Contraction of human airway smooth muscle by endothelin-1 and IRL 1620: effect of bosentan.
作者： Tsuneyuki Takahashi , Peter J Barnes , Ivana Kawikova , Magdi H Yacoub , Timothy D Warner
DOI: 10.1016/S0014-2999(97)10008-5
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摘要: Abstract We have examined whether 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2,2′-bipyrimidin-4-yl]-benzenesulfonamide (bosentan; endothelin ETA/B receptor antagonist) and (R)2-[(R)-2-[(S)-2-[[1-(hexahydro-1H-azepinyl)]carbonyl] amino-4-methylpentanoil]amino-3-[3-(1-methyl-1H-indoyl)]propionyl]amino-3-(2-pyridyl) propionic acid (FR 139317; ETA inhibit contractions of human airway smooth muscle induced by endothelin-1 or Suc-[Glu9,Ala11,15]enthothelin-1-(8–21) (IRL 1620; ETB agonist). Endothelin-1 IRL 1620 were equipotent. Bosentan FR 139317 (each 10 μM) produced a small shift in response curves to (1.6- 1.5-fold, respectively). However, bosentan was more potent against elicited (10 μM, 11.2-fold shift) suggesting that these agonists exhibit different kinetic interactions with receptors implying an interaction novel subtype airways.
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