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Chemical Compound Review

Atosiban     (2S)-N-[(1S)-4-amino-1...

Synonyms: Antocin, Atosibanum, deTVT, dE-TVT, d(TVT), ...
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Disease relevance of Atosiban

  • Moreover, atosiban, by acting on a G(i)-mediated pathway(,) inhibits cell growth of HEK293 and Madin-Darby canine kidney cells stably transfected with OTRs and of DU145 prostate cancer cells expressing endogenous OTRs [1].
  • Barusiban, a new highly potent and long-acting oxytocin antagonist: pharmacokinetic and pharmacodynamic comparison with atosiban in a cynomolgus monkey model of preterm labor [2].
  • A significant increase in the incidence of fetal deaths was found, however, when rats were treated with a combination of atosiban and ICI-118.551 [3].
  • The oxytocin receptor antagonists, atosiban and L-371257, potently and concentration-dependently inhibited oxytocin-induced [Ca(2+)](i) increase and hyperplasia [4].
  • Moreover, intrathecal administration of atosiban alone induced a hyperalgesia in rats with inflammation, indicating that endogenous oxytocin is involved in the transmission and regulation of nociceptive information in the spinal cord of rats with inflammation [5].

Psychiatry related information on Atosiban

  • Finally, the oxytocin blocker, atosiban, reduced both operant and reflexive social behavior [6].
  • Findings to date implicate vasopressin in the behavioral changes in males, that in later life followed a single exposure to an oxytocin antagonist, and suggest caution in the clinical use of agents such as Atosiban, which may have the potential to influence infant development [7].
  • Satiation scores areas in healthy subjects after receiving atosiban or oxytocin did not show any significant differences [8].

High impact information on Atosiban

  • The oxytocin receptor antagonist atosiban inhibits cell growth via a "biased agonist" mechanism [1].
  • Notably, atosiban leads to persistent ERK1/2 activation and p21(WAF1/CIP1) induction, the same signaling events leading to oxytocin-mediated cell growth inhibition via a G(i) pathway [1].
  • Finally, atosiban exposure did not cause OTR internalization and led to only a modest decrease (20%) in the number of high affinity cell membrane OTRs, two observations consistent with the finding that atosiban did not lead to any desensitization of the oxytocin-induced activation of the G(q)-phospholipase C pathway [1].
  • Here, we report that atosiban, an oxytocin derivative that acts as a competitive antagonist on OTR/G(q) coupling, displays agonistic properties on OTR/G(i) coupling, as shown by specific (35)S-labeled guanosine 5'-3-O-(thio) trisphosphate ([(35)S]GTPgammaS) binding [1].
  • Because oxytocin (OT) is likely to be involved causally in PTL, this study compared two OT receptor antagonists, barusiban and atosiban, for their tocolytic effects [2].

Chemical compound and disease context of Atosiban


Biological context of Atosiban


Anatomical context of Atosiban

  • No fetal adverse effects were seen with atosiban and, in particular, no effect on baseline fetal heart rate, unlike with the beta-adrenoceptor agonists [17].
  • The OTR down-regulation seen after atosiban treatment adds to the direct relaxing effect of atosiban on the myometrium [3].
  • Transplacental passage of atosiban from mother to fetus was assessed at cesarean section under halothane anesthesia in four baboons and in two chronically instrumented fetuses in the absence of anesthesia [16].
  • 1. In myometrial strips from near-term non-labouring human uterus, addition of oxytocin (OT) evoked dose-dependent (10 - 3000 nM) phasic contractions that were antagonized by atosiban (1 microM) and relaxed by addition of the nitric oxide donor S-nitroso L-cysteine (Cys-NO) [18].
  • Similarly, no changes in fetal blood pressure and arterial blood gases were present during the infusion of the atosiban [19].

Associations of Atosiban with other chemical compounds


Gene context of Atosiban

  • Administration of an OT receptor antagonist (Atosiban, d[Dtyr(Et)(2), Thr(4)]ornithine vasotocin) 100 ng icv, to female OT+/+ mice increased anxiety-related behavior by decreasing the percentage of entries (P < 0.01) and time spent (P < 0.04) in the open arms compared with artificial cerebrospinal fluid-treated controls [24].
  • Infusion of the OTR antagonist atosiban down-regulated OTR binding sites in the parturient myometrium and resulted in an impaired contractile response to OT without affecting gestational length [3].
  • Peptides 1-4 and B exhibit respectively 449, 263, 1091, 546 and 129 times greater affinity for the hOTR than atosiban (K(i) = 76.4 nM) [25].
  • The peptide oxytocin (OT) antagonist atosiban, approved for tocolytic use in Europe (under the tradename Tractocile), represents an important new therapeutic advance for the treatment of premature labor [25].
  • 6. Despite predominant involvement of V1A receptors in both vessels, the different Hill slopes of AVP and OT E/[A] curves as well as the steepening of the AVP E/[A] curves by atosiban are indicative of receptor heterogeneity in the rat SMA [20].

Analytical, diagnostic and therapeutic context of Atosiban

  • Animal experiments and pilot clinical studies have examined several agents and, of these, atosiban has been the object of extensive clinical trials [17].
  • In large multicentre studies comparing atosiban with beta-adrenoceptor agonists, the efficacy of the two medications was similar for pregnancy prolongation for 48 hours and for 7 days [17].
  • Given that all patients in this study were eligible for tocolysis and that, in practice, nearly all patients who are eligible for a tocolytic receive one, the benefit of using atosiban is the placebo-like maternal-fetal side effect profile [26].
  • Continuous intravenous infusion of Atosiban (1 mg kg-1 day-1) for 3 or 7 days from day 24 of the 26.5 day gestation significantly delayed births [23].
  • The percentages of patients remaining undelivered and not requiring an alternate tocolytic at 24 hours, 48 hours, and 7 days were significantly higher in the atosiban group than in the control group (all P < or =.008) [26].


  1. The oxytocin receptor antagonist atosiban inhibits cell growth via a "biased agonist" mechanism. Reversi, A., Rimoldi, V., Marrocco, T., Cassoni, P., Bussolati, G., Parenti, M., Chini, B. J. Biol. Chem. (2005) [Pubmed]
  2. Barusiban, a new highly potent and long-acting oxytocin antagonist: pharmacokinetic and pharmacodynamic comparison with atosiban in a cynomolgus monkey model of preterm labor. Reinheimer, T.M., Bee, W.H., Resendez, J.C., Meyer, J.K., Haluska, G.J., Chellman, G.J. J. Clin. Endocrinol. Metab. (2005) [Pubmed]
  3. Effect of oxytocin receptor and beta2-adrenoceptor blockade on myometrial oxytocin receptors in parturient rats. Engstrøm, T., Bratholm, P., Vilhardt, H., Christensen, N.J. Biol. Reprod. (1999) [Pubmed]
  4. Pharmacologic characterization of the oxytocin receptor in human uterine smooth muscle cells. Tahara, A., Tsukada, J., Tomura, Y., Wada, K., Kusayama, T., Ishii, N., Yatsu, T., Uchida, W., Tanaka, A. Br. J. Pharmacol. (2000) [Pubmed]
  5. Involvement of oxytocin in spinal antinociception in rats with inflammation. Yu, S.Q., Lundeberg, T., Yu, L.C. Brain Res. (2003) [Pubmed]
  6. Social and sexual motivation in the mouse. Matthews, T.J., Abdelbaky, P., Pfaff, D.W. Behav. Neurosci. (2005) [Pubmed]
  7. Sex differences and developmental effects of manipulations of oxytocin on alloparenting and anxiety in prairie voles. Bales, K.L., Pfeifer, L.A., Carter, C.S. Developmental psychobiology. (2004) [Pubmed]
  8. The oxytocin/vasopressin receptor antagonist atosiban delays the gastric emptying of a semisolid meal compared to saline in human. Ohlsson, B., Björgell, O., Ekberg, O., Darwiche, G. BMC gastroenterology [electronic resource]. (2006) [Pubmed]
  9. Double-blind, randomized, controlled trial of atosiban and ritodrine in the treatment of preterm labor: a multicenter effectiveness and safety study. Moutquin, J.M., Sherman, D., Cohen, H., Mohide, P.T., Hochner-Celnikier, D., Fejgin, M., Liston, R.M., Dansereau, J., Mazor, M., Shalev, E., Boucher, M., Glezerman, M., Zimmer, E.Z., Rabinovici, J. Am. J. Obstet. Gynecol. (2000) [Pubmed]
  10. Inhibition of premature labor in sheep by a combined treatment of nimesulide, a prostaglandin synthase type 2 inhibitor, and atosiban, an oxytocin receptor antagonist. Grigsby, P.L., Poore, K.R., Hirst, J.J., Jenkin, G. Am. J. Obstet. Gynecol. (2000) [Pubmed]
  11. Intrauterine pressure, ischemia markers, and experienced pain during administration of a vasopressin V1a receptor antagonist in spontaneous and vasopressin-induced dysmenorrhea. Liedman, R., Grant, L., Igidbashian, S., James, I., McLeod, A., Skillern, L., Akerlund, M. Acta obstetricia et gynecologica Scandinavica. (2006) [Pubmed]
  12. Involvement of oxytocin and vasopressin in the pathophysiology of preterm labor and primary dysmenorrhea. Akerlund, M. Prog. Brain Res. (2002) [Pubmed]
  13. Atosiban and nifedipine in acute tocolysis: A comparative study. Al-Omari, W.R., Al-Shammaa, H.B., Al-Tikriti, E.M., Ahmed, K.W. Eur. J. Obstet. Gynecol. Reprod. Biol. (2006) [Pubmed]
  14. The oxytocin antagonist atosiban prevents androstenedione-induced myometrial contractions in the chronically instrumented, pregnant rhesus monkey. Giussani, D.A., Jenkins, S.L., Mecenas, C.A., Winter, J.A., Barbera, M., Honnebier, O.M., Nathanielsz, P.W. Endocrinology (1996) [Pubmed]
  15. 2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 2. Synthesis, chirality, and pharmacokinetics. Borthwick, A.D., Davies, D.E., Exall, A.M., Livermore, D.G., Sollis, S.L., Nerozzi, F., Allen, M.J., Perren, M., Shabbir, S.S., Woollard, P.M., Wyatt, P.G. J. Med. Chem. (2005) [Pubmed]
  16. Effect of the oxytocin antagonist atosiban (1-deamino-2-D-tyr(OET)-4-thr-8-orn-vasotocin/oxytocin) on nocturanl myometrial contractions, maternal cardiovascular function, transplacental passage, and fetal oxygenation in the pregnant baboon during the last third of gestation. Nathanielsz, P.W., Honnebier, M.B., Mecenas, C., Jenkins, S.L., Holland, M.L., Demarest, K. Biol. Reprod. (1997) [Pubmed]
  17. Atosiban for preterm labour. Tsatsaris, V., Carbonne, B., Cabrol, D. Drugs (2004) [Pubmed]
  18. NO-induced relaxation of labouring and non-labouring human myometrium is not mediated by cyclic GMP. Buxton, I.L., Kaiser, R.A., Malmquist, N.A., Tichenor, S. Br. J. Pharmacol. (2001) [Pubmed]
  19. Maternal and fetal cardiovascular effects and placental transfer of the oxytocin antagonist atosiban in late-gestation pregnant sheep. Greig, P.C., Massmann, G.A., Demarest, K.T., Weglein, R.C., Holland, M.L., Figueroa, J.P. Am. J. Obstet. Gynecol. (1993) [Pubmed]
  20. Characterization of receptors mediating contraction of the rat isolated small mesenteric artery and aorta to arginine vasopressin and oxytocin. Stam, W.B., Van der Graaf, P.H., Saxena, P.R. Br. J. Pharmacol. (1998) [Pubmed]
  21. Effect of oxytocin receptor blockade on rat myometrial responsiveness to prostaglandin f(2)(alpha). Engstrøm, T., Bratholm, P., Christensen, N.J., Vilhardt, H. Biol. Reprod. (2000) [Pubmed]
  22. Receptor binding of oxytocin and vasopressin antagonists and inhibitory effects on isolated myometrium from preterm and term pregnant women. Akerlund, M., Bossmar, T., Brouard, R., Kostrzewska, A., Laudanski, T., Lemancewicz, A., Serradeil-Le Gal, C., Steinwall, M. British journal of obstetrics and gynaecology. (1999) [Pubmed]
  23. Infusion with an oxytocin receptor antagonist delays parturition in a marsupial. Renfree, M.B., Parry, L.J., Shaw, G. J. Reprod. Fertil. (1996) [Pubmed]
  24. Female oxytocin-deficient mice display enhanced anxiety-related behavior. Mantella, R.C., Vollmer, R.R., Li, X., Amico, J.A. Endocrinology (2003) [Pubmed]
  25. Design of peptide oxytocin antagonists with strikingly higher affinities and selectivities for the human oxytocin receptor than atosiban. Manning, M., Cheng, L.L., Stoev, S., Wo, N.C., Chan, W.Y., Szeto, H.H., Durroux, T., Mouillac, B., Barberis, C. J. Pept. Sci. (2005) [Pubmed]
  26. An oxytocin receptor antagonist (atosiban) in the treatment of preterm labor: a randomized, double-blind, placebo-controlled trial with tocolytic rescue. Romero, R., Sibai, B.M., Sanchez-Ramos, L., Valenzuela, G.J., Veille, J.C., Tabor, B., Perry, K.G., Varner, M., Goodwin, T.M., Lane, R., Smith, J., Shangold, G., Creasy, G.W. Am. J. Obstet. Gynecol. (2000) [Pubmed]
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