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钙在前列腺素E1和F2α及其拮抗剂聚磷酸根皮苷(PPP)作用机制中的作用。

Role of calcium in the mechanism of action of the prostaglandins E1 and F2 alpha as well as of their antagonist polyphloretin phosphate (PPP).

作者信息

Petkov V, Radomirov R, Petkov O

出版信息

Acta Physiol Pharmacol Bulg. 1978;4(4):27-35.

PMID:752228
Abstract

The contractile effect of PGE1 on guinea-pig ileum is not changed either by increase (to 4 mM) or by decrease (to 1 mM) of the Ca++ content in Krebs solution. The decrease of Ca++ in the medium intensifies the contractile effect of PGE2 alpha. Reduction of Ca++ weakens the antagonistic effect of PPP (100 micrograms/ml) against PGF2 alpha. PPP has a marked aftereffect with respect to the effects of PGF2 alpha--in cases of normal Ca++ content in the Krebs solution this aftereffect appears upon longer (10 min) contact of PPP with the intestinal segment, while in cases of changed Ca++ content it appears already after 2-min PPP action. It is concluded that in order to induce contractions in the guinea-pig ileum, PGE1 and PGF2 alpha utilize the internal Ca++. It is assumed that PGF2 alpha increases the reactivity of the anionic sites of the smooth-muscle membrane for Ca++. As a result of this, the complex compounds of Ca++ at its higher concentration make more difficult the realization of the contractile process. It is assumed that Ca++ is needed for the maximum manifestation of the antagonistic effect of PPP.

摘要

前列腺素E1(PGE1)对豚鼠回肠的收缩作用,并不会因克雷布斯溶液中钙离子(Ca++)含量增加(至4毫摩尔)或减少(至1毫摩尔)而发生改变。培养基中Ca++含量降低会增强前列腺素E2α(PGE2α)的收缩作用。Ca++含量减少会削弱苯哌丙烷(PPP,100微克/毫升)对前列腺素F2α(PGF2α)的拮抗作用。就PGF2α的作用而言,PPP具有显著的后效应——在克雷布斯溶液中Ca++含量正常的情况下,PPP与肠段接触较长时间(10分钟)后会出现这种后效应,而在Ca++含量改变的情况下,PPP作用2分钟后就会出现。得出的结论是,为了在豚鼠回肠中诱导收缩,PGE1和PGF2α利用的是细胞内的Ca++。据推测,PGF2α会增加平滑肌膜阴离子位点对Ca++的反应性。由此导致,Ca++浓度较高时形成的复合化合物会使收缩过程的实现更加困难。据推测,要使PPP的拮抗作用充分显现,需要Ca++的参与。

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