Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: ex vivo and in vivo studies
Keyword(s):
Ex Vivo
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Endothelins (ETs), 21-amino-acid peptides involved in the pathogenesis of various diseases, bind to ETA and ETB receptors to initiate their effects. Based on the same core structure, we have developed four small-molecule ET receptor antagonists, ABT-627 (atrasentan), ABT-546, A-182086 and A-192621, which exhibit differences in selectivity for ETA and ETB receptors. In this report, we compare the efficacy, potency and pharmacokinetic properties of these four antagonists, including potency in inhibiting ET-1- or Sarafotoxin 6c-induced vessel constriction in isolated arteries and efficacy in antagonizing ET-1-, big ET-1- or Sarafotoxin 6c-induced pressor responses in rats.
1999 ◽
Vol 165
(2)
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pp. 163-168
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1994 ◽
Vol 112
(1)
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pp. 207-213
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Keyword(s):
2017 ◽
Vol 10
(5)
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pp. 3827-3835
Monocytes as Carriers of Magnetic Nanoparticles for Tracking Inflammation in the Epileptic Rat Brain
2019 ◽
Vol 16
(7)
◽
pp. 637-644
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Keyword(s):
Ex Vivo
◽