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Functional estimation of endothelin-1 receptor antagonism by bosentan， macitentan and ambrisentan in human pulmonary and radial arteries in vitro

Eur. J. Pharmacol.. 2017-06; 
AngusJames A, SoedingPaul F, HughesRichard J A, WrightChristi
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Biochemicals … Drugs used were: acetylcholine bromide (Sigma, St Louis, MO, USA); ambrisentan (a gift from GSK, Stevenage, UK); bosentan sodium salt (a gift from Actelion Pharmaceutical Ltd., Allschwil, Switzerland); endothelin-1 (Genscript, Piscataway, NJ, USA); macitentan (a gift from … Get A Quote

摘要

Endothelin receptor antagonists are approved for pulmonary arterial hypertension. Development of selective ET-receptor antagonists over mixed or dual receptor antagonists has depended on a range of receptor binding assays， second messenger assays and functional blood vessel assays. This study compared the 3 clinically-approved endothelin receptor antagonists in assays of human isolated pulmonary and radial arteries in vitro.

关键词

Ambrisentan，Ambrisentan (PubChem CID: 6918493)，Bosentan，ET(1)-receptors，Endothelin-1，Human pulmonary artery，Human radial artery，Macitentan，and macitentan (PubChem CID: 16004692)，bosentan sodium (PubChem CID: 44387533)，endothelin-1 (PubChem CID: 16132
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