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聚磷酸根皮素通过干扰E型前列腺素降低缓激肽的致痛作用。

Polyphloretin phosphate reduces the algesic action of bradykinin by interfering with E-type prostaglandins.

作者信息

Juan H, Lembeck F

出版信息

Agents Actions. 1976 Sep;6(5):646-50. doi: 10.1007/BF01971585.

Abstract

(1) The method of the isolated perfused rabbit ear connected to the body by its nerve only was used to investigate the influence of the prostaglandin-antagonist polyphloretin phosphate (PPP) on the algesic effect of bradykinin (B) and acetylcholine (ACh). (2) Intra-arterial injections of B and ACh into the ear elicit a reflex fall in systemic blood pressure of the anaesthetized animal. PPP reduces this effects of B in proportion to the dose. The effect of ACh is reduced only to a small extent and only under higher concentrations of PPP than those necessary for inhibiting the effect of B. (3) Prostaglandin E1 (PGE1), when infused i.a. into the ear, enhances the effect of B and ACh by a sensitizing action on the perivascular pain receptors. PPP reduces or totally abolishes the PGE1-induced enhancement of the effect of B and ACh. (4) It is concluded that PPP reduces the effect of B mainly by inhibiting directly the pain enhancing action of the endogenously released PGs of the E-type. The effect of ACh is reduced only in the high concentration of PPP to a small extent probably by inhibiting the ACh-action rather than the sensitizing action of the only minimal released amounts of PGs. The PG-antagonizing action of PPP is further proven by the fact that during an additional infusion of PGE1 the enhanced effects of both B as well as ACh are reduced or abolished by PPP.

摘要

(1) 采用仅通过神经与身体相连的离体灌注兔耳方法,研究前列腺素拮抗剂多聚磷酸根皮苷(PPP)对缓激肽(B)和乙酰胆碱(ACh)致痛作用的影响。(2) 向兔耳动脉内注射B和ACh会引起麻醉动物全身血压反射性下降。PPP按剂量比例降低B的这种作用。ACh的作用仅在较高浓度的PPP作用下有小幅度降低,且该浓度高于抑制B作用所需的浓度。(3) 前列腺素E1(PGE1)经耳动脉内输注时,通过对血管周围痛觉感受器的致敏作用增强B和ACh的作用。PPP可降低或完全消除PGE1诱导的B和ACh作用增强。(4) 得出结论,PPP主要通过直接抑制内源性释放的E型前列腺素的致痛增强作用来降低B的作用。ACh的作用仅在高浓度PPP时稍有降低,可能是通过抑制ACh的作用而非仅极少量释放的前列腺素的致敏作用。在额外输注PGE1期间,PPP可降低或消除B和ACh的增强作用,这一事实进一步证明了PPP的前列腺素拮抗作用。

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