Endothelin Receptor
ETs represent a group of three distinctive 21-amino acid peptides: ET-1, ET-2, and ET-3, with ET-1 being the main isoform produced in the cardiovascular system. Each ET isoform is synthesized as a large pre proendothelin(pre-pro-ET) that is cleaved to pro-ET (big ET-1, -2, and -3) and then further processed by ET-converting enzymes (ECE-1 and ECE-2) to yield mature ET. ET-1 exerts its action through two pharmacologically distinct G protein-coupled receptors, namely, ETA and ETB receptors. The ETA receptor is mostly expressed on vascular smooth muscle cells, fibroblasts, and cardiomyocytes and mediates the vasoconstrictor and proliferative effects of ETs. The ETB receptor is expressed on vascular endothelial cells where it induces endothelial-dependent vasodilatation through NO production and clearance of circulating ET-1.
The ETB receptor is also present on vascular smooth muscle cells, where its activation induces vasoconstriction and cell proliferation, and on fibroblasts, where it mediates cell proliferation, matrix contraction, and collagen production. Both ETA and ETB receptors mediate the detrimental actions of ET-1. Because of a “cross talk” between ETA and ETB receptors, selective antagonism of only one receptor subtype may result in compensation by the other receptor subtype and may be insufficient, whereas dual antagonism may be necessary for complete inhibition. The molecular basis of this cross talk between receptors could be the formation of ETA–ETB heterodimers in cells expressing both receptor subtypes, which may further modulate the functionality of the receptors.
The ETB receptor is also present on vascular smooth muscle cells, where its activation induces vasoconstriction and cell proliferation, and on fibroblasts, where it mediates cell proliferation, matrix contraction, and collagen production. Both ETA and ETB receptors mediate the detrimental actions of ET-1. Because of a “cross talk” between ETA and ETB receptors, selective antagonism of only one receptor subtype may result in compensation by the other receptor subtype and may be insufficient, whereas dual antagonism may be necessary for complete inhibition. The molecular basis of this cross talk between receptors could be the formation of ETA–ETB heterodimers in cells expressing both receptor subtypes, which may further modulate the functionality of the receptors.
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Endothelin Receptor
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Sarafotoxin S6c
catalog no : M30800
cas no: 121695-87-2
Highly selective ETB endothelin receptor agonist (Ki values are 0.29 and 28000 nM at ETB and ETA receptors respectively). -
Sarafotoxin S6a
catalog no : M30799
cas no: 126738-34-9
Endothelin receptor agonist (EC50 values are 7.5 and > 150 nM for contraction of pig coronary artery and guinea pig aorta respectively). Nociceptive in vivo. -
[Ala1,3,11,15]-Endothelin
catalog no : M30774
cas no: 121204-87-3
Selective ETB endothelin receptor agonist (IC50 values are 0.33 and 2200 nM for displacing [125I]-ET-1 from ETB and ETA receptors respectively). -
Atrial Natriuretic Peptide (ANP) (1-28), rat
catalog no : M29920
cas no: 88898-17-3
Atrial Natriuretic Peptide (1-28), rat is the major circulating form of ANP in rats. -
Carperitide
catalog no : M29919
cas no: 89213-87-6
Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) inhibits endothelin-1 secretion in a dose-dependent way.