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Antagonism of thromboxane receptor induced contractions in isolated human groin lymphatics

Sjöberg, Trygve LU ; Andersson, K E; Norgren, Lars LU and Steen, Stig LU (1989) In Lymphology 22(3). p.135-140
Abstract
In vitro studies were performed on lymphatics obtained from the groin in 19 patients undergoing vascular surgery. The lymphatics were mounted in tissue baths, and isometric contractions were induced by increasing concentrations of the thromboxane A2 (TXA2) mimetic U-46619. In comparison to K+ (124mM)-induced contraction, which were used as an internal standard, the response to U-46619 had an Emax of 105 +/- 5.9%. The pEC50-value was 8.14 +/- 0.09. The effects of two thromboxane receptor (TP-receptor) antagonists, L-636,499 and BM-13,505, were investigated. Both antagonists caused concentration-dependent right-ward shifts without depression of Emax of the U-46619 concentration-response curves. The slopes of the regression lines in a Schild... (More)
In vitro studies were performed on lymphatics obtained from the groin in 19 patients undergoing vascular surgery. The lymphatics were mounted in tissue baths, and isometric contractions were induced by increasing concentrations of the thromboxane A2 (TXA2) mimetic U-46619. In comparison to K+ (124mM)-induced contraction, which were used as an internal standard, the response to U-46619 had an Emax of 105 +/- 5.9%. The pEC50-value was 8.14 +/- 0.09. The effects of two thromboxane receptor (TP-receptor) antagonists, L-636,499 and BM-13,505, were investigated. Both antagonists caused concentration-dependent right-ward shifts without depression of Emax of the U-46619 concentration-response curves. The slopes of the regression lines in a Schild plot for both antagonists did not differ from one, indicating competitive antagonism. The pA2-value of BM-13,505 (7.89) was 65 times higher than that of L-636,499 (6.08). The results suggest that the receptor involved in the prostanoid contraction in human groin lymphatics is of the TP-subtype. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Lymphology
volume
22
issue
3
pages
135 - 140
publisher
International Society of Lymphology
external identifiers
  • pmid:2532276
  • scopus:0024457591
ISSN
0024-7766
language
English
LU publication?
yes
id
a6054b33-54ee-48e1-aec1-31d67794112b (old id 1104838)
date added to LUP
2008-08-06 15:58:29
date last changed
2017-01-01 06:38:41
@article{a6054b33-54ee-48e1-aec1-31d67794112b,
  abstract     = {In vitro studies were performed on lymphatics obtained from the groin in 19 patients undergoing vascular surgery. The lymphatics were mounted in tissue baths, and isometric contractions were induced by increasing concentrations of the thromboxane A2 (TXA2) mimetic U-46619. In comparison to K+ (124mM)-induced contraction, which were used as an internal standard, the response to U-46619 had an Emax of 105 +/- 5.9%. The pEC50-value was 8.14 +/- 0.09. The effects of two thromboxane receptor (TP-receptor) antagonists, L-636,499 and BM-13,505, were investigated. Both antagonists caused concentration-dependent right-ward shifts without depression of Emax of the U-46619 concentration-response curves. The slopes of the regression lines in a Schild plot for both antagonists did not differ from one, indicating competitive antagonism. The pA2-value of BM-13,505 (7.89) was 65 times higher than that of L-636,499 (6.08). The results suggest that the receptor involved in the prostanoid contraction in human groin lymphatics is of the TP-subtype.},
  author       = {Sjöberg, Trygve and Andersson, K E and Norgren, Lars and Steen, Stig},
  issn         = {0024-7766},
  language     = {eng},
  number       = {3},
  pages        = {135--140},
  publisher    = {International Society of Lymphology},
  series       = {Lymphology},
  title        = {Antagonism of thromboxane receptor induced contractions in isolated human groin lymphatics},
  volume       = {22},
  year         = {1989},
}