Akerlund M, Hauksson A, Lundin S, Melin P, Trojnar J
Br J Obstet Gynaecol. 1986 Jan;93(1):22-7. doi: 10.1111/j.1471-0528.1986.tb07807.x.
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.
对三种垂体后叶激素类似物，即1-去氨基-2-D-酪氨酸（乙酯）-4-缬氨酸-8-鸟氨酸-加压素（dE-VVT）、1-去氨基-2-D-酪氨酸（乙酯）-4-苏氨酸-8-鸟氨酸-加压素（dE-TVT）和1-去氨基-2-D-酪氨酸（乙酯）-催产素（dE-OXY），在健康女性中对血管加压素（VP）诱导的子宫活动的抑制作用进行了比较。在月经期间，记录子宫内压力时（11名女性进行了18次记录），静脉输注赖氨酸加压素（LVP，1纳克/分钟/千克体重）会导致子宫活动增加和痛经样症状。静脉注射所有类似物（10微克/千克体重）均可缓解症状并抑制子宫活动，dE-TVT最有效，dE-OXY活性最低。注射dE-TVT后，在最初10分钟内几乎完全抑制了子宫收缩。该类似物的作用持续时间也最长（40 - 50分钟）。只有dE-OXY对子宫自发活动有激动作用。静脉注射dE-TVT（10纳克/千克体重）的药代动力学研究表明，血浆半衰期约为16分钟，清除率为30升/小时。经鼻给予100纳克/千克的生物利用度约为5.5%。建议进一步研究。
