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Inhibitory effect of barusiban and atosiban on oxytocin-induced contractions of myometrium from preterm and term pregnant women

Pierzynski, P; Lemancewicz, A; Reinheimer, T; Åkerlund, Mats LU and Laudanski, T (2004) In Journal of the Society for Gynecologic Investigation 11(6). p.384-387
Abstract
BACKGROUND: A synthetic oxytocin analogue, barusiban, was shown to potently inhibit oxytocin-induced activity of myometrium from term pregnant women. The responsiveness to vasopressin was not influenced by the compound. OBJECTIVE: To test the effect of barusiban and a reference compound, atosiban, on oxytocin-induced activity of myometrium from women at preterm pregnancy in comparison to myometrium from women at term. METHODS: Fifteen preterm (30-36 gestational weeks) and 12 term pregnant women (38-41 weeks) who underwent cesarean delivery donated myometrial tissue for the study. Concentration-response curves following oxytocin, administration to isolated myometrial strips were recorded in control experiments, in the presence of barusiban... (More)
BACKGROUND: A synthetic oxytocin analogue, barusiban, was shown to potently inhibit oxytocin-induced activity of myometrium from term pregnant women. The responsiveness to vasopressin was not influenced by the compound. OBJECTIVE: To test the effect of barusiban and a reference compound, atosiban, on oxytocin-induced activity of myometrium from women at preterm pregnancy in comparison to myometrium from women at term. METHODS: Fifteen preterm (30-36 gestational weeks) and 12 term pregnant women (38-41 weeks) who underwent cesarean delivery donated myometrial tissue for the study. Concentration-response curves following oxytocin, administration to isolated myometrial strips were recorded in control experiments, in the presence of barusiban at concentrations of 2.5, 25, and 250 nM, and of atosiban at concentrations of 25, 250, and 750 nM. Effective concentration 50% (EC50) and pA(2) values were calculated. RESULTS: Both antagonists in higher concentrations increased the EC50 values to oxytocin. The median pA(2) value for preterm myometrium with barusiban was 9.76 and with atosiban 7.86. For term myometrium the corresponding pA(2), results were 9.89 and 7.8 1, respectively. None of these pA(2) values differed to any statistically significant degree. CONCLUSION: The selective oxytocin antagonist, barusiban, concentration-dependently inhibits oxytocin-induced myometrial contractions of both preterm and term myometrium at least as potently as atosiban. It remains to be determined if the selectivity of barusiban for the oxytocin receptor confers an advantage over atosiban as a tocolytic in preterm labor. Copyright (C) 2004 by the Society for Gynecologic Investigation. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
value, pA(2), human myometrial activity, oxytocin, receptor antagonist, barusiban, atosiban
in
Journal of the Society for Gynecologic Investigation
volume
11
issue
6
pages
384 - 387
publisher
SAGE Publications Inc.
external identifiers
  • pmid:15350251
  • wos:000224009000007
  • scopus:4444296991
ISSN
1071-5576
DOI
10.1016/j.jsgi.2004.02.008
language
English
LU publication?
yes
id
83f12564-f059-4d2e-aaa2-a54930d446d8 (old id 266298)
date added to LUP
2007-10-30 07:16:11
date last changed
2017-12-10 04:27:24
@article{83f12564-f059-4d2e-aaa2-a54930d446d8,
  abstract     = {BACKGROUND: A synthetic oxytocin analogue, barusiban, was shown to potently inhibit oxytocin-induced activity of myometrium from term pregnant women. The responsiveness to vasopressin was not influenced by the compound. OBJECTIVE: To test the effect of barusiban and a reference compound, atosiban, on oxytocin-induced activity of myometrium from women at preterm pregnancy in comparison to myometrium from women at term. METHODS: Fifteen preterm (30-36 gestational weeks) and 12 term pregnant women (38-41 weeks) who underwent cesarean delivery donated myometrial tissue for the study. Concentration-response curves following oxytocin, administration to isolated myometrial strips were recorded in control experiments, in the presence of barusiban at concentrations of 2.5, 25, and 250 nM, and of atosiban at concentrations of 25, 250, and 750 nM. Effective concentration 50% (EC50) and pA(2) values were calculated. RESULTS: Both antagonists in higher concentrations increased the EC50 values to oxytocin. The median pA(2) value for preterm myometrium with barusiban was 9.76 and with atosiban 7.86. For term myometrium the corresponding pA(2), results were 9.89 and 7.8 1, respectively. None of these pA(2) values differed to any statistically significant degree. CONCLUSION: The selective oxytocin antagonist, barusiban, concentration-dependently inhibits oxytocin-induced myometrial contractions of both preterm and term myometrium at least as potently as atosiban. It remains to be determined if the selectivity of barusiban for the oxytocin receptor confers an advantage over atosiban as a tocolytic in preterm labor. Copyright (C) 2004 by the Society for Gynecologic Investigation.},
  author       = {Pierzynski, P and Lemancewicz, A and Reinheimer, T and Åkerlund, Mats and Laudanski, T},
  issn         = {1071-5576},
  keyword      = {value,pA(2),human myometrial activity,oxytocin,receptor antagonist,barusiban,atosiban},
  language     = {eng},
  number       = {6},
  pages        = {384--387},
  publisher    = {SAGE Publications Inc.},
  series       = {Journal of the Society for Gynecologic Investigation},
  title        = {Inhibitory effect of barusiban and atosiban on oxytocin-induced contractions of myometrium from preterm and term pregnant women},
  url          = {http://dx.doi.org/10.1016/j.jsgi.2004.02.008},
  volume       = {11},
  year         = {2004},
}