7-氧杂-13-前列腺炔酸的血管平滑肌活性

Vascular smooth muscle activity of 7-oxa-13-prostynoic acid.

作者信息

Ozaki N, Kohli J D, Goldberg L I, Fried J

出版信息

Blood Vessels. 1979;16(1):52-7. doi: 10.1159/000158190.

Abstract

The effects of 7-oxa-13-prostynoic acid (7-OPA), alone and as an antagonist of PGE2 and PGF2alpha, were investigaed in isolated rabbit aortic and canine renal arterial (diameter approximentaly 0.5 mm) strips. 7-OPA caused contractions in both preparations; threshold concentrations were 3- to 10-fold higher than the PGs and maximum contraction was 50-60%. In concentrations of 10(-5) M, 7-OPA inhibited contractions by PGF2alpha and PGE2. The same concentration of 7-OPA did not inhibit norepinephrine-induced contractions. These data indicate that 7-OPA is a partial agonist of PG receptors and produces its antagonism of PGE2 and PGF2alpha by that mechanism.

摘要

研究了7-氧杂-13-前列腺炔酸（7-OPA）单独以及作为前列腺素E2（PGE2）和前列腺素F2α（PGF2α）拮抗剂时，对离体兔主动脉条和犬肾动脉条（直径约0.5毫米）的作用。7-OPA在两种标本中均引起收缩；阈浓度比前列腺素高3至10倍，最大收缩为50%-60%。在10⁻⁵ M浓度下，7-OPA抑制PGF2α和PGE2引起的收缩。相同浓度的7-OPA不抑制去甲肾上腺素诱导的收缩。这些数据表明，7-OPA是PG受体的部分激动剂，并通过该机制对PGE2和PGF2α产生拮抗作用。