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The strong contractile effect of the thromboxane receptor agonist U-46619 in isolated human pulmonary arteries and its competitive antagonism by BM-13.505

Sjöberg, Trygve LU and Steen, Stig LU (1989) In Acta Physiologica Scandinavica 136(2). p.161-165
Abstract
Ring segments (I mm in diameter) of the pulmonary artery obtained from 16 patients undergoing thoracic surgery were mounted in tissue baths. Cumulative concentration-response curves of some prostanoids and amines were obtained, and Emax and pEC50 values calculated. Noradrenaline, phenylephrine, clonidine and serotonin (5-HT) showed low intrinsic activities. Prostaglandin F2 alpha (PGF2 alpha) induced strong contractions with an Emax of 126% of the preceding K+ (124 mM)-induced contraction, but its potency was low (pEC50 = 5.70). The thromboxane receptor agonists U-46619 and U-44069 induced strong contractions (Emax = 139% and 133% respectively) and were significantly more potent than the other drugs used (pEC50 = 8.43 and 8.30... (More)
Ring segments (I mm in diameter) of the pulmonary artery obtained from 16 patients undergoing thoracic surgery were mounted in tissue baths. Cumulative concentration-response curves of some prostanoids and amines were obtained, and Emax and pEC50 values calculated. Noradrenaline, phenylephrine, clonidine and serotonin (5-HT) showed low intrinsic activities. Prostaglandin F2 alpha (PGF2 alpha) induced strong contractions with an Emax of 126% of the preceding K+ (124 mM)-induced contraction, but its potency was low (pEC50 = 5.70). The thromboxane receptor agonists U-46619 and U-44069 induced strong contractions (Emax = 139% and 133% respectively) and were significantly more potent than the other drugs used (pEC50 = 8.43 and 8.30 respectively). The thromboxane receptor antagonist BM-13.505 (10(-8) to 10(-6) M) caused rightward parallel shifts of the U-46619 concentration-response curves without reduction of Emax, indicating competitive antagonism. (Less)
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Contribution to journal
publication status
published
subject
in
Acta Physiologica Scandinavica
volume
136
issue
2
pages
161 - 165
publisher
Wiley-Blackwell
external identifiers
  • pmid:2528885
  • scopus:0024312669
ISSN
0001-6772
language
English
LU publication?
yes
id
00557926-713a-451f-9617-3c1d79454dd3 (old id 1104844)
date added to LUP
2016-04-01 17:03:54
date last changed
2021-08-29 04:19:59
@article{00557926-713a-451f-9617-3c1d79454dd3,
  abstract     = {{Ring segments (I mm in diameter) of the pulmonary artery obtained from 16 patients undergoing thoracic surgery were mounted in tissue baths. Cumulative concentration-response curves of some prostanoids and amines were obtained, and Emax and pEC50 values calculated. Noradrenaline, phenylephrine, clonidine and serotonin (5-HT) showed low intrinsic activities. Prostaglandin F2 alpha (PGF2 alpha) induced strong contractions with an Emax of 126% of the preceding K+ (124 mM)-induced contraction, but its potency was low (pEC50 = 5.70). The thromboxane receptor agonists U-46619 and U-44069 induced strong contractions (Emax = 139% and 133% respectively) and were significantly more potent than the other drugs used (pEC50 = 8.43 and 8.30 respectively). The thromboxane receptor antagonist BM-13.505 (10(-8) to 10(-6) M) caused rightward parallel shifts of the U-46619 concentration-response curves without reduction of Emax, indicating competitive antagonism.}},
  author       = {{Sjöberg, Trygve and Steen, Stig}},
  issn         = {{0001-6772}},
  language     = {{eng}},
  number       = {{2}},
  pages        = {{161--165}},
  publisher    = {{Wiley-Blackwell}},
  series       = {{Acta Physiologica Scandinavica}},
  title        = {{The strong contractile effect of the thromboxane receptor agonist U-46619 in isolated human pulmonary arteries and its competitive antagonism by BM-13.505}},
  volume       = {{136}},
  year         = {{1989}},
}