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聚磷酸根皮苷对前列腺素某些平滑肌作用的拮抗作用。

Antagonism of some smooth muscle actions of prostaglandins by polyphloretin phosphate.

作者信息

Eakins K E, Karim S M, Miller J D

出版信息

Br J Pharmacol. 1970 Jul;39(3):556-63. doi: 10.1111/j.1476-5381.1970.tb10363.x.

Abstract
  1. The antagonism of the smooth muscle stimulating actions of PGF(2a) and PGE(2) by polyphloretin phosphate (PPP) was studied on several isolated smooth muscle preparations and on the blood pressure of the anaesthetized rabbit.2. PPP (2.5-20 mug/ml) reversibly inhibited contractions of the jird colon produced by PGE(2) or PGF(2a); PGF(2a) was more readily antagonized than PGE(2).3. PPP (2.5-30 mug/ml) reversibly antagonized contractions produced by PGE(2) and PGF(2a) on the isolated rabbit jejunum and uterus. In these preparations PPP antagonized PGE(2) as readily as PGF(2a).4. It is concluded that PPP is a selective antagonist to the prostaglandins on these tissues, for contractions produced by other agonists, such as acetylcholine, angiotensin, 5-hydroxytryptamine and bradykinin were not reduced by concentrations of PPP which markedly antagonized responses to the prostaglandins.5. Intravenous injections of PPP (25-200 mg/kg) resulted in a variable antagonism to the fall in blood pressure produced by intravenous injections of PGF(2a) in the anaesthetized rabbit; vasodepressor responses produced by PGE(2) and acetylcholine were not antagonized.6. The mechanism of this antagonism by PPP is not clear and must await further investigation.
摘要
  1. 研究了聚磷酸根皮苷(PPP)对PGF(2α)和PGE(2)平滑肌刺激作用的拮抗作用,实验对象为几种离体平滑肌标本和麻醉兔的血压。

  2. PPP(2.5 - 20微克/毫升)可逆性抑制PGE(2)或PGF(2α)引起的沙鼠结肠收缩;PGF(2α)比PGE(2)更容易被拮抗。

  3. PPP(2.5 - 30微克/毫升)可逆性拮抗PGE(2)和PGF(2α)对离体兔空肠和子宫的收缩作用。在这些标本中,PPP对PGE(2)和PGF(2α)的拮抗作用相当。

  4. 得出结论,PPP在这些组织上是前列腺素的选择性拮抗剂,因为其他激动剂如乙酰胆碱、血管紧张素、5 - 羟色胺和缓激肽引起的收缩,不会被能显著拮抗前列腺素反应的PPP浓度所降低。

  5. 静脉注射PPP(25 - 200毫克/千克)对麻醉兔静脉注射PGF(2α)引起的血压下降产生不同程度的拮抗作用;PGE(2)和乙酰胆碱引起的血管降压反应未被拮抗。

  6. PPP这种拮抗作用的机制尚不清楚,必须等待进一步研究。

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The effects of prostaglandins on the intraocular pressure of the rabbit.前列腺素对兔眼内压的影响。
Br J Pharmacol. 1969 Sep;37(1):158-67. doi: 10.1111/j.1476-5381.1969.tb09533.x.

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