Vasotocin analogues which competitively inhibit vasopressin stimulated uterine activity in healthy women.

Abstract

Three analogues of posterior pituitary hormones, 1-deamino-2-D-Tyr(OEt)-4-Val-8-Orn-vasotocin(dE-VVT), 1-deamino-2-D-Tyr(OEt)-4-Thr-8-Orn-vasotocin(dE-TVT) and 1-deamino-2-D-Tyr(OEt)-oxytocin(dE-OXY) were compared for their inhibitory effects on vasopressin (VP)-induced uterine activity in healthy women. At menstruation, during recording of intrauterine pressure (18 recording sessions in 11 women), intravenous infusion of lysine vasopressin (LVP, 1 ng/min/kg/body weight) induced an increase of the uterine activity and dysmenorrhoea-like symptoms. Intravenous injections of all analogues (10 micrograms/kg body weight) caused relief of symptoms and inhibition of uterine activity, dE-TVT was the most effective and dE-OXY was least active. With dE-TVT almost complete inhibition of contractions was seen during the first 10 min after injection. The duration of effect was also greatest with that analogue (40-50 min). Only dE-OXY had an agonist effect on spontaneous uterine activity. Pharmacokinetic studies of intravenous dE-TVT (10 ng/kg body weight) showed that the plasma half-life was approximately 16 min and the clearance 30 l/h. The bioavailability of 100 ng/kg given intranasally was about 5.5%. Further studies are recommended.

• Authors: M Akerlund, A Hauksson, S Lundin, P Melin, J Trojnar
• Journal: British journal of obstetrics and gynaecology (Br J Obstet Gynaecol) Vol. 93 Issue 1 Pg. 22-7 (Jan 1986) ISSN: 0306-5456 [Print] England
• PMID: 3942702 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• atosiban
• vasotocin, 1-desamino-OEt-Tyr(2)-Val(4)-Orn(8)-
• Oxytocin
• Lypressin
• oxytocin, 1-desamino-(O-Et-Tyr)(2)-
• Vasotocin

Topics

• Adult
• Biological Availability
• Female
• Half-Life
• Humans
• Injections, Intravenous
• Kinetics
• Lypressin (pharmacology)
• Male
• Menstruation (drug effects)
• Oxytocin (analogs & derivatives, pharmacology)
• Uterine Contraction (drug effects)
• Uterus (drug effects)
• Vasotocin (analogs & derivatives, pharmacology)