Interaction between oxytocin and 'sidaverin' on the gravid and non-gravid rat uterus

Interaction between oxytocin and 'sidaverin' on the gravid and non-gravid rat uterus
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DOI:
10.1016/s1043-6618(95)80014-x
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发表时间:
1995-07-01
影响因子:
9.3
通讯作者:
Lutterodt, GD
Lutterodt, GD
中科院分区:
医学1区
文献类型:
--
作者:
Lutterodt, GD

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西达维林(Sidaverin)是一种从西达veronicaefolia (Lam)极性部分提取的结晶化合物,在未妊娠的大鼠离体子宫制剂中引起催产素样收缩,并呈浓度-反应关系。使用匹配的反应,催产素和西达维林的等效浓度分别约为0.16 U和0.4 μ g ml(-1)。西达弗林诱导的收缩反应是阿托品可逆的。西达弗林和催产素的浓度-反应曲线平行,两种反应均被特异性催产素拮抗剂阿托西班抑制,提示催产素受体可能参与了西达弗林的作用。不管给药顺序如何,一种药物对另一种药物的作用都有增强作用,甚至在把第一种药物洗掉之后再给第二种药物。在妊娠子宫中,西达弗林在第1天至第6天或第7天使制剂产生收缩,在第7-11天引起松弛,并在第11天至足月期间引起收缩,制剂的敏感性随足月呈指数增长,持续强烈的收缩。除第7-11天外,当西达弗林拮抗催产素作用时,它增强了催产素对子宫的作用。(C) 1995年意大利药理学学会
Sidaverin, a crystalline compound extracted from a polar fraction of Sida veronicaefolia (Lam), elicited oxytocin-like contractions in the non-gravid rat isolated uterus preparation with a concentration-response relationship. Equipotent concentrations of oxytocin and sidaverin, using matched responses, were approximately 0.16 U and 0.4 mu g ml(-1), respectively. Sidaverin-induced contractile response was atropine reversible. The concentration-response curves for sidaverin and oxytocin were parallel, and both responses were inhibited by the specific oxytocin antagonist, Atosiban, indicating possible involvement of oxytocin receptors in the action of sidaverin. There were potentiation of action of one drug to that of the other, irrespective of the order of administration and even after washing off the first before introducing the second drug. In the gravid uterus, sidaverin produced contractions in preparations from day 1 to day 6 or 7, caused relaxation in days 7-11, and elicited contractions in day 11 through term, the sensitivity of the preparations increasing exponentially toward term with strong sustained contractions. With the exception of days 7-11, when sidaverin antagonized oxytocin action, it potentiated action of oxytocin on the gravid uterus. (C) 1995 The Italian Pharmacological Society