- 4[3,4-(methylenedioxy)phenyl]-3-pyrrolidinecarboxylic acid	ET_A	20050042172^* [92]
BMS 182874	5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1- naphthalenesulfonamide	ET_A
Bosentan	4-t-butyl-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2,2′- bipyrimidin-4-yl)benzenesulfonamide	ET_A, ET_B	20030176356^* [93]
BQ 123	Cyclo(D-α-aspartyl-L-prolyl-D-valyl-L-leucyl-D-tryptophyl)	ET_A	6573285 [91]
BQ 610	Homopiperidinyl-CO-Leu-D-Trp(CHO)-D-Trp-OH	ET_A	20030176356^* [93]
BQ 788	N-cis-2,6-dimethylpiperidinocarbonyl-γ-methylleucyl-tryptophyl(COOMe)-norleucine	ET_B	20030176356^* [93]
FR 139317 (PD 147953)	N-(N-(N-((hexahydro-1H-azepin-1-yl)carbonyl)-L-leucyl)-1-methyl-D-tryptophyl)-3-(2-pyridinyl)-2-((1-(hexahydro-1H-azepinyl)carbonyl)amino-4-methyl-pentanoyl)-3-(-(1-methyl-1H-indolyl)propionyl)amino-3-(2-pyridyl)propionic acid	ET_A	20030176356^* [93]
LU 135252	2-(4,6-dimethoxypyrimidin-2-yloxy)-3-methoxy-3,3-diphenylpropionic acid	ET_A	20030176356^* [93]
PD 142893	Ac-D-(3,3-diphenylalanine)-leu-Asp-Ile-Ile-Trp-OH	ET_A, ET_B	20030176356^* [93]
PD 145065	Ac-D-(5H-dibenzo[a,d]cycloheptene-5-glycine)-Leu-Asp-Ile-Ile- Trp-OH	ET_A, ET_B	20030176356^* [93]
PD 156707	Sodium 2-benzo[1,3]dioxol-5-yl-4-(4-methoxy-phenyl)-4-oxo-3-(3,4,5-trimethoxy-benzyl)-but-2-enoate	ET_A	6573285 [91]
RES 701–1	L-Tryptophan, glycyl-L-asparaginyl-L-tryptophyl-L-histidylglycyl- L-threonyl-L-alanyl-L-prolyl-L-α-aspartyl-L-tryptophyl-L- phenylalanyl-L-phenylalanyl-L-asparaginyl-L-tyrosyl-L- tyrosyl-, cyclic (9–1)-peptide	ET_B2	6855701 [94]
SB 209670	3-(2-(carboxymethoxy)-4-methoxyphenyl)-1-(3,4-(methylene dioxy)phenyl)-5-(prop-1-yloxy)indan-2-carboxylic acid	ET_A, ET_B1	6573285 [91]
TAK 044	cyclo(D-alpha-aspartyl-3-((4-phenylpiperazin-1-yl)carbonyl)-L-alanyl-L-alpha-aspartyl-D-2-(2-thienyl)glycyl-L-leucyl-D-tryptophyl) disodium salt	ET_A, ET_B	6573285 [91]

US patent application number.

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